A Knowledge Based Approach to Drug Repurposing for Socially Important and Rare Diseases
RSF - DST Project # 16-45-02012 - INT/RUS/RSF/12

World wide approved drugs

Database contains information on about 4,108 medications, including the name of the drug, synonyms, the structural formula of the drug substance, pharmacotherapeutic fields and mechanisms of action.

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Structure Brand Name Target Pharmacotheraputic application Pharmacological class Approved link PDB link PASSOnline prediction
Structure Brand Name Target Pharmacotheraputic application Pharmacological class Approved link PDB link PASSOnline prediction
Click to view acalabrutinib Tyrosine-protein kinase BTK (Organism: Homo sapiens, class: Kinase, accessions: Q06187, gene: BTK, swissprot: BTK_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/210259s000lbl.pdf) Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/210259s000lbl.pdf) Cytoplasmic tyrosine-protein kinase BMX (Organism: Homo sapiens, class: Kinase, accessions: P51813, gene: BMX, swissprot: BMX_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/26641137) Tyrosine-protein kinase Tec (Organism: Homo sapiens, class: Kinase, accessions: P42680, gene: TEC, swissprot: TEC_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/26641137) Tyrosine-protein kinase TXK (Organism: Homo sapiens, class: Kinase, accessions: P42681, gene: TXK, swissprot: TXK_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/26641137) Receptor tyrosine-protein kinase erbB-4 (Organism: Homo sapiens, class: Kinase, accessions: Q15303, gene: ERBB4, swissprot: ERBB4_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/26641137) Acalabrutinib is a small-molecule inhibitor of BTK. Acalabrutinib and its active metabolite, ACP-5862, form a covalent bond with a cysteine residue in the BTK active site, leading to inhibition of BTK enzymatic activity. BTK is a signaling molecule of the B cell antigen receptor and cytokine receptor pathways. In B cells, BTK signaling results in activation of pathways necessary for B-cell proliferation, trafficking, chemotaxis, an adhesion. In nonclinical studies, acalabrutinib inhibited BTK mediated activation of downstream signaling proteins CD86 and CD69 and inhibited malignant B-cell proliferation and survival. Acalabrutinib is indicated for the treatment of adult patients with mantle cell lymphoma who have received at least one prior therapy. Kinase Inhibitor (Code: N0000175605) Tyrosine Kinase Inhibitors (Code: N0000020001) 2017-10-31 FDA
Click to view latanoprostene bunod Prostaglandin F2-alpha receptor (Organism: Homo sapiens, class: GPCR, accessions: P43088, gene: PTGFR, swissprot: PF2R_HUMAN) agonist (Source: ) Latanoprostene bunod is thought to lower intraocular pressure by increasing outflow of aqueous humor through both the trabecular meshwork and uveoscleral routes. Intraocular pressure is a major modifiable risk factor for glaucoma progression. Reduction of intraocular pressure reduces risk of glaucomatous visual field loss. 2017-11-02 FDA
Click to view letermovir DNA terminase complex (Organism: Human cytomegalovirus (strain Merlin), class: Enzyme, accessions: F5HC79|F5HCU8|F5HGI9, gene: TRM1|TRM2|TRM3, swissprot: TRM1_HCMVM|TRM2_HCMVM|TRM3_HCMVM) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209939Orig1s000,209940Orig1s000lbl.pdf) Letermovir inhibits the CMV DNA terminase complex (pUL51, pUL56, and pUL89) which is required for viral DNA processing and packaging. Biochemical characterization and electron microscopy demonstrated that letermovir affects the production of proper unit length genomes and interferes with virion maturation. Genotypic characterization of virus resistant to letermovir confirmed that letermovir targets the terminase complex. Cytomegalovirus DNA Terminase Complex Inhibitor (Code: N0000193800) DNA Terminase Complex Inhibitors (Code: N0000193801) Cytochrome P450 3A Inhibitors (Code: N0000190114) Organic Anion Transporting Polypeptide 1B1 Inhibitors (Code: N0000190107) Organic Anion Transporting Polypeptide 1B3 Inhibitors (Code: N0000190108) Cytochrome P450 2C8 Inhibitors (Code: N0000187062) Cytochrome P450 2C9 Inducers (Code: N0000185507) Cytochrome P450 2C19 Inducers (Code: N0000185607) 2017-11-08 FDA
Click to view vaborbactam Beta-lactamase (Organism: Klebsiella pneumoniae, class: Enzyme, accessions: Q93LQ9, gene: KPC-2, swissprot: Q93LQ9_KLEPN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/28848018) Beta-lactamase (Organism: Escherichia coli, class: Enzyme, accessions: Q9L5C7, gene: blaCTX-M-14, swissprot: Q9L5C7_ECOLX) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/28848018) Beta-lactamase (Organism: Escherichia coli, class: Enzyme, accessions: A8DZJ2, gene: blaSHV, swissprot: A8DZJ2_ECOLX) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/28848018) Vaborbactam is a non-suicidal beta-lactamase inhibitor that protects meropenem from degradation by certain serine beta-lactamases such as Klebsiella pneumoniae carbapenemase (KPC). Vaborbactam does not have any antibacterial activity. Vaborbactam does not decrease the activity of meropenem against meropenem-susceptible organisms. beta Lactamase Inhibitor (Code: N0000175930) beta Lactamase Inhibitors (Code: N0000000202) 2017-08-29 FDA 4D6
Click to view morinidazole Morinidazole is a nitroimidazole antibiotic indicated for the treatment of sensitive anaerobic bacterial infections including appendicitis and pelvic inflammatory disease caused by anaerobic bacteria. 2014-02-24 China Food and Drug Administration (CFDA)
Click to view forodesine Purine nucleoside phosphorylase (Organism: Homo sapiens, class: Enzyme, accessions: P00491, gene: PNP, swissprot: PNPH_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9628722) S-methyl-5'-thioadenosine phosphorylase (Organism: Homo sapiens, class: Enzyme, accessions: Q13126, gene: MTAP, swissprot: MTAP_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15163207) Forodesine is a transition state analogue that binds preferentially to and inhibits purine nucleotide phosphorylase (PNP), resulting in the accumulation of deoxyguanosine triphosphate and the subsequent inhibition of the enzyme ribonucleoside diphosphate reductase and DNA synthesis. This agent selectively causes apoptosis in stimulated or malignant T-lymphocytes. A transition state analogue is a substrate designed to mimic the properties or the geometry of the transition state of reaction. Forodesine is used for the treatment of different hematologic malignancies. 2017-03-30 PMDA
Click to view midostaurin Receptor-type tyrosine-protein kinase FLT3 (Organism: Homo sapiens, class: Kinase, accessions: P36888, gene: FLT3, swissprot: FLT3_HUMAN) inhibitor (Source: ) Activated CDC42 kinase 1 (Organism: Homo sapiens, class: Kinase, accessions: Q07912, gene: TNK2, swissprot: ACK1_HUMAN Vascular endothelial growth factor receptor 3 (Organism: Homo sapiens, class: Kinase, accessions: P35916, gene: FLT4, swissprot: VGFR3_HUMAN Serine/threonine-protein kinase PAK 3 (Organism: Homo sapiens, class: Kinase, accessions: O75914, gene: PAK3, swissprot: PAK3_HUMAN 3-phosphoinositide-dependent protein kinase 1 (Organism: Homo sapiens, class: Kinase, accessions: O15530, gene: PDPK1, swissprot: PDPK1_HUMAN Phosphorylase b kinase gamma catalytic chain, skeletal muscle/heart isoform (Organism: Homo sapiens, class: Kinase, accessions: Q16816, gene: PHKG1, swissprot: PHKG1_HUMAN Phosphatidylinositol 4-phosphate 5-kinase type-1 alpha (Organism: Homo sapiens, class: Kinase, accessions: Q99755, gene: PIP5K1A, swissprot: PI51A_HUMAN Ribosomal protein S6 kinase alpha-6 (Organism: Homo sapiens, class: Kinase, accessions: Q9UK32, gene: RPS6KA6, swissprot: KS6A6_HUMAN Myosin light chain kinase family member 4 (Organism: Homo sapiens, class: Kinase, accessions: Q86YV6, gene: MYLK4, swissprot: MYLK4_HUMAN Vascular endothelial growth factor receptor 2 (Organism: Homo sapiens, class: Kinase, accessions: P35968, gene: KDR, swissprot: VGFR2_HUMAN Tyrosine-protein kinase Yes (Organism: Homo sapiens, class: Kinase, accessions: P07947, gene: YES1, swissprot: YES_HUMAN Serine/threonine-protein kinase 25 (Organism: Homo sapiens, class: Kinase, accessions: O00506, gene: STK25, swissprot: STK25_HUMAN Tyrosine-protein kinase ZAP-70 (Organism: Homo sapiens, class: Kinase, accessions: P43403, gene: ZAP70, swissprot: ZAP70_HUMAN Phosphatidylinositol 5-phosphate 4-kinase type-2 beta (Organism: Homo sapiens, class: Kinase, accessions: P78356, gene: PIP4K2B, swissprot: PI42B_HUMAN cAMP-dependent protein kinase catalytic subunit beta (Organism: Homo sapiens, class: Kinase, accessions: P22694, gene: PRKACB, swissprot: KAPCB_HUMAN cAMP-dependent protein kinase catalytic subunit PRKX (Organism: Homo sapiens, class: Unclassified, accessions: P51817, gene: PRKX, swissprot: PRKX_HUMAN Protein-tyrosine kinase 2-beta (Organism: Homo sapiens, class: Kinase, accessions: Q14289, gene: PTK2B, swissprot: FAK2_HUMAN Dual specificity protein kinase CLK1 (Organism: Homo sapiens, class: Kinase, accessions: P49759, gene: CLK1, swissprot: CLK1_HUMAN Tyrosine-protein kinase CSK (Organism: Homo sapiens, class: Kinase, accessions: P41240, gene: CSK, swissprot: CSK_HUMAN Tyrosine-protein kinase receptor Tie-1 (Organism: Homo sapiens, class: Kinase, accessions: P35590, gene: TIE1, swissprot: TIE1_HUMAN Angiopoietin-1 receptor (Organism: Homo sapiens, class: Kinase, accessions: Q02763, gene: TEK, swissprot: TIE2_HUMAN TRAF2 and NCK-interacting protein kinase (Organism: Homo sapiens, class: Kinase, accessions: Q9UKE5, gene: TNIK, swissprot: TNIK_HUMAN High affinity nerve growth factor receptor (Organism: Homo sapiens, class: Kinase, accessions: P04629, gene: NTRK1, swissprot: NTRK1_HUMAN BDNF/NT-3 growth factors receptor (Organism: Homo sapiens, class: Kinase, accessions: Q16620, gene: NTRK2, swissprot: NTRK2_HUMAN NT-3 growth factor receptor (Organism: Homo sapiens, class: Kinase, accessions: Q16288, gene: NTRK3, swissprot: NTRK3_HUMAN Dual specificity protein kinase TTK (Organism: Homo sapiens, class: Kinase, accessions: P33981, gene: TTK, swissprot: TTK_HUMAN Casein kinase II subunit alpha (Organism: Homo sapiens, class: Kinase, accessions: P68400, gene: CSNK2A1, swissprot: CSK21_HUMAN Death-associated protein kinase 2 (Organism: Homo sapiens, class: Kinase, accessions: Q9UIK4, gene: DAPK2, swissprot: DAPK2_HUMAN Serine/threonine-protein kinase 17B (Organism: Homo sapiens, class: Kinase, accessions: O94768, gene: STK17B, swissprot: ST17B_HUMAN Dual specificity tyrosine-phosphorylation-regulated kinase 1B (Organism: Homo sapiens, class: Kinase, accessions: Q9Y463, gene: DYRK1B, swissprot: DYR1B_HUMAN Glycogen synthase kinase-3 alpha (Organism: Homo sapiens, class: Kinase, accessions: P49840, gene: GSK3A, swissprot: GSK3A_HUMAN Glycogen synthase kinase-3 beta (Organism: Homo sapiens, class: Kinase, accessions: P49841, gene: GSK3B, swissprot: GSK3B_HUMAN Inhibitor of nuclear factor kappa-B kinase subunit epsilon (Organism: Homo sapiens, class: Kinase, accessions: Q14164, gene: IKBKE, swissprot: IKKE_HUMAN Non-receptor tyrosine-protein kinase TYK2 (Organism: Homo sapiens, class: Kinase, accessions: P29597, gene: TYK2, swissprot: TYK2_HUMAN Mitogen-activated protein kinase 8 (Organism: Homo sapiens, class: Kinase, accessions: P45983, gene: MAPK8, swissprot: MK08_HUMAN Serine/threonine-protein kinase STK11 (Organism: Homo sapiens, class: Kinase, accessions: Q15831, gene: STK11, swissprot: STK11_HUMAN MAP/microtubule affinity-regulating kinase 3 (Organism: Homo sapiens, class: Kinase, accessions: P27448, gene: MARK3, swissprot: MARK3_HUMAN Dual specificity mitogen-activated protein kinase kinase 3 (Organism: Homo sapiens, class: Kinase, accessions: P46734, gene: MAP2K3, swissprot: MP2K3_HUMAN Maternal embryonic leucine zipper kinase (Organism: Homo sapiens, class: Kinase, accessions: Q14680, gene: MELK, swissprot: MELK_HUMAN AP2-associated protein kinase 1 (Organism: Homo sapiens, class: Kinase, accessions: Q2M2I8, gene: AAK1, swissprot: AAK1_HUMAN Serine/threonine-protein kinase 4 (Organism: Homo sapiens, class: Kinase, accessions: Q13043, gene: STK4, swissprot: STK4_HUMAN Eukaryotic translation initiation factor 2-alpha kinase 4 (Organism: Homo sapiens, class: Kinase, accessions: Q9P2K8, gene: EIF2AK4, swissprot: E2AK4_HUMAN Tyrosine-protein kinase HCK (Organism: Homo sapiens, class: Kinase, accessions: P08631, gene: HCK, swissprot: HCK_HUMAN Tyrosine-protein kinase ABL1 (Organism: Homo sapiens, class: Kinase, accessions: P00519, gene: ABL1, swissprot: ABL1_HUMAN Interleukin-1 receptor-associated kinase 3 (Organism: Homo sapiens, class: Kinase, accessions: Q9Y616, gene: IRAK3, swissprot: IRAK3_HUMAN Tyrosine-protein kinase JAK2 (Organism: Homo sapiens, class: Kinase, accessions: O60674, gene: JAK2, swissprot: JAK2_HUMAN Tyrosine-protein kinase JAK3 (Organism: Homo sapiens, class: Kinase, accessions: P52333, gene: JAK3, swissprot: JAK3_HUMAN Mitogen-activated protein kinase 10 (Organism: Homo sapiens, class: Kinase, accessions: P53779, gene: MAPK10, swissprot: MK10_HUMAN Mast/stem cell growth factor receptor Kit (Organism: Homo sapiens, class: Kinase, accessions: P10721, gene: KIT, swissprot: KIT_HUMAN Serine/threonine-protein kinase RIO1 (Organism: Homo sapiens, class: Kinase, accessions: Q9BRS2, gene: RIOK1, swissprot: RIOK1_HUMAN Serine/threonine-protein kinase RIO3 (Organism: Homo sapiens, class: Kinase, accessions: O14730, gene: RIOK3, swissprot: RIOK3_HUMAN Serine/threonine-protein kinase SIK2 (Organism: Homo sapiens, class: Kinase, accessions: Q9H0K1, gene: SIK2, swissprot: SIK2_HUMAN SRSF protein kinase 1 (Organism: Homo sapiens, class: Kinase, accessions: Q96SB4, gene: SRPK1, swissprot: SRPK1_HUMAN SRSF protein kinase 2 (Organism: Homo sapiens, class: Kinase, accessions: P78362, gene: SRPK2, swissprot: SRPK2_HUMAN Non-receptor tyrosine-protein kinase TNK1 (Organism: Homo sapiens, class: Kinase, accessions: Q13470, gene: TNK1, swissprot: TNK1_HUMAN Testis-specific serine/threonine-protein kinase 1 (Organism: Homo sapiens, class: Kinase, accessions: Q9BXA7, gene: TSSK1B, swissprot: TSSK1_HUMAN Tyrosine-protein kinase Fyn (Organism: Homo sapiens, class: Kinase, accessions: P06241, gene: FYN, swissprot: FYN_HUMAN Cyclin-G-associated kinase (Organism: Homo sapiens, class: Kinase, accessions: O14976, gene: GAK, swissprot: GAK_HUMAN ALK tyrosine kinase receptor (Organism: Homo sapiens, class: Kinase, accessions: Q9UM73, gene: ALK, swissprot: ALK_HUMAN 5'-AMP-activated protein kinase catalytic subunit alpha-1 (Organism: Homo sapiens, class: Kinase, accessions: Q13131, gene: PRKAA1, swissprot: AAPK1_HUMAN 5'-AMP-activated protein kinase catalytic subunit alpha-2 (Organism: Homo sapiens, class: Kinase, accessions: P54646, gene: PRKAA2, swissprot: AAPK2_HUMAN Epithelial discoidin domain-containing receptor 1 (Organism: Homo sapiens, class: Kinase, accessions: Q08345, gene: DDR1, swissprot: DDR1_HUMAN Myotonin-protein kinase (Organism: Homo sapiens, class: Kinase, accessions: Q09013, gene: DMPK, swissprot: DMPK_HUMAN RAC-alpha serine/threonine-protein kinase (Organism: Homo sapiens, class: Kinase, accessions: P31749, gene: AKT1, swissprot: AKT1_HUMAN RAC-beta serine/threonine-protein kinase (Organism: Homo sapiens, class: Kinase, accessions: P31751, gene: AKT2, swissprot: AKT2_HUMAN Serine/threonine-protein kinase LATS1 (Organism: Homo sapiens, class: Kinase, accessions: O95835, gene: LATS1, swissprot: LATS1_HUMAN Serine/threonine-protein kinase LATS2 (Organism: Homo sapiens, class: Kinase, accessions: Q9NRM7, gene: LATS2, swissprot: LATS2_HUMAN Tyrosine-protein kinase Lck (Organism: Homo sapiens, class: Kinase, accessions: P06239, gene: LCK, swissprot: LCK_HUMAN Serine/threonine-protein kinase 10 (Organism: Homo sapiens, class: Kinase, accessions: O94804, gene: STK10, swissprot: STK10_HUMAN Leukocyte tyrosine kinase receptor (Organism: Homo sapiens, class: Kinase, accessions: P29376, gene: LTK, swissprot: LTK_HUMAN Tyrosine-protein kinase Lyn (Organism: Homo sapiens, class: Kinase, accessions: P07948, gene: LYN, swissprot: LYN_HUMAN Serine/threonine-protein kinase 17A (Organism: Homo sapiens, class: Kinase, accessions: Q9UEE5, gene: STK17A, swissprot: ST17A_HUMAN Epidermal growth factor receptor (Organism: Homo sapiens, class: Kinase, accessions: P00533, gene: EGFR, swissprot: EGFR_HUMAN NUAK family SNF1-like kinase 1 (Organism: Homo sapiens, class: Kinase, accessions: O60285, gene: NUAK1, swissprot: NUAK1_HUMAN Aurora kinase A (Organism: Homo sapiens, class: Kinase, accessions: O14965, gene: AURKA, swissprot: AURKA_HUMAN Platelet-derived growth factor receptor alpha (Organism: Homo sapiens, class: Kinase, accessions: P16234, gene: PDGFRA, swissprot: PGFRA_HUMAN Platelet-derived growth factor receptor beta (Organism: Homo sapiens, class: Kinase, accessions: P09619, gene: PDGFRB, swissprot: PGFRB_HUMAN Phosphorylase b kinase gamma catalytic chain, liver/testis isoform (Organism: Homo sapiens, class: Kinase, accessions: P15735, gene: PHKG2, swissprot: PHKG2_HUMAN Serine/threonine-protein kinase pim-1 (Organism: Homo sapiens, class: Kinase, accessions: P11309, gene: PIM1, swissprot: PIM1_HUMAN Serine/threonine-protein kinase pim-3 (Organism: Homo sapiens, class: Kinase, accessions: Q86V86, gene: PIM3, swissprot: PIM3_HUMAN cAMP-dependent protein kinase catalytic subunit alpha (Organism: Homo sapiens, class: Kinase, accessions: P17612, gene: PRKACA, swissprot: KAPCA_HUMAN Mitogen-activated protein kinase kinase kinase kinase 1 (Organism: Homo sapiens, class: Kinase, accessions: Q92918, gene: MAP4K1, swissprot: M4K1_HUMAN Mitogen-activated protein kinase kinase kinase kinase 3 (Organism: Homo sapiens, class: Kinase, accessions: Q8IVH8, gene: MAP4K3, swissprot: M4K3_HUMAN Aurora kinase B (Organism: Homo sapiens, class: Kinase, accessions: Q96GD4, gene: AURKB, swissprot: AURKB_HUMAN Tyrosine-protein kinase receptor UFO (Organism: Homo sapiens, class: Kinase, accessions: P30530, gene: AXL, swissprot: UFO_HUMAN BMP-2-inducible protein kinase (Organism: Homo sapiens, class: Kinase, accessions: Q9NSY1, gene: BMP2K, swissprot: BMP2K_HUMAN Tyrosine-protein kinase Blk (Organism: Homo sapiens, class: Kinase, accessions: P51451, gene: BLK, swissprot: BLK_HUMAN Serine/threonine-protein kinase BRSK1 (Organism: Homo sapiens, class: Kinase, accessions: Q8TDC3, gene: BRSK1, swissprot: BRSK1_HUMAN Calcium/calmodulin-dependent protein kinase type 1D (Organism: Homo sapiens, class: Kinase, accessions: Q8IU85, gene: CAMK1D, swissprot: KCC1D_HUMAN Calcium/calmodulin-dependent protein kinase type 1G (Organism: Homo sapiens, class: Kinase, accessions: Q96NX5, gene: CAMK1G, swissprot: KCC1G_HUMAN Mitogen-activated protein kinase kinase kinase kinase 4 (Organism: Homo sapiens, class: Kinase, accessions: O95819, gene: MAP4K4, swissprot: M4K4_HUMAN Mitogen-activated protein kinase kinase kinase kinase 5 (Organism: Homo sapiens, class: Kinase, accessions: Q9Y4K4, gene: MAP4K5, swissprot: M4K5_HUMAN Serine/threonine-protein kinase MARK1 (Organism: Homo sapiens, class: Kinase, accessions: Q9P0L2, gene: MARK1, swissprot: MARK1_HUMAN Serine/threonine-protein kinase MARK2 (Organism: Homo sapiens, class: Kinase, accessions: Q7KZI7, gene: MARK2, swissprot: MARK2_HUMAN MAP/microtubule affinity-regulating kinase 4 (Organism: Homo sapiens, class: Kinase, accessions: Q96L34, gene: MARK4, swissprot: MARK4_HUMAN Dual specificity mitogen-activated protein kinase kinase 4 (Organism: Homo sapiens, class: Kinase, accessions: P45985, gene: MAP2K4, swissprot: MP2K4_HUMAN Tyrosine-protein kinase Mer (Organism: Homo sapiens, class: Kinase, accessions: Q12866, gene: MERTK, swissprot: MERTK_HUMAN Hepatocyte growth factor receptor (Organism: Homo sapiens, class: Kinase, accessions: P08581, gene: MET, swissprot: MET_HUMAN Calcium/calmodulin-dependent protein kinase type II subunit alpha (Organism: Homo sapiens, class: Kinase, accessions: Q9UQM7, gene: CAMK2A, swissprot: KCC2A_HUMAN Calcium/calmodulin-dependent protein kinase type II subunit beta (Organism: Homo sapiens, class: Kinase, accessions: Q13554, gene: CAMK2B, swissprot: KCC2B_HUMAN Calcium/calmodulin-dependent protein kinase type II subunit delta (Organism: Homo sapiens, class: Kinase, accessions: Q13557, gene: CAMK2D, swissprot: KCC2D_HUMAN Calcium/calmodulin-dependent protein kinase type II subunit gamma (Organism: Homo sapiens, class: Kinase, accessions: Q13555, gene: CAMK2G, swissprot: KCC2G_HUMAN Calcium/calmodulin-dependent protein kinase kinase 1 (Organism: Homo sapiens, class: Kinase, accessions: Q8N5S9, gene: CAMKK1, swissprot: KKCC1_HUMAN Calcium/calmodulin-dependent protein kinase kinase 2 (Organism: Homo sapiens, class: Kinase, accessions: Q96RR4, gene: CAMKK2, swissprot: KKCC2_HUMAN Cyclin-dependent kinase 19 (Organism: Homo sapiens, class: Kinase, accessions: Q9BWU1, gene: CDK19, swissprot: CDK19_HUMAN MAP kinase-interacting serine/threonine-protein kinase 2 (Organism: Homo sapiens, class: Kinase, accessions: Q9HBH9, gene: MKNK2, swissprot: MKNK2_HUMAN Mitogen-activated protein kinase kinase kinase 9 (Organism: Homo sapiens, class: Kinase, accessions: P80192, gene: MAP3K9, swissprot: M3K9_HUMAN Mitogen-activated protein kinase kinase kinase 10 (Organism: Homo sapiens, class: Kinase, accessions: Q02779, gene: MAP3K10, swissprot: M3K10_HUMAN Mitogen-activated protein kinase kinase kinase 11 (Organism: Homo sapiens, class: Kinase, accessions: Q16584, gene: MAP3K11, swissprot: M3K11_HUMAN Serine/threonine-protein kinase 3 (Organism: Homo sapiens, class: Kinase, accessions: Q13188, gene: STK3, swissprot: STK3_HUMAN Myosin light chain kinase, smooth muscle (Organism: Homo sapiens, class: Kinase, accessions: Q15746, gene: MYLK, swissprot: MYLK_HUMAN Serine/threonine-protein kinase Chk1 (Organism: Homo sapiens, class: Kinase, accessions: O14757, gene: CHEK1, swissprot: CHK1_HUMAN Dual specificity protein kinase CLK2 (Organism: Homo sapiens, class: Kinase, accessions: P49760, gene: CLK2, swissprot: CLK2_HUMAN Dual specificity protein kinase CLK4 (Organism: Homo sapiens, class: Kinase, accessions: Q9HAZ1, gene: CLK4, swissprot: CLK4_HUMAN Macrophage colony-stimulating factor 1 receptor (Organism: Homo sapiens, class: Kinase, accessions: P07333, gene: CSF1R, swissprot: CSF1R_HUMAN Death-associated protein kinase 1 (Organism: Homo sapiens, class: Kinase, accessions: P53355, gene: DAPK1, swissprot: DAPK1_HUMAN Death-associated protein kinase 3 (Organism: Homo sapiens, class: Kinase, accessions: O43293, gene: DAPK3, swissprot: DAPK3_HUMAN Serine/threonine-protein kinase PAK 1 (Organism: Homo sapiens, class: Kinase, accessions: Q13153, gene: PAK1, swissprot: PAK1_HUMAN Serine/threonine-protein kinase PAK 2 (Organism: Homo sapiens, class: Kinase, accessions: Q13177, gene: PAK2, swissprot: PAK2_HUMAN Tyrosine-protein kinase FRK (Organism: Homo sapiens, class: Kinase, accessions: P42685, gene: FRK, swissprot: FRK_HUMAN Aurora kinase C (Organism: Homo sapiens, class: Kinase, accessions: Q9UQB9, gene: AURKC, swissprot: AURKC_HUMAN Serine/threonine-protein kinase BRSK2 (Organism: Homo sapiens, class: Kinase, accessions: Q8IWQ3, gene: BRSK2, swissprot: BRSK2_HUMAN Calcium/calmodulin-dependent protein kinase type 1 (Organism: Homo sapiens, class: Kinase, accessions: Q14012, gene: CAMK1, swissprot: KCC1A_HUMAN STE20-like serine/threonine-protein kinase (Organism: Homo sapiens, class: Kinase, accessions: Q9H2G2, gene: SLK, swissprot: SLK_HUMAN NUAK family SNF1-like kinase 2 (Organism: Homo sapiens, class: Kinase, accessions: Q9H093, gene: NUAK2, swissprot: NUAK2_HUMAN Serine/threonine-protein kinase SIK1 (Organism: Homo sapiens, class: Kinase, accessions: P57059, gene: SIK1, swissprot: SIK1_HUMAN Proto-oncogene tyrosine-protein kinase Src (Organism: Homo sapiens, class: Kinase, accessions: P12931, gene: SRC, swissprot: SRC_HUMAN Serine/threonine-protein kinase 16 (Organism: Homo sapiens, class: Kinase, accessions: O75716, gene: STK16, swissprot: STK16_HUMAN Tyrosine-protein kinase SYK (Organism: Homo sapiens, class: Kinase, accessions: P43405, gene: SYK, swissprot: KSYK_HUMAN Serine/threonine-protein kinase N1 (Organism: Homo sapiens, class: Kinase, accessions: Q16512, gene: PKN1, swissprot: PKN1_HUMAN Serine/threonine-protein kinase N2 (Organism: Homo sapiens, class: Kinase, accessions: Q16513, gene: PKN2, swissprot: PKN2_HUMAN Serine/threonine-protein kinase PLK4 (Organism: Homo sapiens, class: Kinase, accessions: O00444, gene: PLK4, swissprot: PLK4_HUMAN Protein kinase C delta type (Organism: Homo sapiens, class: Kinase, accessions: Q05655, gene: PRKCD, swissprot: KPCD_HUMAN Protein kinase C epsilon type (Organism: Homo sapiens, class: Kinase, accessions: Q02156, gene: PRKCE, swissprot: KPCE_HUMAN Protein kinase C eta type (Organism: Homo sapiens, class: Kinase, accessions: P24723, gene: PRKCH, swissprot: KPCL_HUMAN Protein kinase C theta type (Organism: Homo sapiens, class: Kinase, accessions: Q04759, gene: PRKCQ, swissprot: KPCT_HUMAN Tubulin alpha-1A chain (Organism: Rattus norvegicus, class: Structural, accessions: P68370, gene: Tuba1a, swissprot: TBA1A_RAT Tyrosine-protein kinase Fer (Organism: Homo sapiens, class: Kinase, accessions: P16591, gene: FER, swissprot: FER_HUMAN Serine/threonine-protein kinase D2 (Organism: Homo sapiens, class: Kinase, accessions: Q9BZL6, gene: PRKD2, swissprot: KPCD2_HUMAN Serine/threonine-protein kinase D3 (Organism: Homo sapiens, class: Kinase, accessions: O94806, gene: PRKD3, swissprot: KPCD3_HUMAN cGMP-dependent protein kinase 1 (Organism: Homo sapiens, class: Kinase, accessions: Q13976, gene: PRKG1, swissprot: KGP1_HUMAN cGMP-dependent protein kinase 2 (Organism: Homo sapiens, class: Kinase, accessions: Q13237, gene: PRKG2, swissprot: KGP2_HUMAN Interferon-induced, double-stranded RNA-activated protein kinase (Organism: Homo sapiens, class: Kinase, accessions: P19525, gene: EIF2AK2, swissprot: E2AK2_HUMAN Proto-oncogene tyrosine-protein kinase receptor Ret (Organism: Homo sapiens, class: Kinase, accessions: P07949, gene: RET, swissprot: RET_HUMAN Fibroblast growth factor receptor 1 (Organism: Homo sapiens, class: Kinase, accessions: P11362, gene: FGFR1, swissprot: FGFR1_HUMAN Fibroblast growth factor receptor 2 (Organism: Homo sapiens, class: Kinase, accessions: P21802, gene: FGFR2, swissprot: FGFR2_HUMAN Fibroblast growth factor receptor 3 (Organism: Homo sapiens, class: Kinase, accessions: P22607, gene: FGFR3, swissprot: FGFR3_HUMAN Tyrosine-protein kinase Fgr (Organism: Homo sapiens, class: Kinase, accessions: P09769, gene: FGR, swissprot: FGR_HUMAN Vascular endothelial growth factor receptor 1 (Organism: Homo sapiens, class: Kinase, accessions: P17948, gene: FLT1, swissprot: VGFR1_HUMAN Proto-oncogene tyrosine-protein kinase ROS (Organism: Homo sapiens, class: Kinase, accessions: P08922, gene: ROS1, swissprot: ROS1_HUMAN Ribosomal protein S6 kinase alpha-1 (Organism: Homo sapiens, class: Kinase, accessions: Q15418, gene: RPS6KA1, swissprot: KS6A1_HUMAN Ribosomal protein S6 kinase alpha-2 (Organism: Homo sapiens, class: Kinase, accessions: Q15349, gene: RPS6KA2, swissprot: KS6A2_HUMAN Ribosomal protein S6 kinase alpha-3 (Organism: Homo sapiens, class: Kinase, accessions: P51812, gene: RPS6KA3, swissprot: KS6A3_HUMAN Ribosomal protein S6 kinase alpha-4 (Organism: Homo sapiens, class: Kinase, accessions: O75676, gene: RPS6KA4, swissprot: KS6A4_HUMAN Ribosomal protein S6 kinase alpha-5 (Organism: Homo sapiens, class: Kinase, accessions: O75582, gene: RPS6KA5, swissprot: KS6A5_HUMAN SRSF protein kinase 3 (Organism: Homo sapiens, class: Kinase, accessions: Q9UPE1, gene: SRPK3, swissprot: SRPK3_HUMAN Dual specificity tyrosine-phosphorylation-regulated kinase 1A (Organism: Homo sapiens, class: Kinase, accessions: Q13627, gene: DYRK1A, swissprot: DYR1A_HUMAN Ephrin type-B receptor 6 (Organism: Homo sapiens, class: Kinase, accessions: O15197, gene: EPHB6, swissprot: EPHB6_HUMAN Receptor tyrosine-protein kinase erbB-4 (Organism: Homo sapiens, class: Kinase, accessions: Q15303, gene: ERBB4, swissprot: ERBB4_HUMAN Serine/threonine-protein kinase/endoribonuclease IRE1 (Organism: Homo sapiens, class: Kinase, accessions: O75460, gene: ERN1, swissprot: ERN1_HUMAN Rhodopsin kinase (Organism: Homo sapiens, class: Kinase, accessions: Q15835, gene: GRK1, swissprot: RK_HUMAN G protein-coupled receptor kinase 4 (Organism: Homo sapiens, class: Kinase, accessions: P32298, gene: GRK4, swissprot: GRK4_HUMAN G protein-coupled receptor kinase 7 (Organism: Homo sapiens, class: Kinase, accessions: Q8WTQ7, gene: GRK7, swissprot: GRK7_HUMAN Homeodomain-interacting protein kinase 2 (Organism: Homo sapiens, class: Kinase, accessions: Q9H2X6, gene: HIPK2, swissprot: HIPK2_HUMAN Homeodomain-interacting protein kinase 3 (Organism: Homo sapiens, class: Kinase, accessions: Q9H422, gene: HIPK3, swissprot: HIPK3_HUMAN Homeodomain-interacting protein kinase 4 (Organism: Homo sapiens, class: Kinase, accessions: Q8NE63, gene: HIPK4, swissprot: HIPK4_HUMAN Hormonally up-regulated neu tumor-associated kinase (Organism: Homo sapiens, class: Kinase, accessions: P57058, gene: HUNK, swissprot: HUNK_HUMAN Inhibitor of nuclear factor kappa-B kinase subunit alpha (Organism: Homo sapiens, class: Kinase, accessions: O15111, gene: CHUK, swissprot: IKKA_HUMAN Tyrosine-protein kinase JAK1 (Organism: Homo sapiens, class: Kinase, accessions: P23458, gene: JAK1, swissprot: JAK1_HUMAN Mitogen-activated protein kinase kinase kinase 13 (Organism: Homo sapiens, class: Kinase, accessions: O43283, gene: MAP3K13, swissprot: M3K13_HUMAN Mitogen-activated protein kinase kinase kinase 2 (Organism: Homo sapiens, class: Kinase, accessions: Q9Y2U5, gene: MAP3K2, swissprot: M3K2_HUMAN Mitogen-activated protein kinase kinase kinase 3 (Organism: Homo sapiens, class: Kinase, accessions: Q99759, gene: MAP3K3, swissprot: M3K3_HUMAN Mitogen-activated protein kinase kinase kinase kinase 2 (Organism: Homo sapiens, class: Kinase, accessions: Q12851, gene: MAP4K2, swissprot: M4K2_HUMAN Misshapen-like kinase 1 (Organism: Homo sapiens, class: Kinase, accessions: Q8N4C8, gene: MINK1, swissprot: MINK1_HUMAN Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit beta (Organism: Homo sapiens, class: Kinase, accessions: O00750, gene: PIK3C2B, swissprot: P3C2B_HUMAN Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit gamma (Organism: Homo sapiens, class: Kinase, accessions: O75747, gene: PIK3C2G, swissprot: P3C2G_HUMAN Protein kinase C alpha type (Organism: Homo sapiens, class: Kinase, accessions: P17252, gene: PRKCA, swissprot: KPCA_HUMAN U4/U6 small nuclear ribonucleoprotein Prp4 (Organism: Homo sapiens, class: Unclassified, accessions: O43172, gene: PRPF4, swissprot: PRP4_HUMAN Serine/threonine-protein kinase SIK3 (Organism: Homo sapiens, class: Kinase, accessions: Q9Y2K2, gene: SIK3, swissprot: SIK3_HUMAN Serine/threonine-protein kinase RIO2 (Organism: Homo sapiens, class: Kinase, accessions: Q9BVS4, gene: RIOK2, swissprot: RIOK2_HUMAN Rho-associated protein kinase 1 (Organism: Homo sapiens, class: Kinase, accessions: Q13464, gene: ROCK1, swissprot: ROCK1_HUMAN Rho-associated protein kinase 2 (Organism: Homo sapiens, class: Kinase, accessions: O75116, gene: ROCK2, swissprot: ROCK2_HUMAN Mitogen-activated protein kinase kinase kinase 7 (Organism: Homo sapiens, class: Kinase, accessions: O43318, gene: MAP3K7, swissprot: M3K7_HUMAN Serine/threonine-protein kinase TBK1 (Organism: Homo sapiens, class: Kinase, accessions: Q9UHD2, gene: TBK1, swissprot: TBK1_HUMAN Tankyrase-2 (Organism: Homo sapiens, class: Enzyme, accessions: Q9H2K2, gene: TNKS2, swissprot: TNKS2_HUMAN Serine/threonine-protein kinase ULK3 (Organism: Homo sapiens, class: Kinase, accessions: Q6PHR2, gene: ULK3, swissprot: ULK3_HUMAN Mitogen-activated protein kinase kinase kinase 19 (Organism: Homo sapiens, class: Kinase, accessions: Q56UN5, gene: MAP3K19, swissprot: M3K19_HUMAN Serine/threonine-protein kinase 32A (Organism: Homo sapiens, class: Kinase, accessions: Q8WU08, gene: STK32A, swissprot: ST32A_HUMAN Inhibitor of nuclear factor kappa-B kinase subunit beta (Organism: Homo sapiens, class: Kinase, accessions: O14920, gene: IKBKB, swissprot: IKKB_HUMAN Dual specificity mitogen-activated protein kinase kinase 6 (Organism: Homo sapiens, class: Kinase, accessions: P52564, gene: MAP2K6, swissprot: MP2K6_HUMAN Ribosomal protein S6 kinase beta-1 (Organism: Homo sapiens, class: Kinase, accessions: P23443, gene: RPS6KB1, swissprot: KS6B1_HUMAN Wee1-like protein kinase (Organism: Homo sapiens, class: Kinase, accessions: P30291, gene: WEE1, swissprot: WEE1_HUMAN Serine/threonine-protein kinase PRP4 homolog (Organism: Homo sapiens, class: Kinase, accessions: Q13523, gene: PRPF4B, swissprot: PRP4B_HUMAN Dual specificity protein kinase CLK3 (Organism: Homo sapiens, class: Kinase, accessions: P49761, gene: CLK3, swissprot: CLK3_HUMAN RAC-gamma serine/threonine-protein kinase (Organism: Homo sapiens, class: Kinase, accessions: Q9Y243, gene: AKT3, swissprot: AKT3_HUMAN Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (Organism: Homo sapiens, class: Kinase, accessions: P42336, gene: PIK3CA, swissprot: PK3CA_HUMAN Serine/threonine-protein kinase pim-2 (Organism: Homo sapiens, class: Kinase, accessions: Q9P1W9, gene: PIM2, swissprot: PIM2_HUMAN Serine/threonine-protein kinase Sgk3 (Organism: Homo sapiens, class: Kinase, accessions: Q96BR1, gene: SGK3, swissprot: SGK3_HUMAN Serine/threonine-protein kinase ICK (Organism: Homo sapiens, class: Kinase, accessions: Q9UPZ9, gene: ICK, swissprot: ICK_HUMAN Microtubule-associated serine/threonine-protein kinase 1 (Organism: Homo sapiens, class: Kinase, accessions: Q9Y2H9, gene: MAST1, swissprot: MAST1_HUMAN Serine/threonine-protein kinase 33 (Organism: Homo sapiens, class: Kinase, accessions: Q9BYT3, gene: STK33, swissprot: STK33_HUMAN Mitogen-activated protein kinase 9 (Organism: Homo sapiens, class: Kinase, accessions: P45984, gene: MAPK9, swissprot: MK09_HUMAN Myosin light chain kinase 3 (Organism: Homo sapiens, class: Kinase, accessions: Q32MK0, gene: MYLK3, swissprot: MYLK3_HUMAN Leucine-rich repeat serine/threonine-protein kinase 2 (Organism: Homo sapiens, class: Kinase, accessions: Q5S007, gene: LRRK2, swissprot: LRRK2_HUMAN Dual serine/threonine and tyrosine protein kinase (Organism: Homo sapiens, class: Kinase, accessions: Q6XUX3, gene: DSTYK, swissprot: DUSTY_HUMAN Calcium-dependent protein kinase 1 (Organism: Plasmodium falciparum, class: Kinase, accessions: P62344, gene: CPK1, swissprot: CDPK1_PLAF7 Midostaurin is a small molecule that inhibits multiple receptor tyrosine kinases. In vitro biochemical or cellular assays have shown that midostaurin or its major human active metabolites CGP62221 and CGP52421 inhibit the activity of wild type FLT3, FLT3 mutant kinases (ITD and TKD), KIT (wild type and D816V mutant), PDGFR-alfa/beta, VEGFR2, as well as members of the serine/threonine kinase PKC (protein kinase C) family. Midostaurin demonstrated the ability to inhibit FLT3 receptor signaling and cell proliferation, and it induced apoptosis in leukemic cells expressing ITD and TKD mutant FLT3 receptors or overexpressing wild type FLT3 and PDGF receptors. Midostaurin also demonstrated the ability to inhibit KIT signaling, cell proliferation and histamine release and induce apoptosis in mast cells. antineoplastic agent (Code: CHEBI:35610) Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Protein Kinase Inhibitors (Code: D047428) Kinase Inhibitor (Code: N0000175605) Receptor Tyrosine Kinase Inhibitors (Code: N0000020000) 2017-04-28 FDA 2K2
Click to view macimorelin Growth hormone secretagogue receptor type 1 (Organism: Homo sapiens, class: GPCR, accessions: Q92847, gene: GHSR, swissprot: GHSR_HUMAN) agonist (Source: ) Macimorelin stimulates GH release by activating growth hormone secretagogue receptors present in the pituitary and hypothalamus. Growth Hormone Secretagogue Receptor Agonist (Code: N0000193785) Growth Hormone Secretagogue Receptor Agonists (Code: N0000193786) 2017-12-20 FDA
Click to view baricitinib Tyrosine-protein kinase JAK1 (Organism: Homo sapiens, class: Kinase, accessions: P23458, gene: JAK1, swissprot: JAK1_HUMAN) inhibitor (Source: http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Product_Information/human/004085/WC500223723.pdf) Tyrosine-protein kinase JAK2 (Organism: Homo sapiens, class: Kinase, accessions: O60674, gene: JAK2, swissprot: JAK2_HUMAN) inhibitor (Source: http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Product_Information/human/004085/WC500223723.pdf) Non-receptor tyrosine-protein kinase TYK2 (Organism: Homo sapiens, class: Kinase, accessions: P29597, gene: TYK2, swissprot: TYK2_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/20363976) Multidrug and toxin extrusion protein 2 (Organism: Homo sapiens, class: Transporter, accessions: Q86VL8, gene: SLC47A2, swissprot: S47A2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/207924Orig1s000lbl.pdf) Multidrug and toxin extrusion protein 1 (Organism: Homo sapiens, class: Transporter, accessions: Q96FL8, gene: SLC47A1, swissprot: S47A1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/207924Orig1s000lbl.pdf) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/207924Orig1s000lbl.pdf) Solute carrier family 22 member 6 (Organism: Homo sapiens, class: Transporter, accessions: Q4U2R8, gene: SLC22A6, swissprot: S22A6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/207924Orig1s000lbl.pdf) Solute carrier family 22 member 8 (Organism: Homo sapiens, class: Transporter, accessions: Q8TCC7, gene: SLC22A8, swissprot: S22A8_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/207924Orig1s000lbl.pdf) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/207924Orig1s000lbl.pdf) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/207924Orig1s000lbl.pdf) Baricitinib is a selective and reversible inhibitor of Janus kinase (JAK)1 and JAK2. Janus kinases (JAKs) are enzymes that transduce intracellular signals from cell surface receptors for a number of cytokines and growth factors involved in haematopoiesis, inflammation and immune function. Within the intracellular signalling pathway, JAKs phosphorylate and activate signal transducers and activators of transcription (STATs), which activate gene expression within the cell. Baricitinib modulates these signalling pathways by partially inhibiting JAK1 and JAK2 enzymatic activity, thereby reducing the phosphorylation and activation of STATs. Baricitinib is indicated for the treatment of moderate to severe active rheumatoid arthritis in adult patients who have responded inadequately to, or who are intolerant to one or more disease-modifying anti-rheumatic drugs as monotherapy or in combination with methotrexate. 2017-02-13 EMA 3JW
Click to view rucaparib Poly [ADP-ribose] polymerase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P09874, gene: PARP1, swissprot: PARP1_HUMAN) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/209115s000lbl.pdf) Poly [ADP-ribose] polymerase 2 (Organism: Homo sapiens, class: Enzyme, accessions: Q9UGN5, gene: PARP2, swissprot: PARP2_HUMAN) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/209115s000lbl.pdf) Poly [ADP-ribose] polymerase 3 (Organism: Homo sapiens, class: Enzyme, accessions: Q9Y6F1, gene: PARP3, swissprot: PARP3_HUMAN) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/209115s000lbl.pdf) Poly [ADP-ribose] polymerase 4 (Organism: Homo sapiens, class: Enzyme, accessions: Q9UKK3, gene: PARP4, swissprot: PARP4_HUMAN) inhibitor (Source: http://dx.doi.org/10.1021/acs.jmedchem.6b00990) Tankyrase-1 (Organism: Homo sapiens, class: Enzyme, accessions: O95271, gene: TNKS, swissprot: TNKS1_HUMAN) inhibitor (Source: http://dx.doi.org/10.1021/acs.jmedchem.6b00990) Tankyrase-2 (Organism: Homo sapiens, class: Enzyme, accessions: Q9H2K2, gene: TNKS2, swissprot: TNKS2_HUMAN) inhibitor (Source: http://dx.doi.org/10.1021/acs.jmedchem.6b00990) Poly [ADP-ribose] polymerase 10 (Organism: Homo sapiens, class: Enzyme, accessions: Q53GL7, gene: PARP10, swissprot: PAR10_HUMAN) inhibitor (Source: http://dx.doi.org/10.1021/acs.jmedchem.6b00990) Poly [ADP-ribose] polymerase 12 (Organism: Homo sapiens, class: Enzyme, accessions: Q9H0J9, gene: PARP12, swissprot: PAR12_HUMAN) inhibitor (Source: http://dx.doi.org/10.1021/acs.jmedchem.6b00990) Poly [ADP-ribose] polymerase 14 (Organism: Homo sapiens, class: Enzyme, accessions: Q460N5, gene: PARP14, swissprot: PAR14_HUMAN) inhibitor (Source: http://dx.doi.org/10.1021/acs.jmedchem.6b00990) Poly [ADP-ribose] polymerase 15 (Organism: Homo sapiens, class: Enzyme, accessions: Q460N3, gene: PARP15, swissprot: PAR15_HUMAN) inhibitor (Source: http://dx.doi.org/10.1021/acs.jmedchem.6b00990) Rucaparib is an inhibitor of poly (ADP-ribose) polymerase (PARP) enzymes, including PARP-1, PARP-2, and PARP-3, which play a role in DNA repair. In vitro studies have shown that rucaparib-induced cytotoxicity may involve inhibition of PARP enzymatic activity and increased formation of PARP-DNA complexes resulting in DNA damage, apoptosis, and cell death. Increased rucaparib-induced cytotoxicity was observed in tumor cell lines with deficiencies in BRCA1/2 and other DNA repair genes. Rucaparib has been shown to decrease tumor growth in mouse xenograft models of human cancer with or without deficiencies in BRCA. Poly(ADP-Ribose) Polymerase Inhibitor (Code: N0000191623) Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Poly(ADP-ribose) Polymerase Inhibitors (Code: D000067856) 2016-12-19 FDA RPB
Click to view icotinib Epidermal growth factor receptor (Organism: Homo sapiens, class: Kinase, accessions: P00533, gene: EGFR, swissprot: EGFR_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/22088449) Icotinib is a new epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) that developed and used in China for the treatment of patients with non-small cell lung cancer (NSCLC). 2011 China Food and Drug Administration (CFDA)
Click to view olmutinib Epidermal growth factor receptor (Organism: Homo sapiens, class: Kinase, accessions: P00533, gene: EGFR, swissprot: EGFR_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/27357069) Tyrosine-protein kinase BTK (Organism: Homo sapiens, class: Kinase, accessions: Q06187, gene: BTK, swissprot: BTK_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4835877/pdf/13075_2016_Article_988.pdf) Olmutinib is an oral, third-generation epidermal growth factor receptor tyrosine kinase inhibitor (EGFR TKI) for the treatment of non-small cell lung cancer (NSCLC). Third-generation EGFR TKIs with covalent binding to the receptors demonstrate irreversible enzymatic inhibition of activating EGFR mutations and T790M mutation (a common reason for acquired EGFR TKI resistance), while sparing wild-type EGFR. 2016-05 Korean Food and Drug Administration (KFDA)
Click to view crisaborole Phosphodiesterase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P27815|Q07343|Q08493|Q08499, gene: PDE4A|PDE4B|PDE4C|PDE4D, swissprot: PDE4A_HUMAN|PDE4B_HUMAN|PDE4C_HUMAN|PDE4D_HUMAN) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/207695s000lbl.pdf) High affinity cAMP-specific 3',5'-cyclic phosphodiesterase 7A (Organism: Homo sapiens, class: Enzyme, accessions: Q13946, gene: PDE7A, swissprot: PDE7A_HUMAN) inhibitor (Source: https://doi.org/10.1016/j.bmcl.2009.03.007) Crisaborole is a phosphodiesterase 4 (PDE-4) inhibitor. PDE-4 inhibition results in increased intracellular cyclic adenosine monophosphate (cAMP) levels. The specific mechanism(s) by which crisaborole exerts its therapeutic action for the treatment of atopic dermatitis is not well defined. antipsoriatic (Code: CHEBI:50748) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) Phosphodiesterase 4 Inhibitor (Code: N0000182961) Phosphodiesterase 4 Inhibitors (Code: N0000182960) 2016-12-14 FDA
Click to view radotinib Tyrosine-protein kinase ABL1 (Organism: Homo sapiens, class: Kinase, accessions: P00519, gene: ABL1, swissprot: ABL1_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/25676420) Radotinib is a second-generation tyrosine kinase inhibitor of Bcr-Abl fusion protein and the platelet-derived growth factor receptor (PDGFR), with potential antineoplastic activity. Upon administration, radotinib specifically inhibits the Bcr-Abl fusion protein, an abnormal enzyme expressed in Philadelphia chromosome-positive chronic myeloid leukemia (CML) cells. In addition, this agent also inhibits PDGFR thereby blocking PDGFR-mediated signal transduction pathways. The inhibitory effect of radotinib on these specific tyrosine kinases may decrease cellular proliferation and inhibit angiogenesis. This agent has shown potent efficacy in CML cells that are resistant to the first-generation standard tyrosine kinase inhibitors, such as imatinib, nilotinib and dasatinib. Radotinib is used as a second-line Chronic Myeloid Leukemia treatment. 2012-01-05 Korean Food and Drug Administration (KFDA)
Click to view lifitegrast Integrin alpha-L/beta-2 (Organism: Homo sapiens, class: Adhesion, accessions: P05107|P20701, gene: ITGAL|ITGB2, swissprot: ITAL_HUMAN|ITB2_HUMAN) antagonist (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208073s000lbl.pdf) Solute carrier organic anion transporter family member 1A2 (Organism: Homo sapiens, class: Transporter, accessions: P46721, gene: SLCO1A2, swissprot: SO1A2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208073Orig1s000ClinPharmR.pdf) Solute carrier organic anion transporter family member 2B1 (Organism: Homo sapiens, class: Transporter, accessions: O94956, gene: SLCO2B1, swissprot: SO2B1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208073Orig1s000ClinPharmR.pdf) Lifitegrast is a lymphocyte function-associated antigen-1 ( LFA-1) antagonist, blocks the interaction of LFA-1 with its cognate ligand intercellular adhesion molecule-1 (ICAM-1), LFA-1/ICAM-1 interaction can contribute to the formation of an immunological synapse resulting in T-cell activation and migration to target tissues. Lifitegrast is used as an ophthalmic solution for the treatment of the signs and symptoms of dry eye disease. anti-inflammatory drug (Code: CHEBI:35472) Lymphocyte Function-Associated Antigen-1 Antagonist (Code: N0000192701) Lymphocyte Function-Associated Antigen-1 Antagonists (Code: N0000192700) Ophthalmic Solutions (Code: D009883) Pharmaceutical Solutions (Code: D019999) 2016-07-11 FDA
Click to view pemafibrate Peroxisome proliferator-activated receptor alpha (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: Q07869, gene: PPARA, swissprot: PPARA_HUMAN) agonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/17553678) Peroxisome proliferator-activated receptor gamma (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P37231, gene: PPARG, swissprot: PPARG_HUMAN) agonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/17553678) Peroxisome proliferator-activated receptor delta (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: Q03181, gene: PPARD, swissprot: PPARD_HUMAN) agonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/17553678) Pemafibrate is a selective PPAR-alpha modulator (SPPARM-alpha) that has antihyperlipidaemic activity. 2017-07-03 PMDA
Click to view zabofloxacin Zabofloxacin is a fluoroquinolone antibiotic with enhanced in-vitro activity against Streptococcus pneumoniae, including strains resistant to other antibiotics. The spectrum of activity of Zabofloxacin includes those bacterial strains that are responsible for most community-acquired respiratory infections. 2015-03-20 Korean Food and Drug Administration (KFDA)
Click to view imrecoxib Prostaglandin G/H synthase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P35354, gene: PTGS2, swissprot: PGH2_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/15210067) Imrecoxib is a selective cyclooxygenase-2 (COX-2) inhibitor indicated for treatment of osteoarthritis. 2011-05-20 China Food and Drug Administration (CFDA)
Click to view enasidenib Isocitrate dehydrogenase [NADP], mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P48735, gene: IDH2, swissprot: IDHP_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209606s000lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209606s000lbl.pdf) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209606s000lbl.pdf) Solute carrier family 22 member 6 (Organism: Homo sapiens, class: Transporter, accessions: Q4U2R8, gene: SLC22A6, swissprot: S22A6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209606s000lbl.pdf) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209606s000lbl.pdf) Solute carrier family 22 member 8 (Organism: Homo sapiens, class: Transporter, accessions: Q8TCC7, gene: SLC22A8, swissprot: S22A8_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209606s000lbl.pdf) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209606s000lbl.pdf) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209606s000lbl.pdf) Enasidenib is a small molecule inhibitor of the isocitrate dehydrogenase 2 (IDH2) enzyme. Enasidenib targets the mutant IDH2 variants R140Q, R172S, and R172K at approximately 40-fold lower concentrations than the wild-type enzyme in vitro. Inhibition of the mutant IDH2 enzyme by enasidenib led to decreased 2-hydroxyglutarate (2-HG) levels and induced myeloid differentiation in vitro and in vivo in mouse xenograft models of IDH2 mutated AML. In blood samples from patients with AML with mutated IDH2, enasidenib decreased 2-HG levels, reduced blast counts and increased percentages of mature myeloid cells. Isocitrate Dehydrogenase 2 Inhibitor (Code: N0000193615) Isocitrate Dehydrogenase 2 Inhibitors (Code: N0000193614) 2017-08-01 FDA 69Q
Click to view fluciclovine (18F) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208054Orig1s000PharmR.pdf) Multidrug resistance-associated protein 4 (Organism: Homo sapiens, class: Transporter, accessions: O15439, gene: ABCC4, swissprot: MDR4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208054Orig1s000PharmR.pdf) Fluciclovine (18F) is a radiotracer containing a synthetic amino acid analogue of L-leucine radiolabeled with fluorine F 18 with diagnostic imaging use. Fluciclovine (18F) transported across mammalian cell membranes by amino acid transporters, such as LAT-1 and ASCT2, which are upregulated in prostate cancer cells, but as was shown, this compound has a higher affinity for ASCT2 in comparison with other transporters. Fluciclovine (18F) is used as a radioactive diagnostic agent indicated for positron emission tomography (PET) imaging in men with suspected prostate cancer recurrence. Radioactive Diagnostic Agent (Code: N0000177914) Positron Emitting Activity (Code: N0000175869) 2016-05-27 FDA
Click to view hydrocortisone phosphate Hydrocortisone phosphate is a steroid phosphate that is the 21-O-phospho derivative of cortisol. (See: hydrocortisone) 1960-08-06 FDA
Click to view meglumine Meglumine (N-methyl-D-glucamine) is a poorly metabolized derivative of sorbitol that has regulatory acceptance as a benign excipient for drug formulation to increase aqueous solubility of lipophilic drugs and improve their absorption. Meglumine is used in the preparation of certain radiopaque media such as diatrizoate meglumine and iodipamide meglumine. Meglumine is combined as an excipient (an inert substance) not an active ingredient. Excipients are added to ensure that the shelf-life of the active ingredients can be long enough to be active until internal use. Excipients are combined also to support the active ingredients, so that the latter can be easily administered or absorbed in the body. Examples of meglumine-combined drugs are flunixin meglumine (non-steroidal anti-inflammatory drugs, used as a veterinary anti-inflammatory and analgesic) and meglumine antimoniate (antiprotozoal to treat leishmaniasis). Meglumine is used in ion-exchange resins to chelate boron ions selectively. Contrast Media (Code: D003287) Diagnostic Uses of Chemicals (Code: D064907) 1974-04-30 FDA
Click to view cefathiamidine Cefathiamidine is a beta-lactam antibiotic that exhibits a broad spectrum of bactericidal activity against gram-positive bacteria. By binding to specific penicillin-binding proteins (PBPs) located inside the bacterial cell wall, it inhibits the third and last stage of bacterial cell wall synthesis. Cefathiamidine is used for the treatment of respiratory, liver, five senses, urinary tract infections, endocarditis and sepsis. 2012-12-11 China Food and Drug Administration (CFDA)
Click to view eldecalcitol Vitamin D3 receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P11473, gene: VDR, swissprot: VDR_HUMAN) agonist (Source: http://www.kegg.jp/entry/D07578) Vitamin D3 receptor (Organism: Rattus norvegicus, class: Transcription factor, accessions: P13053, gene: Vdr, swissprot: VDR_RAT) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/8396500?dopt=AbstractPlus) Eldecalcitol is an analog of the active form of vitamin D. Eldecalcitol has a higher affinity for serum vitamin D-binding protein (DBP), binds more weakly to vitamin D receptor, and shows lower potency in suppression of serum parathyroid hormone. Eldecalcitol has been approved for the treatment of osteoporosis. Bone Density Conservation Agents (Code: D050071) 2011-01-21 PMDA ED9
Click to view pentapiperium metilsulfate Pentapiperium metilsulfate is a synthetic quaternary ammonium anticholinergic and antisecretory agent used especially in the treatment of peptic ulcer.
Click to view pimavanserin 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) inverse agonist (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/207318lbl.pdf) 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) inverse agonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/16469866) Pimavanserin is an atypical antipsychotic. Mechanism of action of pimavanserin in the treatment of hallucinations and delusions associated with Parkinson's disease psychosis is unknown. However, the effect of pimavanserin could be mediated through a combination of inverse agonist and antagonist activity at serotonin 5-HT2A receptors and to a lesser extent at serotonin 5-HT2C receptors. Pimavanserin is indicated for the treatment of hallucinations and delusions associated with Parkinson’s disease psychosis. antipsychotic agent (Code: CHEBI:35476) serotonergic antagonist (Code: CHEBI:48279) Atypical Antipsychotic (Code: N0000175430) Anti-Dyskinesia Agents (Code: D018726) Antiparkinson Agents (Code: D000978) Antipsychotic Agents (Code: D014150) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Neurotransmitter Agents (Code: D018377) Psychotropic Drugs (Code: D011619) Serotonin 5-HT2 Receptor Agonists (Code: D058826) Serotonin Agents (Code: D018490) Serotonin Receptor Agonists (Code: D017366) Tranquilizing Agents (Code: D014149) 2016-04-29 FDA
Click to view opicapone Catechol O-methyltransferase (Organism: Homo sapiens, class: Enzyme, accessions: P21964, gene: COMT, swissprot: COMT_HUMAN) inhibitor (Source: https://www.ema.europa.eu/documents/product-information/ongentys-epar-product-information_en.pdf) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) inhibitor (Source: https://www.ema.europa.eu/documents/product-information/ongentys-epar-product-information_en.pdf) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.ema.europa.eu/documents/product-information/ongentys-epar-product-information_en.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.ema.europa.eu/documents/product-information/ongentys-epar-product-information_en.pdf) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) substrate (Source: https://www.ema.europa.eu/documents/product-information/ongentys-epar-product-information_en.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.ema.europa.eu/documents/product-information/ongentys-epar-product-information_en.pdf) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) substrate (Source: https://www.ema.europa.eu/documents/product-information/ongentys-epar-product-information_en.pdf) Opicapone is a peripheral, selective and reversible catechol-O-methyltransferase (COMT) inhibitor. In the presence of a DOPA decarboxylase inhibitor (DDCI), COMT becomes the major metabolising enzyme for levodopa, catalysing its conversion to 3-O-methyldopa (3-OMD) in the brain and periphery. In patients taking levodopa and a peripheral DDCI, such as carbidopa or benserazide, opicapone increases levodopa plasma levels thereby improving the clinical response to levodopa. Opicapone is indicated as adjunctive therapy to preparations of levodopa/ DOPA decarboxylase inhibitors (DDCI) in adult patients with Parkinson’s disease and end-of-dose motor fluctuations who cannot be stabilised on those combinations. Anti-Dyskinesia Agents (Code: D018726) Antiparkinson Agents (Code: D000978) Catechol O-Methyltransferase Inhibitors (Code: D065098) Central Nervous System Agents (Code: D002491) Enzyme Inhibitors (Code: D004791) 2016-06-24 EMA
Click to view neratinib Epidermal growth factor receptor (Organism: Homo sapiens, class: Kinase, accessions: P00533, gene: EGFR, swissprot: EGFR_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208051s000lbl.pdf) Receptor tyrosine-protein kinase erbB-2 (Organism: Homo sapiens, class: Kinase, accessions: P04626, gene: ERBB2, swissprot: ERBB2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208051s000lbl.pdf) Receptor tyrosine-protein kinase erbB-4 (Organism: Homo sapiens, class: Kinase, accessions: Q15303, gene: ERBB4, swissprot: ERBB4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208051s000lbl.pdf) Neratinib is a kinase inhibitor that irreversibly binds to Epidermal Growth Factor Receptor (EGFR), Human Epidermal Growth Factor Receptor 2 (HER2), and HER4. In vitro, neratinib reduces EGFR and HER2 autophosphorylation, downstream MAPK and AKT signaling pathways, and showed antitumor activity in EGFR and/or HER2 expressing carcinoma cell lines. Neratinib human metabolites M3, M6, M7 and M11 inhibited the activity of EGFR, HER2 and HER4 in vitro. In vivo, oral administration of neratinib inhibited tumor growth in mouse xenograft models with tumor cell lines expressing HER2 and EGFR. antineoplastic agent (Code: CHEBI:35610) Kinase Inhibitor (Code: N0000175605) Kinase Inhibitors (Code: N0000175082) P-Glycoprotein Inhibitors (Code: N0000185503) 2017-07-17 FDA
Click to view venetoclax Apoptosis regulator Bcl-2 (Organism: Homo sapiens, class: Cytosolic other, accessions: P10415, gene: BCL2, swissprot: BCL2_HUMAN) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf) Bcl-2-like protein 1 (Organism: Homo sapiens, class: Cytosolic other, accessions: Q07817, gene: BCL2L1, swissprot: B2CL1_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/23291630) Apoptosis regulator Bcl-W (Organism: Homo sapiens, class: Cytosolic other, accessions: Q92843, gene: BCL2L2, swissprot: B2CL2_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/23291630) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf) Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf) UDP-glucuronosyltransferase 1-1 (Organism: Homo sapiens, class: Enzyme, accessions: P22309, gene: UGT1A1, swissprot: UD11_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf) Venetoclax is a selective and orally bioavailable small-molecule inhibitor of BCL-2, an anti-apoptotic protein. Overexpression of BCL-2 has been demonstrated in CLL cells where it mediates tumor cell survival and has been associated with resistance to chemotherapeutics. Venetoclax helps restore the process of apoptosis by binding directly to the BCL-2 protein, displacing pro-apoptotic proteins like BIM, triggering mitochondrial outer membrane permeabilization and the activation of caspases. In nonclinical studies, venetoclax has demonstrated cytotoxic activity in tumor cells that overexpress BCL-2. Venetoclax is indicated for the treatment of adult patients with chronic lymphocytic leukemia or small lymphocytic lymphoma. Venetoclax also is indicated in combination with azacitidine or decitabine or low-dose cytarabine for the treatment of newly-diagnosed acute myeloid leukemia in adults who are age 75 years or older, or who have comorbidities that preclude use of intensive induction chemotherapy. antineoplastic agent (Code: CHEBI:35610) Antineoplastic Agents (Code: D000970) BCL-2 Inhibitor (Code: N0000192515) Increased Cellular Death (Code: N0000009176) P-Glycoprotein Inhibitors (Code: N0000185503) 2016-04-11 FDA
Click to view brivaracetam Synaptic vesicle glycoprotein 2A (Organism: Homo sapiens, class: Transporter, accessions: Q7L0J3, gene: SV2A, swissprot: SV2A_HUMAN) modulator (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/205836s005,205837s004,205838s003lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/205836s005,205837s004,205838s003lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/205836s005,205837s004,205838s003lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/205836s005,205837s004,205838s003lbl.pdf) Epoxide hydrolase 1 (Organism: Homo sapiens, class: Unclassified, accessions: P07099, gene: EPHX1, swissprot: HYEP_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/205836s005,205837s004,205838s003lbl.pdf) Brivaracetam displays a high and selective affinity for synaptic vesicle protein 2A (SV2A) in the brain, which may contribute to the anticonvulsant effect. Brivaracetam is indicated for the treatment of partial-onset seizures in patients 4 years of age and older. anticonvulsant (Code: CHEBI:35623) Epoxide Hydrolase Inhibitors (Code: N0000192345) Anticonvulsants (Code: D000927) Central Nervous System Agents (Code: D002491) 2016-01-14 EMA
Click to view bictegravir Integrase (Organism: Human immunodeficiency virus 1, class: Enzyme, accessions: Q7ZJM1, gene: pol, swissprot: Q7ZJM1_9HIV1) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209360s000lbl.pdf) Multidrug and toxin extrusion protein 1 (Organism: Homo sapiens, class: Transporter, accessions: Q96FL8, gene: SLC47A1, swissprot: S47A1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210251s000lbl.pdf) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210251s000lbl.pdf) Bictegravir inhibits the strand transfer activity of HIV-1 integrase (integrase strand transfer inhibitor; INSTI), an HIV-1 encoded enzyme that is required for viral replication. Inhibition of integrase prevents the integration of linear HIV-1 DNA into host genomic DNA, blocking the formation of the HIV-1 provirus and propagation of the virus. 2018-02-07 FDA
Click to view tezacaftor Cystic fibrosis transmembrane conductance regulator (Organism: Homo sapiens, class: Ion channel, accessions: P13569, gene: CFTR, swissprot: CFTR_HUMAN) activator (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210491lbl.pdf) Tezacaftor facilitates the cellular processing and trafficking of normal and select mutant forms of CFTR (including F508del-CFTR) to increase the amount of mature CFTR protein delivered to the cell surface. 2018-02-12 FDA
Click to view etelcalcetide Extracellular calcium-sensing receptor (Organism: Homo sapiens, class: GPCR, accessions: P41180, gene: CASR, swissprot: CASR_HUMAN) agonist (Source: https://www.ema.europa.eu/documents/product-information/parsabiv-epar-product-information_en.pdf) Etelcalcetide is a synthetic peptide calcimimetic agent which reduces parathyroid hormone (PTH) secretion through binding and activation of the calcium-sensing receptor. The reduction in PTH is associated with a concomitant decrease in serum calcium and phosphate levels. Etelcalcetide was approved for the treatment of secondary hyperparathyroidism in adult patients with chronic kidney disease on hemodialysis. Calcium-sensing Receptor Agonist (Code: N0000175902) Increased Calcium-sensing Receptor Sensitivity (Code: N0000020081) 2016-11-11 EMA
Click to view mepiprazole Mepiprazole is a psychotropic drug exhibiting effects on the uptake and retention of monoamines. It is a pyrazolyl-alkyl-piperazine derivative. Mepiprazole mediates a weak inhibitory action on the uptake of 5-HT on hypothalamic neurons. Mepiprazole is marketed for the treatment of anxiety neuroses.
Click to view lorpiprazole Lorpiprazole is a serotonin antagonist and reuptake inhibitor used for the treatment of major depressive disorder.
Click to view elobixibat Ileal sodium/bile acid cotransporter (Organism: Homo sapiens, class: Transporter, accessions: Q12908, gene: SLC10A2, swissprot: NTCP2_HUMAN) inhibitor (Source: http://dx.doi.org/10.1016/S0016-5085(10)61017-7) Elobixibat is an ileal bile acid transporter inhibitor. By inhibiting the uptake of bile acids, elobixibat increases the bile acid concentration in the gut, and this accelerates intestinal passage and softens the stool. It is used for the treatment of chronic constipation. 2018-01-19 PMDA
Click to view apalutamide Androgen receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P10275, gene: AR, swissprot: ANDR_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210951s000lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210951s000lbl.pdf) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210951s000lbl.pdf) Multidrug and toxin extrusion protein 2 (Organism: Homo sapiens, class: Transporter, accessions: Q86VL8, gene: SLC47A2, swissprot: S47A2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210951s000lbl.pdf) Multidrug and toxin extrusion protein 1 (Organism: Homo sapiens, class: Transporter, accessions: Q96FL8, gene: SLC47A1, swissprot: S47A1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210951s000lbl.pdf) Solute carrier family 22 member 8 (Organism: Homo sapiens, class: Transporter, accessions: Q8TCC7, gene: SLC22A8, swissprot: S22A8_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210951s000lbl.pdf) Apalutamide is an Androgen Receptor (AR) inhibitor that binds directly to the ligand-binding domain of the AR. Apalutamide inhibits AR nuclear translocation, inhibits DNA binding, and impedes AR-mediated transcription. A major metabolite, N-desmethyl apalutamide, is a less potent inhibitor of AR, and exhibited one-third the activity of apalutamide in an in vitro transcriptional reporter assay. Apalutamide is indicated for the treatment of patients with metastatic castration-sensitive or non-metastatic castration-resistant prostate cancer. 2018-02-14 FDA
Click to view velpatasvir Genome polyprotein (Organism: Hepatitis C virus genotype 1a (isolate H), class: Polyprotein, accessions: P27958, gene: None, swissprot: POLG_HCVH) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208341s000lbl.pdf) Genome polyprotein (Organism: Hepatitis C virus genotype 1b (isolate BK), class: Polyprotein, accessions: P26663, gene: None, swissprot: POLG_HCVBK) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208341s000lbl.pdf) Genome polyprotein (Organism: Hepatitis C virus genotype 2a (isolate JFH-1), class: Polyprotein, accessions: Q99IB8, gene: None, swissprot: POLG_HCVJF) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208341s000lbl.pdf) Genome polyprotein (Organism: Hepatitis C virus genotype 4a (isolate ED43), class: Polyprotein, accessions: O39929, gene: None, swissprot: POLG_HCVED) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208341s000lbl.pdf) Genome polyprotein (Organism: Hepatitis C virus genotype 3a (isolate k3a) (HCV), class: Polyprotein, accessions: Q81495, gene: None, swissprot: POLG_HCVK3) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208341s000lbl.pdf) Genome polyprotein (Organism: Hepatitis C virus genotype 2b (isolate JPUT971017) (HCV), class: Polyprotein, accessions: Q9DHD6, gene: None, swissprot: POLG_HCVJP) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208341s000lbl.pdf) Genome polyprotein (Organism: Hepatitis C virus genotype 5a (isolate SA13) (HCV), class: Polyprotein, accessions: O91936, gene: None, swissprot: POLG_HCVSA) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208341s000lbl.pdf) Genome polyprotein (Organism: Hepatitis C virus genotype 6a (isolate 6a33) (HCV), class: Polyprotein, accessions: Q5I2N3, gene: None, swissprot: POLG_HCV6A) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208341s000lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208341s000lbl.pdf) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208341s000lbl.pdf) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208341s000lbl.pdf) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208341s000lbl.pdf) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: O94956, gene: SLCO2B1, swissprot: SO2B1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208341s000lbl.pdf) pan-genotypic NS5A inhibitor for the treatment of chronic genotype 1-6 hepatitis C virus (HCV) infection antiviral drug (Code: CHEBI:36044) Hepatitis C Virus NS5A Inhibitor (Code: N0000191256) Breast Cancer Resistance Protein Inhibitors (Code: N0000190113) P-Glycoprotein Inhibitors (Code: N0000185503) Organic Anion Transporting Polypeptide 1B1 Inhibitors (Code: N0000190107) Organic Anion Transporting Polypeptide 1B3 Inhibitors (Code: N0000190108) Organic Anion Transporting Polypeptide 2B1 Inhibitors (Code: N0000190109) Anti-Infective Agents (Code: D000890) Antiviral Agents (Code: D000998) 2016-06-28 FDA
Click to view monoxerutin Monoxerutin is a flavonol which has antioxidant properties. It is used for the treatment of varicose veins and chronic venous insufficiency.
Click to view oxiglutatione Glutathione reductase, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P00390, gene: GSR, swissprot: GSHR_HUMAN) (Source: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=f69655c5-cf32-6461-e00e-3a5c4a761344) A GLUTATHIONE dimer formed by a disulfide bond between the cysteine sulfhydryl side chains during the course of being oxidized. 2008-07-24 FDA GDS
Click to view elbasvir Genome polyprotein (Organism: Hepatitis C virus genotype 1a (isolate H), class: Polyprotein, accessions: P27958, gene: None, swissprot: POLG_HCVH) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208261Orig1s000lbl.pdf) Genome polyprotein (Organism: Hepatitis C virus genotype 1b (isolate BK), class: Polyprotein, accessions: P26663, gene: None, swissprot: POLG_HCVBK) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208261Orig1s000lbl.pdf) Genome polyprotein (Organism: Hepatitis C virus genotype 4a (isolate ED43), class: Polyprotein, accessions: O39929, gene: None, swissprot: POLG_HCVED) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208261Orig1s000lbl.pdf) Multidrug resistance protein 1 (Organism:Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208261Orig1s000lbl.pdf) inhibits NS5A protein of hepatitis C virus antiviral drug (Code: CHEBI:36044) hepatoprotective agent (Code: CHEBI:62868) Hepatitis C Virus NS5A Inhibitor (Code: N0000191256) Breast Cancer Resistance Protein Inhibitors (Code: N0000190113) 2016-01-28 FDA
Click to view etimicin Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) 2014-09-15 China Food and Drug Administration (CFDA)
Click to view obeticholic acid Bile acid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: Q96RI1, gene: NR1H4, swissprot: NR1H4_HUMAN) agonist (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/207999s000lbl.pdf) obeticholic acid is an agonist for FXR, a nuclear receptor expressed in the liver and intestine hepatoprotective agent (Code: CHEBI:62868) Farnesoid X Receptor Agonist (Code: N0000192561) Farnesoid X Receptor Agonists (Code: N0000192560) 2016-05-27 FDA CHC
Click to view grazoprevir Genome polyprotein (Organism: Hepatitis C virus genotype 1a (isolate H), class: Polyprotein, accessions: P27958, gene: None, swissprot: POLG_HCVH) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208261Orig1s000lbl.pdf) Genome polyprotein (Organism: Hepatitis C virus genotype 1b (isolate BK), class: Polyprotein, accessions: P26663, gene: None, swissprot: POLG_HCVBK) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208261Orig1s000lbl.pdf) Genome polyprotein (Organism: Hepatitis C virus genotype 4a (isolate ED43), class: Polyprotein, accessions: O39929, gene: None, swissprot: POLG_HCVED) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208261Orig1s000lbl.pdf) Multidrug resistance protein 1 (Organism:Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208261Orig1s000lbl.pdf) Grazoprevir is a direct acting antiviral medication used as part of combination therapy to treat chronic Hepatitis C, an infectious liver disease caused by infection with Hepatitis C Virus antiviral drug (Code: CHEBI:36044) hepatoprotective agent (Code: CHEBI:62868) Anti-Infective Agents (Code: D000890) Antiviral Agents (Code: D000998) 2016-01-28 FDA SUE
Click to view climbazole Climbazole is a conazole fungicide. It is also use in shampoo and cleaner as an anti-dandruff agents and anti-bacteria agent.
Click to view trenbolone hexahydrobenzylcarbonate Trenbolone hexahydrobenzylcarbonate is a synthetic anabolic-androgenic steroid. It is a prodrug of trenbolone. Trenbolone hexahydrobenzylcarbonate was voluntarily discontinued by its manufacturer in 1997.
Click to view ixazomib Proteasome subunit beta type-5 (Organism: Homo sapiens, class: Enzyme, accessions: P28074, gene: PSMB5, swissprot: PSB5_HUMAN) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208462lbl.pdf) Proteasome subunit beta type-2 (Organism: Homo sapiens, class: Enzyme, accessions: P49721, gene: PSMB2, swissprot: PSB2_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/20160034) Proteasome subunit beta type-1 (Organism: Homo sapiens, class: Enzyme, accessions: P20618, gene: PSMB1, swissprot: PSB1_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/20160034) Ixazomib is a small molecule proteasome inhibitor that is used in combination with other antineoplastic agents to treat refractory multiple myeloma. orphan drug (Code: CHEBI:71031) proteasome inhibitor (Code: CHEBI:52726) antineoplastic agent (Code: CHEBI:35610) Proteasome Inhibitors (Code: N0000175075) Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Protease Inhibitors (Code: D011480) 2015-11-20 FDA 6V8
Click to view alfadolone acetate Alfadolone acetate is a neuroactive steroid and general anesthetic. It was often used in combination with alfaxalobe as intravenous anesthetic.
Click to view cobimetinib Dual specificity mitogen-activated protein kinase kinase 1 (Organism: Homo sapiens, class: Kinase, accessions: Q02750, gene: MAP2K1, swissprot: MP2K1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206192s000lbl.pdf) Dual specificity mitogen-activated protein kinase kinase 2 (Organism: Homo sapiens, class: Kinase, accessions: P36507, gene: MAP2K2, swissprot: MP2K2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206192s000lbl.pdf) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/26384788) Cobimetinib is a reversible inhibitor of mitogen-activated protein kinase (MAPK)/extracellular signal regulated kinase 1 (MEK1) and MEK2. MEK proteins are upstream regulators of the extracellular signal-related kinase (ERK) pathway, which promotes cellular proliferation. BRAF V600E and K mutations result in constitutive activation of the BRAF pathway which includes MEK1 and MEK2. In mice implanted with tumor cell lines expressing BRAF V600E, cobimetinib inhibited tumor cell growth. antineoplastic agent (Code: CHEBI:35610) Kinase Inhibitor (Code: N0000175605) Kinase Inhibitors (Code: N0000175082) 2015-11-10 FDA EUI
Click to view saroglitazar Peroxisome proliferator-activated receptor alpha (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: Q07869, gene: PPARA, swissprot: PPARA_HUMAN) agonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/26171220) Peroxisome proliferator-activated receptor gamma (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P37231, gene: PPARG, swissprot: PPARG_HUMAN) agonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/26171220) Saroglitazar is a dual peroxisome proliferator-activated receptor (PPAR) agonist indicated for the treatment of hypertriglyceridemia in Type II diabetics. hypoglycemic agent (Code: CHEBI:35526) 2013-02-25 CDSCO (INDIA)
Click to view pitolisant Histamine H3 receptor (Organism: Homo sapiens, class: GPCR, accessions: Q9Y5N1, gene: HRH3, swissprot: HRH3_HUMAN) inverse agonist (Source: https://www.ema.europa.eu/documents/product-information/wakix-epar-product-information_en.pdf) Solute carrier family 22 member 1 (Organism: Homo sapiens, class: Transporter, accessions: O15245, gene: SLC22A1, swissprot: S22A1_HUMAN) inhibitor (Source: https://www.ema.europa.eu/documents/product-information/wakix-epar-product-information_en.pdf) Pitolisant is a potent, orally active histamine H3-receptor antagonist/inverse agonist which, via its blockade of histamine auto-receptors enhances the activity of brain histaminergic neurons, a major arousal system with widespread projections to the whole brain. Pitolisant also modulates various neurotransmitter systems, increasing acetylcholine, noradrenaline and dopamine release in the brain. 2016-03-31 EMA
Click to view flibanserin 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) agonist (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/022526lbl.pdf) 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) antagonist (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/022526lbl.pdf) D(4) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21917, gene: DRD4, swissprot: DRD4_HUMAN) antagonist (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/022526lbl.pdf) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) 5-hydroxytryptamine receptor 2B (Organism: Homo sapiens, class: GPCR, accessions: P41595, gene: HTR2B, swissprot: 5HT2B_HUMAN) antagonist (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/022526lbl.pdf) 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) antagonist (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/022526lbl.pdf) a serotonin receptor modulator with high affinity for the following serotonin (5-hydroxytryptamine or 5-T) receptors: agonist activity at 5-HT1A and antagonist activity at 5-HT2A. Flibanserin also has moderate antagonist activities at the 5-HT2B, 5-HT2C, and dopamine D4 receptors, used in the treatment of premenopausal women with hypoactive sexual desire disorder serotonergic agonist (Code: CHEBI:35941) serotonergic antagonist (Code: CHEBI:48279) antidepressant (Code: CHEBI:35469) P-Glycoprotein Inhibitors (Code: N0000185503) 2015-08-18 FDA
Click to view trelagliptin Dipeptidyl peptidase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P27487, gene: DPP4, swissprot: DPP4_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/26115728) Trelagliptin is an orally active dipeptidyl peptidase (DPP)-4 inhibitor developed by Takeda and approved in Japan for the treatment of type 2 diabetes mellitus. 2015-03-26 PMDA 6RL
Click to view gluconolactone Gluconolactone is a naturally occurring polyhydroxy acid (PHA) with metal chelating, moisturizing and antioxidant activity. Gluconolactone can be produced by enzymatic oxidation of D-glucose oxidation. Its ability in free radicals scavenging accounts for its antioxidant property. It is used in cosmetic product and as a coagulant in tofu processing. Gluconolactone is also used for skin protection from some of the damaging effects of UV radiation. Gluconolactone in combination with Citric Acid and Magnesium Carbonate is indicated for dissolution of bladder calculi of the struvite or apatite variety by local intermittent irrigation and for prevention encrustations of indwelling urethral catheters and cystostomy tubes. Calculi Dissolution Agent (Code: N0000175835) Irrigation (Code: N0000175534) 1990-10-02 FDA LGC
Click to view angiotensin II Type-1 angiotensin II receptor (Organism: Homo sapiens, class: GPCR, accessions: P30556, gene: AGTR1, swissprot: AGTR1_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209360s000lbl.pdf) Type-2 angiotensin II receptor (Organism: Homo sapiens, class: GPCR, accessions: P50052, gene: AGTR2, swissprot: AGTR2_HUMAN) agonist (Source: ) Angiotensin II is a naturally occurring peptide hormone of the renin-angiotensin-aldosterone system (RAAS) that causes vasoconstriction and an increase in blood pressure. Angiotensin II raises blood pressure by vasoconstriction and increased aldosterone release. Direct action of angiotensin II on the vessel wall is mediated by binding to the G-protein-coupled angiotensin II receptor type 1 on vascular smooth muscle cells, which stimulates Ca2+/calmodulin-dependent phosphorylation of myosin and causes smooth muscle contraction. Vasoconstrictor (Code: N0000192562) Vasoconstriction (Code: N0000009908) Cardiovascular Agents (Code: D002317) Vasoconstrictor Agents (Code: D014662) 2017-12-21 FDA
Click to view faropenem medoxil Faropenem medoxomil is a prodrug of faropenem, the first oral penem-type antibiotic. (See: faropenem)
Click to view UREA C14 Urease (Organism: Helicobacter pylori, class: Enzyme, accessions: Q8KT33, gene: ureB, swissprot: Q8KT33_HELPY) substrate (Source: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=13148b04-9295-41bb-bd8b-76dbd4ce7c00) Urea 14C is a urea molecule radiolabelled with a radioactive carbon-14. To detect H. pylori, urea labeled with 14C is swallowed by the patient. If gastric urease from H. pylori is present, urea is split to form CO2 and NH3 at the interface between the gastric epithelium and lumen and 14CO2 is absorbed into the blood and exhaled in the breath. It is currently used for the Urea Breath Test (UBT) and is available as a rapid diagnostic test (marketed as PyTest) for the detection of Helicobacter pylori infections. 1997-05-09 FDA URE
Click to view copanlisib Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (Organism: Homo sapiens, class: Kinase, accessions: P42336, gene: PIK3CA, swissprot: PK3CA_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209936s000lbl.pdf) Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform (Organism: Homo sapiens, class: Kinase, accessions: O00329, gene: PIK3CD, swissprot: PK3CD_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209936s000lbl.pdf) Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform (Organism: Homo sapiens, class: Kinase, accessions: P42338, gene: PIK3CB, swissprot: PK3CB_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/24170767) Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform (Organism: Homo sapiens, class: Kinase, accessions: P48736, gene: PIK3CG, swissprot: PK3CG_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/24170767) Multidrug and toxin extrusion protein 2 (Organism: Homo sapiens, class: Transporter, accessions: Q86VL8, gene: SLC47A2, swissprot: S47A2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209936s000lbl.pdf) Copanlisib is an inhibitor of phosphatidylinositol-3-kinase (PI3K) with inhibitory activity predominantly against PI3K-alpha and PI3K-delta isoforms expressed in malignant B cells. Copanlisib has been shown to induce tumor cell death by apoptosis and inhibition of proliferation of primary malignant B cell lines. Copanlisib inhibits several key cell-signaling pathways, including B-cell receptor (BCR) signaling, CXCR12 mediated chemotaxis of malignant B cells, and NFkB signaling in lymphoma cell lines. Kinase Inhibitor (Code: N0000175605) Kinase Inhibitors (Code: N0000175082) 2017-09-14 FDA 6E2
Click to view sacubitril Neprilysin (Organism: Homo sapiens, class: Enzyme, accessions: P08473, gene: MME, swissprot: NEP_HUMAN) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/207620Orig1s000lbl.pdf) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/207620Orig1s000lbl.pdf) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/207620Orig1s000lbl.pdf) inhibits neprilysin (neutral endopeptidase; NEP) via LBQ657, the active metabolite of the prodrug sacubitril and leads to increased levels of peptides that are degraded by neprilysin such as natriuretic peptides 2015-07-07 FDA
Click to view rolapitant Substance-P receptor (Organism: Homo sapiens, class: GPCR, accessions: P25103, gene: TACR1, swissprot: NK1R_HUMAN) antagonist (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206500s000lbl.pdf) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206500s000lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206500s000lbl.pdf) An orally bioavailable, centrally-acting, selective, neurokinin 1 receptor (NK1-receptor) antagonist with potential antiemetic activity. Upon oral administration, rolapitant competitively binds to and blocks the activity of the NK1-receptor in the central nervous system, thereby inhibiting the binding of the endogenous ligand, substance P (SP). This may prevent both SP-induced emesis and chemotherapy-induced nausea and vomiting (CINV). The interaction of SP with the NK1-receptor plays a key role in the induction of nausea and vomiting caused by emetogenic cancer chemotherapy. Compared to other NK1-receptor antagonists, rolapitant has both a more rapid onset of action and a much longer half-life. antiemetic (Code: CHEBI:50919) Neurokinin 1 Antagonists (Code: N0000010262) Substance P/Neurokinin-1 Receptor Antagonist (Code: N0000175786) Cytochrome P450 2D6 Inhibitors (Code: N0000182137) Breast Cancer Resistance Protein Inhibitors (Code: N0000190113) P-Glycoprotein Inhibitors (Code: N0000185503) 2015-09-01 FDA
Click to view uridine triacetate Uridine triacetate is an acetylated pro-drug of uridine. Following oral administration, uridine triacetate is deacetylated by nonspecific esterases present throughout the body, yielding uridine in the systemic circulation of patients with hereditary orotic aciduria who cannot synthesize adequate quantities of uridine due to a genetic defect in uridine nucleotide synthesis. prodrug (Code: CHEBI:50266) neuroprotective agent (Code: CHEBI:63726) orphan drug (Code: CHEBI:71031) Pyrimidine Analog (Code: N0000191809) Pyrimidines (Code: N0000007587) Analogs/Derivatives (Code: N0000175452) 2015-09-04 FDA
Click to view olanexidine Olanexidine is a monobiguanide compound with bactericidal activity. 2015-07-03 PMDA
Click to view tivozanib Vascular endothelial growth factor receptor 1 (Organism: Homo sapiens, class: Kinase, accessions: P17948, gene: FLT1, swissprot: VGFR1_HUMAN) inhibitor (Source: http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Product_Information/human/004131/WC500239033.pdf) Vascular endothelial growth factor receptor 2 (Organism: Homo sapiens, class: Kinase, accessions: P35968, gene: KDR, swissprot: VGFR2_HUMAN) inhibitor (Source: http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Product_Information/human/004131/WC500239033.pdf) Vascular endothelial growth factor receptor 3 (Organism: Homo sapiens, class: Kinase, accessions: P35916, gene: FLT4, swissprot: VGFR3_HUMAN) inhibitor (Source: http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Product_Information/human/004131/WC500239033.pdf) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) inhibitor (Source: https://www.ema.europa.eu/documents/product-information/fotivda-epar-product-information_en.pdf) Mast/stem cell growth factor receptor Kit (Organism: Homo sapiens, class: Kinase, accessions: P10721, gene: KIT, swissprot: KIT_HUMAN) inhibitor (Source: https://www.ema.europa.eu/documents/product-information/fotivda-epar-product-information_en.pdf) Platelet-derived growth factor receptor beta (Organism: Homo sapiens, class: Kinase, accessions: P09619, gene: PDGFRB, swissprot: PGFRB_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/16982756) Receptor-type tyrosine-protein kinase FLT3 (Organism: Homo sapiens, class: Kinase, accessions: P36888, gene: FLT3, swissprot: FLT3_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/16982756) Fibroblast growth factor receptor 1 (Organism: Homo sapiens, class: Kinase, accessions: P11362, gene: FGFR1, swissprot: FGFR1_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/16982756) Hepatocyte growth factor receptor (Organism: Homo sapiens, class: Kinase, accessions: P08581, gene: MET, swissprot: MET_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/16982756) Ephrin type-B receptor 2 (Organism: Homo sapiens, class: Kinase, accessions: P29323, gene: EPHB2, swissprot: EPHB2_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/16982756) Platelet-derived growth factor receptor alpha (Organism: Homo sapiens, class: Kinase, accessions: P16234, gene: PDGFRA, swissprot: PGFRA_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/16982756) Angiopoietin-1 receptor (Organism: Homo sapiens, class: Kinase, accessions: Q02763, gene: TEK, swissprot: TIE2_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/16982756) Insulin-like growth factor 1 receptor (Organism: Homo sapiens, class: Kinase, accessions: P08069, gene: IGF1R, swissprot: IGF1R_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/16982756) Tivozanib is an oral, once-daily, vascular endothelial growth factor (VEGF) tyrosine kinase inhibitor (TKI). It is a potent, selective and long half-life inhibitor of all three VEGF receptors and is designed to optimize VEGF blockade while minimizing off-target toxicities, potentially resulting in improved efficacy and minimal dose modifications. Tivozanib is indicated as first line treatment of adult patients with advanced renal cell carcinoma (RCC) and for adult patients who are VEGFR and mTOR pathway inhibitor-naive following disease progression after one prior treatment with cytokine therapy for advanced RCC. 2017-08-24 EMA
Click to view menadiol sodium diphosphate a Vitamin K derivative, it has been found to have carcinogenic potential in mammalian cells as well as cytotoxic properties. Studies involving the active metabolite of this formulation, menadione, showed oocyte toxicity in a study of mice. 1941 FDA
Click to view brexpiprazole D(1A) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21728, gene: DRD1, swissprot: DRD1_HUMAN) agonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/24947465) D(4) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21917, gene: DRD4, swissprot: DRD4_HUMAN) agonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/24947465) 5-hydroxytryptamine receptor 1B (Organism: Homo sapiens, class: GPCR, accessions: P28222, gene: HTR1B, swissprot: 5HT1B_HUMAN) 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) 5-hydroxytryptamine receptor 5A (Organism: Homo sapiens, class: GPCR, accessions: P47898, gene: HTR5A, swissprot: 5HT5A_HUMAN) 5-hydroxytryptamine receptor 6 (Organism: Homo sapiens, class: GPCR, accessions: P50406, gene: HTR6, swissprot: 5HT6R_HUMAN) Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/205422s000lbl.pdf) Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) Beta-1 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08588, gene: ADRB1, swissprot: ADRB1_HUMAN) Beta-2 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P07550, gene: ADRB2, swissprot: ADRB2_HUMAN) Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/24947465) Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/24947465) Sodium-dependent dopamine transporter (Organism: Homo sapiens, class: Transporter, accessions: Q01959, gene: SLC6A3, swissprot: SC6A3_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/24947465) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) agonist (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/205422s000lbl.pdf) D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/205422s000lbl.pdf) 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) agonist (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/205422s000lbl.pdf) 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) antagonist (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/205422s000lbl.pdf) 5-hydroxytryptamine receptor 2B (Organism: Homo sapiens, class: GPCR, accessions: P41595, gene: HTR2B, swissprot: 5HT2B_HUMAN) antagonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/24947465) Alpha-1B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35368, gene: ADRA1B, swissprot: ADA1B_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/205422s000lbl.pdf) Alpha-2C adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18825, gene: ADRA2C, swissprot: ADA2C_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/205422s000lbl.pdf) Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/205422s000lbl.pdf) 5-hydroxytryptamine receptor 7 (Organism: Homo sapiens, class: GPCR, accessions: P34969, gene: HTR7, swissprot: 5HT7R_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/205422s000lbl.pdf) Alpha-1D adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P25100, gene: ADRA1D, swissprot: ADA1D_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/205422s000lbl.pdf) Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/205422s000lbl.pdf) an atypical antipsychotic the efficacy of brexpiprazole may be mediated through a combination of partial agonist activity at serotonin 5-HT1A and dopamine D2 receptors, and antagonist activity at serotonin 5-HT2A receptors Atypical Antipsychotic (Code: N0000175430) Dopamine Agents (Code: D015259) Dopamine Agonists (Code: D018491) Neurotransmitter Agents (Code: D018377) Serotonin Agents (Code: D018490) 2015-07-10 FDA
Click to view eluxadoline Kappa-type opioid receptor (Organism: Cavia porcellus, class: GPCR, accessions: P41144, gene: OPRK1, swissprot: OPRK_CAVPO) agonist (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206940s000lbl.pdf) Mu-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P35372, gene: OPRM1, swissprot: OPRM_HUMAN) agonist (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206940s000lbl.pdf) Kappa-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P41145, gene: OPRK1, swissprot: OPRK_HUMAN) agonist (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206940s000lbl.pdf) Delta-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P41143, gene: OPRD1, swissprot: OPRD_HUMAN) antagonist (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206940s000lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25491493) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25491493) Eluxadoline is a mu-opioid receptor agonist; eluxadoline is also a delta opioid receptor antagonist and a kappa opioid receptor agonist. The binding affinities (Ki) of eluxadoline for the human mu and delta opioid receptors are 1.8 nM and 430 nM, respectively. The binding affinity (Ki) of eluxadoline for the human kappa opioid receptor has not been determined; however, the Ki for guinea pig cerebellum kappa opioid receptor is 55 nM. In animals, eluxadoline interacts with opioid receptors in the gut. mu-opioid receptor agonist (Code: CHEBI:55322) delta-opioid receptor antagonist (Code: CHEBI:59283) kappa-opioid receptor agonist (Code: CHEBI:59282) gastrointestinal drug (Code: CHEBI:55324) Gastrointestinal Agents (Code: D005765) Opioid mu-Receptor Agonists (Code: N0000191866) 2015-05-27 FDA
Click to view deoxycholic acid Cell membrane (Organism: None, class: Cell membrane, accessions: None, gene: None, swissprot: None) other (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206333Orig1s000lbl.pdf) fMet-Leu-Phe receptor (Organism: Homo sapiens, class: GPCR, accessions: P21462, gene: FPR1, swissprot: FPR1_HUMAN) antagonist (Source: ) G-protein coupled bile acid receptor 1 (Organism: Homo sapiens, class: GPCR, accessions: Q8TDU6, gene: GPBAR1, swissprot: GPBAR_HUMAN) agonist (Source: ) Steroid Delta-isomerase (Organism: Pseudomonas putida, class: Enzyme, accessions: P07445, gene: ksi, swissprot: SDIS_PSEPU) (Source: https://www.ncbi.nlm.nih.gov/pubmed/?term=11007792) Choloylglycine hydrolase (Organism: Clostridium perfringens (strain 13 / Type A), class: Enzyme, accessions: P54965, gene: cbh, swissprot: CBH_CLOPE) (Source: https://www.ncbi.nlm.nih.gov/pubmed/?term=15823032) Lactaldehyde dehydrogenase (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P25553, gene: aldA, swissprot: ALDA_ECOLI) (Source: https://www.rcsb.org/structure/2OPX) Troponin C, slow skeletal and cardiac muscles (Organism: Homo sapiens, class: Cytosolic other, accessions: P63316, gene: TNNC1, swissprot: TNNC1_HUMAN) (Source: https://www.ncbi.nlm.nih.gov/pubmed/?term=21920370) Protein PrgI (Organism: Salmonella typhimurium (strain LT2 / SGSC1412 / ATCC 700720), class: Transporter, accessions: P41784, gene: prgI, swissprot: PRGI_SALTY) (Source: https://www.ncbi.nlm.nih.gov/pubmed/?term=21829362) Multidrug efflux pump subunit AcrB (Organism: Escherichia coli (strain K12), class: Transporter, accessions: P31224, gene: acrB, swissprot: ACRB_ECOLI) (Source: https://www.ncbi.nlm.nih.gov/pubmed/?term=19023693) A bile acid formed by bacterial action from cholate. It is usually conjugated with glycine or taurine. Deoxycholic acid acts as a detergent to solubilize fats for intestinal absorption, is reabsorbed itself, and is used as a choleretic and detergent. Cytolytic Agent (Code: N0000191548) Decreased Cell Membrane Integrity (Code: N0000008476) Cholagogues and Choleretics (Code: D002756) Gastrointestinal Agents (Code: D005765) 2015-04-29 FDA DXC
Click to view triamcinolone hexacetonide Glucocorticoid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P04150, gene: NR3C1, swissprot: GCR_HUMAN) agonist (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2014/016466s046lbl.pdf) synthetic glucocorticoid analog used for anti-inflammatory effects in disorders of many organ systems Anti-Inflammatory Agents (Code: D000893) 1969-07-29 FDA
Click to view ombitasvir Genome polyprotein (Organism: Hepatitis C virus genotype 1a (isolate H), class: Polyprotein, accessions: P27958, gene: None, swissprot: POLG_HCVH) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206619s003lbl.pdf) Genome polyprotein (Organism: Hepatitis C virus genotype 1b (isolate BK), class: Polyprotein, accessions: P26663, gene: None, swissprot: POLG_HCVBK) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206619s003lbl.pdf) UDP-glucuronosyltransferase 1-1 (Organism: Homo sapiens, class: Enzyme, accessions: P22309, gene: UGT1A1, swissprot: UD11_HUMAN) inhibitor (Source: https://www.ema.europa.eu/documents/product-information/viekirax-epar-product-information_en.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.ema.europa.eu/documents/product-information/viekirax-epar-product-information_en.pdf) an orally available inhibitor of the hepatitis C virus (HCV) non-structural protein 5A (NS5A) replication complex, with potential activity against HCV. Upon oral administration and after intracellular uptake, ombitasvir binds to and blocks the activity of the NS5A protein. This results in the disruption of the viral RNA replication complex, blockage of HCV RNA production, and inhibition of viral replication. NS5A, a zinc-binding and proline-rich hydrophilic phosphoprotein, plays a crucial role in HCV RNA replication. HCV is a small, enveloped, single-stranded RNA virus belonging to the Flaviviridae family; HCV infection is associated with the development of hepatocellular carcinoma (HCC). antiviral drug (Code: CHEBI:36044) Hepatitis C Virus NS5A Inhibitor (Code: N0000191256) UGT1A1 Inhibitors (Code: N0000191272) 2014-11-20 EMA
Click to view isavuconazonium Aspergillus fumigatus (Organism: None, class: Fungi, accessions: None, gene: None, swissprot: None) minimum inhibitory concentration (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/207500Orig1s000lbl.pdf) Candida albicans (Organism: None, class: Fungi, accessions: None, gene: None, swissprot: None) minimum inhibitory concentration (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/207500Orig1s000lbl.pdf) Isavuconazonium sulfate is the prodrug of isavuconazole, an azole antifungal drug. Isavuconazole inhibits the synthesis of ergosterol, a key component of the fungal cell membrane, through the inhibition of cytochrome P-450 dependent enzyme lanosterol 14-alpha-demethylase. This enzyme is responsible for the conversion of lanosterol to ergosterol. An accumulation of methylated sterol precursors and a depletion of ergosterol within the fungal cell membrane weakens the membrane structure and function. Mammalian cell demethylation is less sensitive to isavuconazole inhibition. prodrug (Code: CHEBI:50266) orphan drug (Code: CHEBI:71031) Azole Antifungal (Code: N0000175487) Azoles (Code: N0000008217) Cytochrome P450 3A4 Inhibitors (Code: N0000182141) Organic Cation Transporter 2 Inhibitors (Code: N0000187061) P-Glycoprotein Inhibitors (Code: N0000185503) 2015-03-06 FDA
Click to view isoflupredone acetate Isoflupredone acetate is a derivative of Isoflupredone. Isoflupredone acetate belongs to the class of corticosteroids and exerts its therapeutic effect by binding to glucocorticoid and mineralocorticoid receptors. Isoflupredone acetate is ussualy used in veterinary medicine.
Click to view drofenine Transient receptor potential cation channel subfamily V member 3 (Organism: Homo sapiens, class: Ion Channel, accessions: Q8NET8, gene: TRPV3, swissprot: TRPV3_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/25089200) Drofenine is an atropine-like antispasmodic drug, like papaverine, that acts directly on smooth muscles to stop muscle spasms. Drofenine is used for relaxing smooth muscle, treating dysmenorrhea, and relieving pain in the gastrointestinal tract, biliary passages, and urogenital tract.
Click to view tenofovir alafenamide a phosphonoamidate prodrug of tenofovir (2'deoxyadenosine monophosphate analog). Plasma exposure to tenofovir alafenamide allows for permeation into cells and then tenofovir alafenamide is intracellularly converted to tenofovir through hydrolysis by cathepsin A. Tenofovir is subsequently phosphorylated by cellular kinases to the active metabolite tenofovir diphosphate. Tenofovir diphosphate inhibits HIV replication through incorporation into viral DNA by the HIV reverse transcriptase, which results in DNA chain-termination antiviral drug (Code: CHEBI:36044) prodrug (Code: CHEBI:50266) 2015-05-11 FDA
Click to view avibactam Beta-lactamase TEM (Organism: Escherichia coli, class: Enzyme, accessions: P62593, gene: bla; blaT-3; blaT-4;, swissprot: BLAT_ECOLX) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20921316) Beta-lactamase (Organism: Enterobacter cloacae, class: Enzyme, accessions: P05364, gene: ampC, swissprot: AMPC_ENTCL) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20921316) Solute carrier family 22 member 6 (Organism: Homo sapiens, class: Transporter, accessions: Q4U2R8, gene: SLC22A6, swissprot: S22A6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/206494s005,s006lbl.pdf) Solute carrier family 22 member 8 (Organism: Homo sapiens, class: Transporter, accessions: Q8TCC7, gene: SLC22A8, swissprot: S22A8_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/206494s005,s006lbl.pdf) Avibactam is a non-beta-lactam beta-lactamase inhibitor that inactivates some beta-lactamases and protects ceftazidime from degradation by certain beta-lactamases. Avibactam in combination with ceftazidime is used for the treatment of complicated intra-abdominal infections (caused by Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis, Enterobacter cloacae, Klebsiella oxytoca, Citrobacter freundii complex, and Pseudomonas aeruginosa), complicated urinary tract infections (caused by Escherichia coli, Klebsiella pneumoniae, Enterobacter cloacae, Citrobacter freundii complex, Proteus mirabilis, and Pseudomonas aeruginosa) and hospital-acquired bacterial pneumonia and ventilator-associated bacterial pneumonia (caused by Klebsiella pneumoniae, Enterobacter cloacae, Escherichia coli, Serratia marcescens, Proteus mirabilis, Pseudomonas aeruginosa, and Haemophilus influenzae). antibacterial drug (Code: CHEBI:36047) beta Lactamase Inhibitor (Code: N0000175930) beta Lactamase Inhibitors (Code: N0000000202) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) beta-Lactamase Inhibitors (Code: D065093) Enzyme Inhibitors (Code: D004791) 2015-02-25 FDA
Click to view daclatasvir Genome polyprotein (Organism: Hepatitis C virus genotype 1a (isolate H), class: Polyprotein, accessions: P27958, gene: None, swissprot: POLG_HCVH) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/206843s008lbl.pdf) Genome polyprotein (Organism: Hepatitis C virus genotype 1b (isolate BK), class: Polyprotein, accessions: P26663, gene: None, swissprot: POLG_HCVBK) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/206843s008lbl.pdf) Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/206843s008lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/206843s008lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/206843s008lbl.pdf) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/206843s008lbl.pdf) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/206843s008lbl.pdf) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/206843s008lbl.pdf) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion Channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/24521299) Daclatasvir is an inhibitor of hepatitis C virus nonstructural protein 5A (NS5A). Daclatasvir binds to the N-terminus of NS5A and inhibits both viral RNA replication and virion assembly. Daclatasvir is indicated for use with sofosbuvir, with or without ribavirin, for the treatment of chronic HCV genotype 1 or 3 infection. antiviral drug (Code: CHEBI:36044) Hepatitis C Virus NS5A Inhibitor (Code: N0000191256) P-Glycoprotein Inhibitors (Code: N0000185503) Organic Anion Transporting Polypeptide 1B1 Inhibitors (Code: N0000190107) Organic Anion Transporting Polypeptide 1B3 Inhibitors (Code: N0000190108) Breast Cancer Resistance Protein Inhibitors (Code: N0000190113) 2014-09-15 EMA
Click to view palbociclib Cyclin-dependent kinase 4 (Organism: Homo sapiens, class: Kinase, accessions: P11802, gene: CDK4, swissprot: CDK4_HUMAN) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/207103s000lbl.pdf) Cyclin-dependent kinase 6 (Organism: Homo sapiens, class: Kinase, accessions: Q00534, gene: CDK6, swissprot: CDK6_HUMAN) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/207103s000lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/207103s000lbl.pdf) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/207103s000lbl.pdf) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/207103s000lbl.pdf) Solute carrier family 22 member 6 (Organism: Homo sapiens, class: Transporter, accessions: Q4U2R8, gene: SLC22A6, swissprot: S22A6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/207103s000lbl.pdf) Solute carrier family 22 member 8 (Organism: Homo sapiens, class: Transporter, accessions: Q8TCC7, gene: SLC22A8, swissprot: S22A8_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/207103s000lbl.pdf) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/207103s000lbl.pdf) Palbociclib is an inhibitor of cyclin-dependent kinases (CDK) 4 and 6. Cyclin D1 and CDK4/6 are downstream of signaling pathways which lead to cellular proliferation. In vitro, palbociclib reduced cellular proliferation of estrogen receptor (ER)-positive breast cancer cell lines by blocking progression of the cell from G1 into S phase of the cell cycle. Treatment of breast cancer cell lines with the combination of palbociclib and antiestrogens leads to decreased retinoblastoma (Rb) protein phosphorylation resulting in reduced E2F expression and signaling, and increased growth arrest compared to treatment with each drug alone. In vitro treatment of ER-positive breast cancer cell lines with the combination of palbociclib and antiestrogens led to increased cell senescence compared to each drug alone, which was sustained for up to 6 days following palbociclib removal and was greater if antiestrogen treatment was continued. In vivo studies using a patient-derived ER-positive breast cancer xenograft model demonstrated that the combination of palbociclib and letrozole increased the inhibition of Rb phosphorylation, downstream signaling, and tumor growth compared to each drug alone. antineoplastic agent (Code: CHEBI:35610) Kinase Inhibitor (Code: N0000175605) Kinase Inhibitors (Code: N0000175082) Cytochrome P450 3A Inhibitors (Code: N0000190114) Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Protein Kinase Inhibitors (Code: D047428) 2015-02-03 FDA LQQ
Click to view lenvatinib Proto-oncogene tyrosine-protein kinase receptor Ret (Organism: Homo sapiens, class: Kinase, accessions: P07949, gene: RET, swissprot: RET_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206947s000lbl.pdf1) Vascular endothelial growth factor receptor 1 (Organism: Homo sapiens, class: Kinase, accessions: P17948, gene: FLT1, swissprot: VGFR1_HUMAN) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206947s000lbl.pdf) Vascular endothelial growth factor receptor 2 (Organism: Homo sapiens, class: Kinase, accessions: P35968, gene: KDR, swissprot: VGFR2_HUMAN) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206947s000lbl.pdf) Vascular endothelial growth factor receptor 3 (Organism: Homo sapiens, class: Kinase, accessions: P35916, gene: FLT4, swissprot: VGFR3_HUMAN) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206947s000lbl.pdf) Fibroblast growth factor receptor 1 (Organism: Homo sapiens, class: Kinase, accessions: P11362, gene: FGFR1, swissprot: FGFR1_HUMAN) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206947s000lbl.pdf) Platelet-derived growth factor receptor alpha (Organism: Homo sapiens, class: Kinase, accessions: P16234, gene: PDGFRA, swissprot: PGFRA_HUMAN) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206947s000lbl.pdf) Mast/stem cell growth factor receptor Kit (Organism: Homo sapiens, class: Kinase, accessions: P10721, gene: KIT, swissprot: KIT_HUMAN) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206947s000lbl.pdf) Fibroblast growth factor receptor 2 (Organism: Homo sapiens, class: Kinase, accessions: P21802, gene: FGFR2, swissprot: FGFR2_HUMAN) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206947s000lbl.pdf) Fibroblast growth factor receptor 3 (Organism: Homo sapiens, class: Kinase, accessions: P22607, gene: FGFR3, swissprot: FGFR3_HUMAN) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206947s000lbl.pdf) Fibroblast growth factor receptor 4 (Organism: Homo sapiens, class: Kinase, accessions: P22455, gene: FGFR4, swissprot: FGFR4_HUMAN) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206947s000lbl.pdf) UDP-glucuronosyltransferase 1-1 (Organism: Homo sapiens, class: Enzyme, accessions: P22309, gene: UGT1A1, swissprot: UD11_HUMAN) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206947s000lbl.pdf) UDP-glucuronosyltransferase 1-4 (Organism: Homo sapiens, class: Enzyme, accessions: P22310, gene: UGT1A4, swissprot: UD14_HUMAN) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206947s000lbl.pdf) Solute carrier family 22 member 8 (Organism: Homo sapiens, class: Transporter, accessions: Q8TCC7, gene: SLC22A8, swissprot: S22A8_HUMAN) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206947s000lbl.pdf) Solute carrier family 22 member 6 (Organism: Homo sapiens, class: Transporter, accessions: Q4U2R8, gene: SLC22A6, swissprot: S22A6_HUMAN) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206947s000lbl.pdf) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206947s000lbl.pdf) Solute carrier family 22 member 1 (Organism: Homo sapiens, class: Transporter, accessions: O15245, gene: SLC22A1, swissprot: S22A1_HUMAN) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206947s000lbl.pdf) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206947s000lbl.pdf) Bile salt export pump (Organism: Homo sapiens, class: Transporter, accessions: O95342, gene: ABCB11, swissprot: ABCBB_HUMAN) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206947s000lbl.pdf) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/206947s009lbl.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/206947s009lbl.pdf) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/206947s009lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/206947s009lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/206947s009lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/206947s009lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/206947s009lbl.pdf) Lenvatinib is orally available multi-kinase inhibitor and antineoplastic agent that is used in treatment of advanced, metastatic medullary thyroid cancer and refractory renal cell carcinoma. Lenvatinib is associated with a modest rate of serum enzyme elevations during treatment and has been implicated to rare instances of clinically apparent, acute liver injury some of which have been fatal. orphan drug (Code: CHEBI:71031) antineoplastic agent (Code: CHEBI:35610) Kinase Inhibitor (Code: N0000175605) Receptor Tyrosine Kinase Inhibitors (Code: N0000020000) Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Protein Kinase Inhibitors (Code: D047428) 2015-02-13 FDA LEV
Click to view decamethoxine Decamethoxin is a bisquaternary ammonium salt, which close to ethonium in chemical structure and antimicrobial effect. It has a wide range of antimicrobial effects on gram-positive (staphylococcus, streptococcus, pneumococcus), gram-negative (gonococcus, meningococcus) cocci, corynebacteria diphtheria, enterobacteria, pseudomonas, protozoa, dermatophytes, yeast-like fungi of the genus Candida. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Anti-Infective Agents, Local (Code: D000891) 2008-10-17 Ministry of Health of the Russian Federation
Click to view finafloxacin DNA gyrase (Organism: Staphylococcus aureus subsp. aureus, class: Enzyme, accessions: P20831|P0A0K8, gene: gyrA|gyrB, swissprot: GYRA_STAAU|GYRB_STAAU) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/206307s000lbl.pdf) DNA gyrase (Organism: Pseudomonas aeruginosa, class: Enzyme, accessions: P48372|Q9I7C2, gene: gyrA|gyrB, swissprot: GYRA_PSEAE|GYRB_PSEAE) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/206307s000lbl.pdf) Topoisomerase IV (Organism: Staphylococcus aureus subsp. aureus, class: Enzyme, accessions: P0C1U9|P0C1S7, gene: parC|parE, swissprot: PARC_STAAU|PARE_STAAU) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/206307s000lbl.pdf) Topoisomerase IV (Organism: Pseudomonas aeruginosa, class: Enzyme, accessions: Q9HUK1|Q9HUJ8, gene: parC|parE, swissprot: PARC_PSEAE|PARE_PSEAE) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/206307s000lbl.pdf) Finafloxacin belongs to the fluoroquinolone class of antibacterials which involves the inhibition of bacterial type II topoisomerase enzymes, DNA gyrase and topoisomerase IV, which are required for bacterial DNA replication, transcription, repair and recombination. antibacterial drug (Code: CHEBI:36047) Quinolone Antimicrobial (Code: N0000175937) Quinolones (Code: N0000007606) 2014-12-17 FDA
Click to view safinamide Amine oxidase [flavin-containing] B (Organism: Homo sapiens, class: Enzyme, accessions: P27338, gene: MAOB, swissprot: AOFB_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/207145lbl.pdf) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/207145lbl.pdf) Safinamide acts through both dopaminergic and non-dopaminergic mechanisms of action. Safinamide is a highly selective and reversible MAO-B inhibitor causing an increase in extracellular levels of dopamine in the striatum. Safinamide is associated with state-dependent inhibition of voltage-gated sodium (Na+) channels, and modulation of stimulated release of glutamate. To what extent the nondopaminergic effects contribute to the overall effect has not been established. Monoamine Oxidase Type B Inhibitor (Code: N0000175762) Monoamine Oxidase-B Inhibitors (Code: N0000175761) Breast Cancer Resistance Protein Inhibitors (Code: N0000190113) 2014-03-30 EMA
Click to view ceftolozane Peptidoglycan D,D-transpeptidase FtsI (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P0AD68, gene: ftsI, swissprot: FTSI_ECOLI) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/206829lbl.pdf) Peptidoglycan D,D-transpeptidase FtsI (Organism: Pseudomonas aeruginosa, class: Enzyme, accessions: Q51504, gene: pbpB, swissprot: Q51504_PSEAI) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/206829lbl.pdf) Penicillin-binding protein 1B (Organism: Pseudomonas aeruginosa, class: Enzyme, accessions: Q9X6W0, gene: ponB, swissprot: Q9X6W0_PSEAI) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/206829lbl.pdf) Ceftolozane belongs to the cephalosporin class of antibacterial drugs. The bactericidal action of ceftolozane results from inhibition of cell wall biosynthesis, and is mediated through binding to penicillin-binding proteins (PBPs). Ceftolozane is an inhibitor of PBPs of P. aeruginosa (e.g., PBP1b, PBP1c, and PBP3) and E. coli (e.g., PBP3). Cephalosporin Antibacterial (Code: N0000175488) Cephalosporins (Code: N0000011161) 2014-12-19 FDA
Click to view acotiamide Acetylcholinesterase (Organism: Rattus norvegicus (Rat), class: Enzyme, accessions: P37136, gene: Ache, swissprot: ACES_RAT) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/21651906) A prokinetic agent with gastrointestinal (GI) motility-enhancing activity. Although the exact mechanism by which acotiamide exerts its effect has yet to be fully elucidated, this agent appears to inhibit acetylcholinesterase (AchE), an enzyme responsible for the breakdown of acetylcholine (Ach). Increased Ach concentrations lead to an improvement of gastric emptying and GI motility and eventually to a reduction of dyspepsia symptoms. 2013-03-25 PMDA
Click to view felypressin Vasopressin V1a receptor (Organism: Homo sapiens, class: GPCR, accessions: P37288, gene: AVPR1A, swissprot: V1AR_HUMAN) agonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/18655903) A synthetic analog of LYPRESSIN with a PHENYLALANINE substitution at residue 2. Felypressin is a vasoconstrictor with reduced antidiuretic activity. vasoconstrictor agent (Code: CHEBI:50514) vasopressin receptor agonist (Code: CHEBI:59727) Cardiovascular Agents (Code: D002317) Vasoconstrictor Agents (Code: D014662) 1969-12-31 New Zealand Medicines and Medical Devices Safety Authority
Click to view netupitant Substance-P receptor (Organism: Homo sapiens, class: GPCR, accessions: P25103, gene: TACR1, swissprot: NK1R_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205718s000lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205718s000lbl.pdf) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205718s000lbl.pdf) a selective antagonist of human substance P/neurokinin 1 (NK1) receptors, inhibits substance P mediated emesis responses antiemetic (Code: CHEBI:50919) Neurokinin 1 Antagonists (Code: N0000010262) Substance P/Neurokinin-1 Receptor Antagonist (Code: N0000175786) Cytochrome P450 3A4 Inhibitors (Code: N0000182141) P-Glycoprotein Inhibitors (Code: N0000185503) Breast Cancer Resistance Protein Inhibitors (Code: N0000190113) 2014-10-10 FDA
Click to view ledipasvir Genome polyprotein (Organism: Hepatitis C virus genotype 1a (isolate H), class: Polyprotein, accessions: P27958, gene: None, swissprot: POLG_HCVH) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205834s000lbl.pdf) Genome polyprotein (Organism: Hepatitis C virus genotype 1b (isolate BK), class: Polyprotein, accessions: P26663, gene: None, swissprot: POLG_HCVBK) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205834s000lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205834s000lbl.pdf) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205834s000lbl.pdf) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205834s000lbl.pdf) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205834s000lbl.pdf) Bile salt export pump (Organism: Homo sapiens, class: Transporter, accessions: O95342, gene: ABCB11, swissprot: ABCBB_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205834s000lbl.pdf) Ledipasvir is an inhibitor of the Hepatitis C Virus (HCV) NS5A protein required for viral RNA replication and assembly of HCV virions. Ledipasvir is indicated in combination with sofosbuvir for the treatment of HCV genotype 1 with or without cirrhosis. antiviral drug (Code: CHEBI:36044) Hepatitis C Virus NS5A Inhibitor (Code: N0000191256) P-Glycoprotein Inhibitors (Code: N0000185503) Breast Cancer Resistance Protein Inhibitors (Code: N0000190113) Anti-Infective Agents (Code: D000890) Antiviral Agents (Code: D000998) 2014-10-10 FDA
Click to view diquafosol P2Y purinoceptor 2 (Organism: Homo sapiens, class: GPCR, accessions: P41231, gene: P2RY2, swissprot: P2RY2_HUMAN) agonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/18232657) P2Y purinoceptor 6 (Organism: Homo sapiens, class: GPCR, accessions: Q15077, gene: P2RY6, swissprot: P2RY6_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/22107038) Diquafosol is an agonist for purinergic P2Y2 receptor. Diquafosol stimulated water and mucin secretion by acting on the conjunctival epithelial and goblet cell membrane and elevating intracellular calcium ion concentrations. Diquafosol is approved for the treatment of dry eye. 2010-02-26 PMDA
Click to view belinostat Histone deacetylase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P56524, gene: HDAC4, swissprot: HDAC4_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/12939461) Histone deacetylase 10 (Organism: Homo sapiens, class: Enzyme, accessions: Q969S8, gene: HDAC10, swissprot: HDA10_HUMAN) inhibitor (Source: ) Histone deacetylase 11 (Organism: Homo sapiens, class: Enzyme, accessions: Q96DB2, gene: HDAC11, swissprot: HDA11_HUMAN) inhibitor (Source: ) Histone deacetylase 8 (Organism: Homo sapiens, class: Enzyme, accessions: Q9BY41, gene: HDAC8, swissprot: HDAC8_HUMAN) inhibitor (Source: ) Histone deacetylase 9 (Organism: Homo sapiens, class: Enzyme, accessions: Q9UKV0, gene: HDAC9, swissprot: HDAC9_HUMAN) inhibitor (Source: ) Histone deacetylase 6 (Organism: Homo sapiens, class: Enzyme, accessions: Q9UBN7, gene: HDAC6, swissprot: HDAC6_HUMAN) inhibitor (Source: ) Histone deacetylase 1 (Organism: Homo sapiens, class: Enzyme, accessions: Q13547, gene: HDAC1, swissprot: HDAC1_HUMAN) inhibitor (Source: ) Histone deacetylase 3 (Organism: Homo sapiens, class: Enzyme, accessions: O15379, gene: HDAC3, swissprot: HDAC3_HUMAN) inhibitor (Source: ) Histone deacetylase 2 (Organism: Homo sapiens, class: Enzyme, accessions: Q92769, gene: HDAC2, swissprot: HDAC2_HUMAN) inhibitor (Source: ) Histone deacetylase 5 (Organism: Homo sapiens, class: Enzyme, accessions: Q9UQL6, gene: HDAC5, swissprot: HDAC5_HUMAN) inhibitor (Source: ) Histone deacetylase 7 (Organism: Homo sapiens, class: Enzyme, accessions: Q8WUI4, gene: HDAC7, swissprot: HDAC7_HUMAN) inhibitor (Source: ) Belinostat is a hydroxamate-type histone deacetylase inhibitor. Belinostat causes the accumulation of acetylated histones and other proteins, inducing cell cycle arrest and/or apoptosis of some transformed cells. Belinostat targets HDAC enzymes, thereby inhibiting tumor cell proliferation, inducing apoptosis, promoting cellular differentiation, and inhibiting angiogenesis. This agent may sensitize drug-resistant tumor cells to other antineoplastic agents, possibly through a mechanism involving the down-regulation of thymidylate synthase. Belinostat is indicated for the treatment of relapsed or refractory peripheal T-cell lymphoma. antineoplastic agent (Code: CHEBI:35610) Histone Deacetylase Inhibitor (Code: N0000175588) Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Histone Deacetylase Inhibitors (Code: D056572) 2014-07-03 FDA 5OG
Click to view imidafenacin Muscarinic acetylcholine receptor M1 (Organism: Rattus norvegicus, class: GPCR, accessions: P08482, gene: Chrm1, swissprot: ACM1_RAT) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/17396619) Muscarinic acetylcholine receptor M3 (Organism: Rattus norvegicus, class: GPCR, accessions: P10980, gene: Chrm3, swissprot: ACM3_RAT) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/17396619) Muscarinic acetylcholine receptor M2 (Organism: Rattus norvegicus, class: GPCR, accessions: P08483, gene: Chrm2, swissprot: ACM2_RAT) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/17396619) Imidafenacin antagonizes subtypes M3 and M1 in vitro. In the urinary bladder, imidafenacin inhibits acetylcholine release by antagonizing subtype M1 and contraction of smooth muscles by antagonizing subtype M3. 2007-04-18 PMDA
Click to view nintedanib Vascular endothelial growth factor receptor 2 (Organism: Homo sapiens, class: Kinase, accessions: P35968, gene: KDR, swissprot: VGFR2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205832s000lbl.pdf) Fibroblast growth factor receptor 1 (Organism: Homo sapiens, class: Kinase, accessions: P11362, gene: FGFR1, swissprot: FGFR1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205832s000lbl.pdf) Fibroblast growth factor receptor 2 (Organism: Homo sapiens, class: Kinase, accessions: P21802, gene: FGFR2, swissprot: FGFR2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205832s000lbl.pdf) Fibroblast growth factor receptor 3 (Organism: Homo sapiens, class: Kinase, accessions: P22607, gene: FGFR3, swissprot: FGFR3_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205832s000lbl.pdf) Platelet-derived growth factor receptor alpha (Organism: Homo sapiens, class: Kinase, accessions: P16234, gene: PDGFRA, swissprot: PGFRA_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205832s000lbl.pdf) Vascular endothelial growth factor receptor 1 (Organism: Homo sapiens, class: Kinase, accessions: P17948, gene: FLT1, swissprot: VGFR1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205832s000lbl.pdf) Vascular endothelial growth factor receptor 3 (Organism: Homo sapiens, class: Kinase, accessions: P35916, gene: FLT4, swissprot: VGFR3_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205832s000lbl.pdf) Receptor-type tyrosine-protein kinase FLT3 (Organism: Homo sapiens, class: Kinase, accessions: P36888, gene: FLT3, swissprot: FLT3_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205832s000lbl.pdf) Tyrosine-protein kinase Lck (Organism: Homo sapiens, class: Kinase, accessions: P06239, gene: LCK, swissprot: LCK_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205832s000lbl.pdf) Tyrosine-protein kinase Lyn (Organism: Homo sapiens, class: Kinase, accessions: P07948, gene: LYN, swissprot: LYN_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205832s000lbl.pdf) Proto-oncogene tyrosine-protein kinase Src (Organism: Homo sapiens, class: Kinase, accessions: P12931, gene: SRC, swissprot: SRC_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205832s000lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205832s000lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205832s000lbl.pdf) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205832s000lbl.pdf) Solute carrier family 22 member 1 (Organism: Homo sapiens, class: Transporter, accessions: O15245, gene: SLC22A1, swissprot: S22A1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205832s000lbl.pdf) Nintedanib is a small molecule that inhibits multiple receptor tyrosine kinases (RTKs) and non-receptor tyrosine kinases (nRTKs). Nintedanib is a drug indicated for the treatment of idiopathic pulmonary fibrosis (IPF). antineoplastic agent (Code: CHEBI:35610) angiogenesis inhibitor (Code: CHEBI:48422) Kinase Inhibitor (Code: N0000175605) Protein Kinase Inhibitors (Code: N0000175076) Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) 2014-10-15 FDA XIN
Click to view cetilistat Pancreatic triacylglycerol lipase (Organism: Homo sapiens, class: Enzyme, accessions: P16233, gene: PNLIP, swissprot: LIPP_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/18500680) Cetilistat is a pancreatic lipase inhibitor. Cetilistat is used for the treatment of obesity in patients with or without diabetes. Anti-Obesity Agents (Code: D019440) Central Nervous System Agents (Code: D002491) Enzyme Inhibitors (Code: D004791) Lipid Regulating Agents (Code: D057847) 2013-09-20 PMDA
Click to view efinaconazole Lanosterol 14-alpha demethylase (Organism: Trichophyton rubrum, class: Enzyme, accessions: None, gene: None, swissprot: None) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/203567s000lbl.pdf) Lanosterol 14-alpha demethylase (Organism: Trichophyton mentagrophytes, class: Enzyme, accessions: None, gene: None, swissprot: None) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/203567s000lbl.pdf) Efinaconazole is an azole antifungal. Efinaconazole inhibits fungal lanosterol 14-alpha demethylase involved in the biosynthesis of ergosterol, a constituent of fungal cell membranes. Azole Antifungal (Code: N0000175487) Azoles (Code: N0000008217) Anti-Infective Agents (Code: D000890) Antifungal Agents (Code: D000935) 2014-06-06 FDA
Click to view favipiravir Favipiravir is an anti-viral compound with a unique mechanism of action that is active against a wide range of RNA-based viruses in laboratory tests. Favipiravir is phosphoribosylated by cellular enzymes to its active form, favipiravir-ribofuranosyl-5'- triphosphate (RTP). Favipiravir is active against a broad range of influenza viruses, including A(H1N1)pdm09, A(H5N1) and A(H7N9) avian virus. It also inhibits influenza strains resistant to current antiviral drugs, and shows a synergistic effect in combination with oseltamivir, thereby expanding influenza treatment options. In addition to its anti-influenza activity, favipiravir blocks the replication of many other RNA viruses, including arenaviruses (Junin, Machupo and Pichinde); phleboviruses (Rift Valley fever, sandfly fever and Punta Toro); hantaviruses (Maporal, Dobrava, and Prospect Hill); flaviviruses (yellow fever and West Nile); enteroviruses (polio- and rhinoviruses); an alphavirus, Western equine encephalitis virus; a paramyxovirus, respiratory syncytial virus; and noroviruses. 2014-02-03 PMDA
Click to view topiroxostat Xanthine dehydrogenase/oxidase (Organism: Homo sapiens, class: Enzyme, accessions: P47989, gene: XDH, swissprot: XDH_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/19783139) Topiroxostat is a xanthine oxidase inhibitor. Topiroxostat could reduce the production of uric acid in the body through the inhibition of xanthine oxidase. Topiroxostat is used for the treatment of gout and hyperuricemia. Enzyme Inhibitors (Code: D004791) 2013-04-26 PMDA FYX
Click to view asunaprevir Genome polyprotein (Organism: Hepatitis C virus genotype 1a (isolate H), class: Polyprotein, accessions: P27958, gene: None, swissprot: POLG_HCVH) inhibitor (Source: https://pdf.hres.ca/dpd_pm/00037935.PDF) Genome polyprotein (Organism: Hepatitis C virus genotype 1b (isolate BK), class: Polyprotein, accessions: P26663, gene: None, swissprot: POLG_HCVBK) inhibitor (Source: https://pdf.hres.ca/dpd_pm/00037935.PDF) Genome polyprotein (Organism: Hepatitis C virus genotype 2a (isolate HC-J6), class: Polyprotein, accessions: P26660, gene: None, swissprot: POLG_HCVJ6) inhibitor (Source: https://pdf.hres.ca/dpd_pm/00037935.PDF) Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) substrate (Source: https://pdf.hres.ca/dpd_pm/00037935.PDF) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://pdf.hres.ca/dpd_pm/00037935.PDF) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) substrate (Source: https://pdf.hres.ca/dpd_pm/00037935.PDF) Solute carrier organic anion transporter family member 2B1 (Organism: Homo sapiens, class: Transporter, accessions: O94956, gene: SLCO2B1, swissprot: SO2B1_HUMAN) substrate (Source: https://pdf.hres.ca/dpd_pm/00037935.PDF) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://pdf.hres.ca/dpd_pm/00037935.PDF) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) inhibitor (Source: https://pdf.hres.ca/dpd_pm/00037935.PDF) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://pdf.hres.ca/dpd_pm/00037935.PDF) Solute carrier organic anion transporter family member 2B1 (Organism: Homo sapiens, class: Transporter, accessions: O94956, gene: SLCO2B1, swissprot: SO2B1_HUMAN) inhibitor (Source: https://pdf.hres.ca/dpd_pm/00037935.PDF) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://pdf.hres.ca/dpd_pm/00037935.PDF) Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) inducer (Source: https://pdf.hres.ca/dpd_pm/00037935.PDF) Solute carrier family 22 member 6 (Organism: Homo sapiens, class: Transporter, accessions: Q4U2R8, gene: SLC22A6, swissprot: S22A6_HUMAN) inhibitor (Source: https://pdf.hres.ca/dpd_pm/00037935.PDF) Solute carrier family 22 member 8 (Organism: Homo sapiens, class: Transporter, accessions: Q8TCC7, gene: SLC22A8, swissprot: S22A8_HUMAN) inhibitor (Source: https://pdf.hres.ca/dpd_pm/00037935.PDF) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) inhibitor (Source: https://pdf.hres.ca/dpd_pm/00037935.PDF) Solute carrier family 22 member 1 (Organism: Homo sapiens, class: Transporter, accessions: O15245, gene: SLC22A1, swissprot: S22A1_HUMAN) inhibitor (Source: https://pdf.hres.ca/dpd_pm/00037935.PDF) Bile salt export pump (Organism: Homo sapiens, class: Transporter, accessions: O95342, gene: ABCB11, swissprot: ABCBB_HUMAN) inhibitor (Source: https://pdf.hres.ca/dpd_pm/00037935.PDF) Asunaprevir is an inhibitor of the HCV NS3/4A serine protease complex. This NS3/4A enzyme complex is responsible for processing the HCV polyprotein to yield mature viral proteins required for viral replication. Studies in vitro demonstrated a significant antiviral activity in HCV replicon cell systems with an EC50 of 4nm and 1nm against the HCV genotype 1a and 1b respectively.2 These studies showed a limited activity against the genotypes 2 and 3. This property makes asunaprevir a highly selective anti-HCV agent that is not effective against HCV closely related virus. Asunaprevir is indicated in combination with other agents for the treatment of chronic hepatitis C in adult patients with hepatitis C virus genotypes 1 or 4 and compensated liver cirrhosis. Enzyme Inhibitors (Code: D004791) Protease Inhibitors (Code: D011480) 2014-06-24 PMDA 2R9
Click to view ipragliflozin Sodium/glucose cotransporter 2 (Organism: Homo sapiens, class: Transporter, accessions: P31639, gene: SLC5A2, swissprot: SC5A2_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/22139434) Sodium/glucose cotransporter 1 (Organism: Homo sapiens, class: Transporter, accessions: P13866, gene: SLC5A1, swissprot: SC5A1_HUMAN) Sodium/glucose cotransporter 1 (Organism: Mus musculus, class: Transporter, accessions: Q8C3K6, gene: Slc5a1, swissprot: SC5A1_MOUSE) inhibitor (Source: ) Sodium/glucose cotransporter 1 (Organism: Rattus norvegicus, class: Transporter, accessions: P53790, gene: Slc5a1, swissprot: SC5A1_RAT) inhibitor (Source: ) Sodium/glucose cotransporter 2 (Organism: Mus musculus, class: Transporter, accessions: Q923I7, gene: Slc5a2, swissprot: SC5A2_MOUSE) inhibitor (Source: ) Sodium/glucose cotransporter 2 (Organism: Rattus norvegicus, class: Transporter, accessions: P53792, gene: Slc5a2, swissprot: SC5A2_RAT) inhibitor (Source: ) Ipragliflozin is a selective sodium-glucose cotransporter 2 (SGLT2) inhibitor approved for the treatment of type 2 diabetes mellitus. 2014-11-29 PMDA
Click to view luseogliflozin Sodium/glucose cotransporter 2 (Organism: Homo sapiens, class: Transporter, accessions: P31639, gene: SLC5A2, swissprot: SC5A2_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/20302302) Sodium/glucose cotransporter 1 (Organism: Homo sapiens, class: Transporter, accessions: P13866, gene: SLC5A1, swissprot: SC5A1_HUMAN) Luseogliflozin is a sodium-dependent glucose cotransporter (SGLT) 2 inhibitior. Luseogliflozin exhibits a blood glucose lowering effect, excellent urinary glucose excretion properties, and promising pharmacokinetics profiles in animals. Luseogliflozin is used as monotherapy or in combination with other antihyperglycaemic agents for the treatment of patients with type 2 diabetes mellitus. 2014-03-24 PMDA
Click to view suvorexant Orexin receptor type 1 (Organism: Homo sapiens, class: GPCR, accessions: O43613, gene: HCRTR1, swissprot: OX1R_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204569s005lbl.pdf) Orexin receptor type 2 (Organism: Homo sapiens, class: GPCR, accessions: O43614, gene: HCRTR2, swissprot: OX2R_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204569s005lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204569s005lbl.pdf) Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204569s005lbl.pdf) Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204569s005lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204569s005lbl.pdf) Suvorexant is a selective dual antagonist of orexin receptors OX1R and OX2R that promotes sleep by reducing wakefulness and arousal. It has been approved for the treatment of insomnia. central nervous system depressant (Code: CHEBI:35488) Orexin Receptor Antagonist (Code: N0000191000) P-Glycoprotein Inhibitors (Code: N0000185503) Cytochrome P450 3A Inhibitors (Code: N0000190114) Neurotransmitter Agents (Code: D018377) Orexin Receptor Antagonists (Code: D000068796) Sleep Aids, Pharmaceutical (Code: D000068776) 2014-08-13 FDA SUV
Click to view istradefylline Adenosine receptor A1 (Organism: Homo sapiens, class: GPCR, accessions: P30542, gene: ADORA1, swissprot: AA1R_HUMAN Adenosine receptor A2a (Organism: Homo sapiens, class: GPCR, accessions: P29274, gene: ADORA2A, swissprot: AA2AR_HUMAN) antagonist Adenosine receptor A3 (Organism: Homo sapiens, class: GPCR, accessions: P0DMS8, gene: ADORA3, swissprot: AA3R_HUMAN Adenosine receptor A2a (Organism: Rattus norvegicus, class: GPCR, accessions: P30543, gene: Adora2a, swissprot: AA2AR_RAT Adenosine receptor A1 (Organism: Rattus norvegicus, class: GPCR, accessions: P25099, gene: Adora1, swissprot: AA1R_RAT Istradefylline is an adenosine A2A receptor antagonist. Istradefylline is indicated for the improvement of wearing-off phenomena in patients with Parkinson’s disease on concomitant treatment with levodopa-containing products. Adenosine A2 Receptor Antagonists (Code: D058917) Neurotransmitter Agents (Code: D018377) Purinergic Agents (Code: D058905) Purinergic Antagonists (Code: D058914) Purinergic P1 Receptor Antagonists (Code: D058915) 2013-03-8 PMDA
Click to view simetride Simetride is a analgesic agent indicated for low back pain, symptomatic neuralgia, headache, menstrual pain, pharyngalgia/earache due to inflammation, toothache, postoperative pain, combined with caffeine. 1965 PMDA
Click to view tedizolid phosphate Tedizolid phosphate a phosphate prodrug, is converted to tedizolid in the presence of phosphatases. The antibacterial activity of tedizolid is mediated by binding to the 50S subunit of the bacterial ribosome resulting in inhibition of protein synthesis. Tedizolid has been shown to be active against most isolates of the following bacteria: Staphylococcus aureus (including methicillin-resistant and methicillin-susceptible isolates), Streptococcus pyogenes, Streptococcus agalactiae, Streptococcus anginosus Group (including S. anginosus, S. intermedius, and S. constellatus), Enterococcus faecalis. prodrug (Code: CHEBI:50266) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Oxazolidinone Antibacterial (Code: N0000175495) Oxazolidinones (Code: N0000007568) Breast Cancer Resistance Protein Inhibitors (Code: N0000190113) 2014-06-20 FDA
Click to view tavaborole Leucine--tRNA ligase, cytoplasmic (Organism: Saccharomyces cerevisiae (strain ATCC 204508 / S288c), class: Enzyme, accessions: P26637, gene: CDC60, swissprot: SYLC_YEAST) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17588934) Tavaborole is a boron-based pharmaceutical agent. The mechanism of action of tavaborole is inhibition of fungal protein synthesis. Tavaborole inhibits protein synthesis by inhibition of an aminoacyl-transfer ribonucleic acid (tRNA) synthetase (AARS). Tavaborole is indicated for the topical treatment of toenail onychomycosis, a fungal infection of the nail and nail bed due to Trichophyton rubrum or Trichophyton mentagrophytes infection. Oxaborole Antifungal (Code: N0000191279) Protein Synthesis Inhibitors (Code: N0000000150) Boron Compounds (Code: N0000008253) Anti-Infective Agents (Code: D000890) Antifungal Agents (Code: D000935) 2014-07-07 FDA
Click to view idelalisib Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform (Organism: Homo sapiens, class: Kinase, accessions: O00329, gene: PIK3CD, swissprot: PK3CD_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/20959606) Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform (Organism: Homo sapiens, class: Kinase, accessions: P48736, gene: PIK3CG, swissprot: PK3CG_HUMAN) Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform (Organism: Homo sapiens, class: Kinase, accessions: P42338, gene: PIK3CB, swissprot: PK3CB_HUMAN) Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (Organism: Homo sapiens, class: Kinase, accessions: P42336, gene: PIK3CA, swissprot: PK3CA_HUMAN) DNA-dependent protein kinase catalytic subunit (Organism: Homo sapiens, class: Kinase, accessions: P78527, gene: PRKDC, swissprot: PRKDC_HUMAN Idelalisib is an inhibitor of PI3K-delta kinase, which is expressed in normal and malignant B-cells. Idelalisib induced apoptosis and inhibited proliferation in cell lines derived from malignant B-cells and in primary tumor cells. Idelalisib inhibits several cell signaling pathways, including B-cell receptor (BCR) signaling and the CXCR4 and CXCR5 signaling, which are involved in trafficking and homing of B-cells to the lymph nodes and bone marrow. antineoplastic agent (Code: CHEBI:35610) Kinase Inhibitor (Code: N0000175605) Kinase Inhibitors (Code: N0000175082) Cytochrome P450 3A Inhibitors (Code: N0000190114) Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) 2014-07-23 FDA 40L
Click to view ataluren Ataluren is approved for the treatment of Duchenne muscular dystrophy caused by a nonsense mutation. A nonsense mutation in DNA results in a premature stop codon within an mRNA. This premature stop codon in the mRNA causes disease by terminating translation before a full-length protein is generated. Ataluren interacts with the ribosome enabling it to read through premature nonsense stop signals on mRNA and allowing the cell to produce a full-length, functional protein. 2014-07-31 EMA
Click to view mebanazine Amine oxidase [flavin-containing] A (Organism: Homo sapiens, class: Enzyme, accessions: P21397, gene: MAOA, swissprot: AOFA_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/5889715) Amine oxidase [flavin-containing] B (Organism: Homo sapiens, class: Enzyme, accessions: P27338, gene: MAOB, swissprot: AOFB_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/5889715) Mebanazine is a monoamine oxidase inhibitor. Mebanazine was previously used as an antidepressant, but later was withdrawn due to hepatotoxicity.
Click to view ceritinib ALK tyrosine kinase receptor (Organism: Homo sapiens, class: Kinase, accessions: Q9UM73, gene: ALK, swissprot: ALK_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf) Insulin-like growth factor 1 receptor (Organism: Homo sapiens, class: Kinase, accessions: P08069, gene: IGF1R, swissprot: IGF1R_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf) Proto-oncogene tyrosine-protein kinase ROS (Organism: Homo sapiens, class: Kinase, accessions: P08922, gene: ROS1, swissprot: ROS1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf) Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23742252) Tyrosine-protein kinase ABL1 (Organism: Homo sapiens, class: Kinase, accessions: P00519, gene: ABL1, swissprot: ABL1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23742252) Cyclin-dependent kinase 2 (Organism: Homo sapiens, class: Kinase, accessions: P24941, gene: CDK2, swissprot: CDK2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23742252) Cyclin-dependent kinase 4 (Organism: Homo sapiens, class: Kinase, accessions: P11802, gene: CDK4, swissprot: CDK4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23742252) Tyrosine-protein kinase BTK (Organism: Homo sapiens, class: Kinase, accessions: Q06187, gene: BTK, swissprot: BTK_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23742252) Epidermal growth factor receptor (Organism: Homo sapiens, class: Kinase, accessions: P00533, gene: EGFR, swissprot: EGFR_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23742252) Fibroblast growth factor receptor 3 (Organism: Homo sapiens, class: Kinase, accessions: P22607, gene: FGFR3, swissprot: FGFR3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23742252) Fibroblast growth factor receptor 4 (Organism: Homo sapiens, class: Kinase, accessions: P22455, gene: FGFR4, swissprot: FGFR4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23742252) Fibroblast growth factor receptor 2 (Organism: Homo sapiens, class: Kinase, accessions: P21802, gene: FGFR2, swissprot: FGFR2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23742252) Receptor-type tyrosine-protein kinase FLT3 (Organism: Homo sapiens, class: Kinase, accessions: P36888, gene: FLT3, swissprot: FLT3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23742252) Tyrosine-protein kinase JAK2 (Organism: Homo sapiens, class: Kinase, accessions: O60674, gene: JAK2, swissprot: JAK2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23742252) Tyrosine-protein kinase JAK1 (Organism: Homo sapiens, class: Kinase, accessions: P23458, gene: JAK1, swissprot: JAK1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23742252) Mast/stem cell growth factor receptor Kit (Organism: Homo sapiens, class: Kinase, accessions: P10721, gene: KIT, swissprot: KIT_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23742252) Hepatocyte growth factor receptor (Organism: Homo sapiens, class: Kinase, accessions: P08581, gene: MET, swissprot: MET_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23742252) Tyrosine-protein kinase Lyn (Organism: Homo sapiens, class: Kinase, accessions: P07948, gene: LYN, swissprot: LYN_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23742252) Tyrosine-protein kinase Lck (Organism: Homo sapiens, class: Kinase, accessions: P06239, gene: LCK, swissprot: LCK_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23742252) MAP kinase-interacting serine/threonine-protein kinase 2 (Organism: Homo sapiens, class: Kinase, accessions: Q9HBH9, gene: MKNK2, swissprot: MKNK2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23742252) Platelet-derived growth factor receptor alpha (Organism: Homo sapiens, class: Kinase, accessions: P16234, gene: PDGFRA, swissprot: PGFRA_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23742252) Proto-oncogene tyrosine-protein kinase receptor Ret (Organism: Homo sapiens, class: Kinase, accessions: P07949, gene: RET, swissprot: RET_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23742252) Tyrosine-protein kinase SYK (Organism: Homo sapiens, class: Kinase, accessions: P43405, gene: SYK, swissprot: KSYK_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23742252) Rho-associated protein kinase 2 (Organism: Homo sapiens, class: Kinase, accessions: O75116, gene: ROCK2, swissprot: ROCK2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23742252) Testis-specific serine/threonine-protein kinase 1 (Organism: Homo sapiens, class: Kinase, accessions: Q9BXA7, gene: TSSK1B, swissprot: TSSK1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23742252) Tyrosine-protein kinase ZAP-70 (Organism: Homo sapiens, class: Kinase, accessions: P43403, gene: ZAP70, swissprot: ZAP70_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23742252) Insulin receptor (Organism: Homo sapiens, class: Kinase, accessions: P06213, gene: INSR, swissprot: INSR_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/23742252) Ceritinib is a kinase inhibitor. Targets of ceritinib inhibition identified in either biochemical or cellular assays at clinically relevant concentrations include ALK, insulin-like growth factor 1 receptor (IGF-1R), insulin receptor (InsR), and ROS1. Among these, ceritinib is most active against ALK. Ceritinib inhibited autophosphorylation of ALK, ALK-mediated phosphorylation of the downstream signaling protein STAT3, and proliferation of ALK-dependent cancer cells in in vitro and in vivo assays. Ceritinib is used for the treatment of ALK-positive metastatic non-small cell lung cancer. antineoplastic agent (Code: CHEBI:35610) Kinase Inhibitor (Code: N0000175605) Tyrosine Kinase Inhibitors (Code: N0000020001) Cytochrome P450 3A Inhibitors (Code: N0000190114) Cytochrome P450 2C9 Inhibitors (Code: N0000185504) Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Protein Kinase Inhibitors (Code: D047428) 2014-04-29 FDA 4MK
Click to view umifenovir Umifenovir is a small indole-derivative molecule, used for prophylaxis and treatment of influenza and other respiratory viral infections. Umifenovir is known to inhibit haemagglutinin-mediated membrane fusion events in influenza A and B virus replication. 1988-03-23 Ministry of Health of the Russian Federation 75U
Click to view furazidin Furazidine is a nitrofuran derivative, acting as an antibacterial medicine with bacteriostatic action. It is active against both gram-positive (Staphylococcus epidermidis, Staphylococcus aureus, Staphylococcus faecalis) and gram-negative microorganisms (Enterobacteriaceae – Salmonella, Shygella, Proteus, Klebsiella, Escherichia, Enterobacter, etc.). It is used for the treatment of urinary tract, skin and soft tissues infections. antibacterial drug (Code: CHEBI:36047) antiinfective agent (Code: CHEBI:35441) Anti-Infective Agents (Code: D000890) Anti-Infective Agents, Urinary (Code: D000892) Renal Agents (Code: D012076) 2007-08-07 Ministry of Health of the Russian Federation
Click to view naloxegol Mu-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P35372, gene: OPRM1, swissprot: OPRM_HUMAN) antagonist (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2014/204760s000lbl.pdf) Naloxegol is a peripherally acting opioid receptor antagonist specific for mu-opioid receptors. Naloxegol is used for the treatment of chronic noncancer pain. Opioid Antagonist (Code: N0000175691) Opioid Antagonists (Code: N0000000154) Central Nervous System Agents (Code: D002491) Narcotic Antagonists (Code: D009292) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 2014-09-16 FDA
Click to view gemigliptin Dipeptidyl peptidase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P27487, gene: DPP4, swissprot: DPP4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/27298192) Dipeptidyl peptidase 9 (Organism: Homo sapiens, class: Enzyme, accessions: Q86TI2, gene: DPP9, swissprot: DPP9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/27298192) Dipeptidyl peptidase 8 (Organism: Homo sapiens, class: Enzyme, accessions: Q6V1X1, gene: DPP8, swissprot: DPP8_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/27298192) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/24304170) Gemigliptin, a novel dipeptidyl peptidase (DPP)-4 inhibitor, is approved for use as a monotherapy or in combination therapy to treat hyperglycemia in patients with type 2 diabetes mellitus. 2012-06-27 Korean Food and Drug Administration (KFDA)
Click to view eliglustat Ceramide glucosyltransferase (Organism: Homo sapiens, class: Enzyme, accessions: Q16739, gene: UGCG, swissprot: CEGT_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/205494s003lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/205494s003lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/205494s003lbl.pdf) Eliglustat tartrate is a small molecule inhibitor of glucosylceramide synthase that resembles the ceramide substrate for the enzyme. Gaucher disease is caused by a deficiency of the lysosomal enzyme acid beta-glucosidase. Acid beta-glucosidase catalyzes the conversion of the sphingolipid glucocerebroside into glucose and ceramide. The enzymatic deficiency causes an accumulation of glucosylceramide (GL-1) primarily in the lysosomal compartment of macrophages, giving rise to foam cells or "Gaucher cells". Glucosylceramide Synthase Inhibitor (Code: N0000175783) Glucosylceramide Synthase Inhibitors (Code: N0000020019) P-Glycoprotein Inhibitors (Code: N0000185503) Cytochrome P450 2D6 Inhibitors (Code: N0000182137) Enzyme Inhibitors (Code: D004791) 2014-08-19 FDA
Click to view ethacizine Ethacizine is an antiarrhythmic. It is used for the treatment of severe or refractory ventricular and supraventricular arrhythmias, refractory tachycardia associated with Wolff–Parkinson–White (WPW) syndrome. Anti-Arrhythmia Agents (Code: D000889) Cardiovascular Agents (Code: D002317) Central Nervous System Agents (Code: D002491) Psychotropic Drugs (Code: D011619) 1984-06-14 Ministry of Health of the Russian Federation
Click to view octisalate Octisalate is an organic compound used as an ingredient in sunscreens and cosmetics to absorb UVB (ultraviolet) rays from the sun. FDA
Click to view omarigliptin Dipeptidyl peptidase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P27487, gene: DPP4, swissprot: DPP4_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/24660890) Dipeptidyl peptidase 4 (Organism: Mus musculus, class: Enzyme, accessions: P28843, gene: Dpp4, swissprot: DPP4_MOUSE Omarigliptin is a dipeptidyl peptidase-4 (DPP-4) inhibitor used for the treatment of type 2 diabetes. It potently but reversibly inhibits DPP-4 enzyme, which prolongs the circulating half-life of glucagon-like peptide-1 that increases insulin secretion in a glucose-dependent manner. 2015-09-28 PMDA
Click to view apremilast cAMP-specific 3',5'-cyclic phosphodiesterase 4D (Organism: Homo sapiens, class: Enzyme, accessions: Q08499, gene: PDE4D, swissprot: PDE4D_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/205437Orig1s007lbl.pdf) cAMP-specific 3',5'-cyclic phosphodiesterase 4A (Organism: Homo sapiens, class: Enzyme, accessions: P27815, gene: PDE4A, swissprot: PDE4A_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/205437Orig1s007lbl.pdf) cAMP-specific 3',5'-cyclic phosphodiesterase 4C (Organism: Homo sapiens, class: Enzyme, accessions: Q08493, gene: PDE4C, swissprot: PDE4C_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/205437Orig1s007lbl.pdf) cAMP-specific 3',5'-cyclic phosphodiesterase 4B (Organism: Homo sapiens, class: Enzyme, accessions: Q07343, gene: PDE4B, swissprot: PDE4B_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/205437Orig1s007lbl.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/205437Orig1s007lbl.pdf) Cytochrome P450 2A6 (Organism: Homo sapiens, class: Enzyme, accessions: P11509, gene: CYP2A6, swissprot: CP2A6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/205437Orig1s007lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/205437Orig1s007lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/205437Orig1s007lbl.pdf) Apremilast is an oral small-molecule inhibitor of phosphodiesterase 4 (PDE4) specific for cyclic adenosine monophosphate (cAMP). PDE4 inhibition results in increased intracellular cAMP levels. The specific mechanism(s) by which apremilast exerts its therapeutic action in psoriatic arthritis patients and psoriasis patients is not well defined. non-steroidal anti-inflammatory drug (Code: CHEBI:35475) Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 2014-03-21 FDA
Click to view empagliflozin Sodium/glucose cotransporter 2 (Organism: Homo sapiens, class: Transporter, accessions: P31639, gene: SLC5A2, swissprot: SC5A2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204629s019lbl.pdf) UDP-glucuronosyltransferase 1-3 (Organism: Homo sapiens, class: Enzyme, accessions: P35503, gene: UGT1A3, swissprot: UD13_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204629s019lbl.pdf) UDP-glucuronosyltransferase 1-9 (Organism: Homo sapiens, class: Enzyme, accessions: O60656, gene: UGT1A9, swissprot: UD19_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204629s019lbl.pdf) UDP-glucuronosyltransferase 1-8 (Organism: Homo sapiens, class: Enzyme, accessions: Q9HAW9, gene: UGT1A8, swissprot: UD18_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204629s019lbl.pdf) UDP-glucuronosyltransferase 2B7 (Organism: Homo sapiens, class: Enzyme, accessions: P16662, gene: UGT2B7, swissprot: UD2B7_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204629s019lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204629s019lbl.pdf) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204629s019lbl.pdf) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204629s019lbl.pdf) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204629s019lbl.pdf) Solute carrier family 22 member 8 (Organism: Homo sapiens, class: Transporter, accessions: Q8TCC7, gene: SLC22A8, swissprot: S22A8_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204629s019lbl.pdf) Empagliflozin is a C-glycosyl compound and a sodium-glucose co-transporter 2 inhibitor used as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. By inhibiting SGLT2, empagliflozin reduces renal reabsorption of filtered glucose and lowers the renal threshold for glucose, and thereby increases urinary glucose excretion. Empagliflozin is indicated as an adjunct to diet and exercise to improve glycemic control with type 2 diabetes mellitus and to reduce the risk of cardiovascular death in adult patients with type 2 diabetes mellitus and established cardiovascular disease. hypoglycemic agent (Code: CHEBI:35526) Sodium-Glucose Cotransporter 2 Inhibitor (Code: N0000187059) Sodium-Glucose Transporter 2 Inhibitors (Code: N0000187058) Hypoglycemic Agents (Code: D007004) 2014-05-22 EMA
Click to view aripiprazole lauroxil Aripiprazole lauroxil is a prodrug of aripiprazole, following intramuscular injection is converted by enzyme-mediated hydrolysis to N-hydroxymethyl aripiprazole which is then hydrolyzed to aripiprazole. (See: aripiprazole) H1-receptor antagonist (Code: CHEBI:37955) second generation antipsychotic (Code: CHEBI:65191) serotonergic agonist (Code: CHEBI:35941) prodrug (Code: CHEBI:50266) Antipsychotic Agents (Code: D014150) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149) 2015-10-05 FDA
Click to view amino(diphenylhydantoin) valeric acid Amino(diphenylhydantoin) valeric acid is a hydantoin derivative. It was used for the treatment of epilepsy.
Click to view meprotixol Meprotixol is a derivative of the thiazanthene group. Meprotixol has a antitussive effect. Meprotixol showed an antitussive effect equal to that of codeine phosphate.
Click to view vintafolide Vintafolide is a water-soluble derivative of folic acid and the vinca alkaloid desacetylvinblastine hydrazide. Vintafolide is targeting the folate receptor, which is overexpressed on certain cancers, such as ovarian cancer. In 2014 manufactures stopped a late-stage study of vintafolide in treating ovarian cancer on the recommendation of a data safety monitoring board, saying that the drug failed to improve progression-free survival.
Click to view etilefrine pivalate Beta-1 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08588, gene: ADRB1, swissprot: ADRB1_HUMAN) agonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/4396765) Etilefrine pivalate is a prodrug of etilefrine, an adrenergic agonist with vasoconstrictive activity. Etilefrine pivalate is hydrolyzed to etilefrine, which binds to and activates alpha-1-adrenergic receptors of the arteriolar and venous vasculature. (See: etilefrine)
Click to view laquinimod Laquinimod is an immunomodulator for oral treatment for multiple sclerosis. 2013-07-05 Ministry of Health of the Russian Federation
Click to view iodohippurate sodium I125 Iodohippurate sodium I125 is an isotopically modified compound, an organic sodium salt and a sodium 2-iodohippurate. It derives from a N-benzoylglycine. It is used as a radiopharmaceutical. It is used for the measurement of effective renal plasma flow in subjects with renal failure. radiopharmaceutical (Code: CHEBI:35232)
Click to view luliconazole Lanosterol 14-alpha demethylase (Organism: Candida albicans (strain SC5314 / ATCC MYA-2876), class: Enzyme, accessions: P10613, gene: ERG11, swissprot: CP51_CANAL) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10520160) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204153s004s005lbl.pdf) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204153s004s005lbl.pdf) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204153s004s005lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204153s004s005lbl.pdf) Luliconazole is an antifungal that belongs to the azole class. Luliconazole appears to inhibit ergosterol synthesis by inhibiting the enzyme lanosterol demethylase, inhibition of this enzyme's activity by azoles results in decreased amounts of ergosterol, a constituent of fungal cell membranes, and a corresponding accumulation of lanosterol. Luliconazole is indicated for the topical treatment of interdigital tinea pedis, tinea cruris, and tinea corporis caused by the organisms Trichophyton rubrum and Epidermophyton floccosum. Azole Antifungal (Code: N0000175487) Azoles (Code: N0000008217) Cytochrome P450 2C19 Inhibitors (Code: N0000182140) 2013-11-14 FDA
Click to view iodohippurate sodium I131 Iodohippurate sodium I131 is a diagnostic aid in determining renal function, renal blood flow, ar urinary tract obstruction, and a renal imaging agent. radiopharmaceutical (Code: CHEBI:35232) 1968-05-24 FDA
Click to view laninamivir octanoate hydrate Neuraminidase (Organism: Influenza A virus (A/RI/5+/1957(H2N2)), class: Enzyme, accessions: Q194T1, gene: None, swissprot: Q194T1_9INFA Neuraminidase (Organism: Influenza A virus (A/WSN/1933(H1N1)), class: Enzyme, accessions: B4URF0, gene: NA, swissprot: B4URF0_9INFA Laninamivir octanoate hydrate is a prodrug of a new neuraminidase inhibitor, laninamivir. Laninamivir octanoate hydrate is used for the treatment and prevention of influenza. 2010-07-29 PMDA LVO
Click to view peramivir Neuraminidase (Organism: Influenza A virus (strain A/Puerto Rico/8/1934 H1N1), class: Enzyme, accessions: P03468, gene: NA, swissprot: NRAM_I34A1) inhibitor (Source: ) Neuraminidase (Organism: Influenza B virus (strain B/Lee/1940), class: Enzyme, accessions: P03474, gene: NA, swissprot: NRAM_INBLE) inhibitor (Source: ) Neuraminidase (Organism: Influenza A virus (strain A/Breig Mission/1/1918 H1N1), class: Enzyme, accessions: Q9IGQ6, gene: NA, swissprot: NRAM_I18A0) inhibitor (Source: ) Neuraminidase (Organism: Influenza A virus (A/WSN/1933(H1N1)), class: Enzyme, accessions: B4URF0, gene: NA, swissprot: B4URF0_9INFA) Peramivir is an inhibitor of influenza virus neuraminidase, an enzyme that releases viral particles from the plasma membrane of infected cells. EC 3.2.1.18 (exo-alpha-sialidase) inhibitor (Code: CHEBI:52425) antiviral drug (Code: CHEBI:36044) Neuraminidase Inhibitor (Code: N0000175524) Neuraminidase Inhibitors (Code: N0000175436) Anti-Infective Agents (Code: D000890) Antiviral Agents (Code: D000998) Enzyme Inhibitors (Code: D004791) 2014-12-19 FDA BCZ
Click to view florbetaben F18 Amyloid beta A4 protein (Organism: Homo sapiens, class: Unclassified, accessions: P05067, gene: APP, swissprot: A4_HUMAN Florbetaben F18 is a F18-labeled stilbene derivative, which binds to beta-amyloid plaques in the brain. The F 18 isotope produces a positron signal that is detected by a PET scanner. Radioactive Diagnostic Agent (Code: N0000177914) Positron Emitting Activity (Code: N0000175869) 2014-03-19 FDA
Click to view delamanid Delamanid is a nitro-dihydro-imidazooxazoles derivative. The pharmacological mode of action of delamanid involves inhibition of the synthesis of the mycobacterial cell wall components, methoxy-mycolic and keto-mycolic acid. The identified metabolites of delamanid do not show anti-mycobacterial activity. Delamanid is indicated for use as part of an appropriate combination regimen for pulmonary multi-drug resistant tuberculosis (MDR-TB) in adult patients when an effective treatment regimen cannot otherwise be composed for reasons of resistance or tolerability. 2014-04-28 EMA
Click to view nordefrin Nordefrin is a structural isomer of epinephrine and has a primary amine group. Corbadrine (Levonordefrin) is a L-isomer of nordefrin and used as a vasoconstrictor in local anesthetic solutions. It has pharmacologic activity similar to that of epinephrine but it is more stable than epinephrine. Levonordefrin is used as a nasal decongestant and vasoconstrictor, most often in dentistry. Cardiovascular Agents (Code: D002317) Vasoconstrictor Agents (Code: D014662) 1960-01-06 FDA
Click to view tasimelteon Melatonin receptor type 1A (Organism: Homo sapiens, class: GPCR, accessions: P48039, gene: MTNR1A, swissprot: MTR1A_HUMAN) agonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/22640220) Melatonin receptor type 1B (Organism: Homo sapiens, class: GPCR, accessions: P49286, gene: MTNR1B, swissprot: MTR1B_HUMAN) agonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/22640220) an agonist at melatonin MT1 and MT2 receptors, these receptors are thought to be involved in the control of circadian rhythms Melatonin Receptor Agonist (Code: N0000175743) Melatonin Receptor Agonists (Code: N0000000250) 2014-01-31 FDA
Click to view rifamycin DNA-directed RNA polymerase subunit beta (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P0A8V2, gene: rpoB, swissprot: RPOB_ECOLI) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210910s000lbl.pdf) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16595711) Bile salt export pump (Organism: Rattus norvegicus, class: Unclassified, accessions: O70127, gene: Abcb11, swissprot: ABCBB_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10648470) Bile salt export pump (Organism: Homo sapiens, class: Transporter, accessions: O95342, gene: ABCB11, swissprot: ABCBB_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12404239) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12085361) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12085361) Solute carrier organic anion transporter family member 2B1 (Organism: Homo sapiens, class: Transporter, accessions: O94956, gene: SLCO2B1, swissprot: SO2B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12085361) Solute carrier organic anion transporter family member 1A2 (Organism: Homo sapiens, class: Transporter, accessions: P46721, gene: SLCO1A2, swissprot: SO1A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12085361) Solute carrier organic anion transporter family member 1A4 (Organism: Rattus norvegicus, class: Transporter, accessions: O35913, gene: Slco1a4, swissprot: SO1A4_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12085361) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210910s000lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210910s000lbl.pdf) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210910s000lbl.pdf) Multidrug and toxin extrusion protein 1 (Organism: Homo sapiens, class: Transporter, accessions: Q96FL8, gene: SLC47A1, swissprot: S47A1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210910s000lbl.pdf) Multidrug and toxin extrusion protein 2 (Organism: Homo sapiens, class: Transporter, accessions: Q86VL8, gene: SLC47A2, swissprot: S47A2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210910s000lbl.pdf) Solute carrier family 22 member 8 (Organism: Homo sapiens, class: Transporter, accessions: Q8TCC7, gene: SLC22A8, swissprot: S22A8_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210910s000lbl.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210910s000lbl.pdf) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210910s000lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210910s000lbl.pdf) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210910s000lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210910s000lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210910s000lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210910s000lbl.pdf) Cytochrome P450 3A5 (Organism: Homo sapiens, class: Enzyme, accessions: P20815, gene: CYP3A5, swissprot: CP3A5_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210910s000lbl.pdf) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) inducer (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210910s000lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inducer (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210910s000lbl.pdf) Rifamycin SV is a derivative of antibiotic rifamycin B (the natural fermentation product of S. mediterranei broths). Rifamycin is a commonly used antimycobacterial drug that inhibits prokaryotic DNA-dependent RNA synthesis and protein synthesis; it blocks RNA-polymerase transcription initiation. Rifamycin has an activity spectrum against Gram-positive and Gram-negative bacteria, but is mainly used for the treatment of travelers’ diarrhea caused by noninvasive strains of Escherichia coli. antitubercular agent (Code: CHEBI:33231) Antirheumatic Agents (Code: D018501) 1988-10-03 Swissmedic (Switzerland)
Click to view olodaterol Beta-2 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P07550, gene: ADRB2, swissprot: ADRB2_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/203108s008lbl.pdf) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/203108s008lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/203108s008lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/203108s008lbl.pdf) UDP-glucuronosyltransferase 1-1 (Organism: Homo sapiens, class: Enzyme, accessions: P22309, gene: UGT1A1, swissprot: UD11_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/203108s008lbl.pdf) UDP-glucuronosyltransferase 1-7 (Organism: Homo sapiens, class: Enzyme, accessions: Q9HAW7, gene: UGT1A7, swissprot: UD17_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/203108s008lbl.pdf) UDP-glucuronosyltransferase 2B7 (Organism: Homo sapiens, class: Enzyme, accessions: P16662, gene: UGT2B7, swissprot: UD2B7_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/203108s008lbl.pdf) UDP-glucuronosyltransferase 1-9 (Organism: Homo sapiens, class: Enzyme, accessions: O60656, gene: UGT1A9, swissprot: UD19_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/203108s008lbl.pdf) Olodaterol is a long-acting beta2-adrenergic agonist. The compound exerts its pharmacological effects by binding and activation of beta2-adrenoceptors after topical administration by inhalation. Olodaterol is indicated for the long-term, once-daily maintenance bronchodilator treatment of airflow obstruction in patients with chronic obstructive pulmonary disease, including chronic bronchitis and emphysema. beta-adrenergic agonist (Code: CHEBI:35522) bronchodilator agent (Code: CHEBI:35523) beta2-Adrenergic Agonist (Code: N0000175779) Adrenergic beta2-Agonists (Code: N0000009922) Anti-Asthmatic Agents (Code: D018927) Autonomic Agents (Code: D001337) Bronchodilator Agents (Code: D001993) Peripheral Nervous System Agents (Code: D018373) Respiratory System Agents (Code: D019141) 2014-07-31 FDA
Click to view umeclidinium Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/205382s010lbl.pdf) Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/205382s010lbl.pdf) Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/205382s010lbl.pdf) Muscarinic acetylcholine receptor M4 (Organism: Homo sapiens, class: GPCR, accessions: P08173, gene: CHRM4, swissprot: ACM4_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/205382s010lbl.pdf) Muscarinic acetylcholine receptor M5 (Organism: Homo sapiens, class: GPCR, accessions: P08912, gene: CHRM5, swissprot: ACM5_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/205382s010lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/205382s010lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/205382s010lbl.pdf) Umeclidinium is a long-acting muscarinic antagonist. It has similar affinity to the subtypes of muscarinic receptors M1 to M5. In the airways, it exhibits pharmacological effects through inhibition of M3 receptors at the smooth muscle leading to bronchodilation. Umeclidinium is indicated for the long-term maintenance treatment of airflow obstruction in patients with chronic obstructive pulmonary disease. muscarinic antagonist (Code: CHEBI:48876) Anticholinergic (Code: N0000175574) Cholinergic Antagonists (Code: N0000175370) 2013-12-18 FDA
Click to view vortioxetine 5-hydroxytryptamine receptor 3A (Organism: Homo sapiens, class: Ion channel, accessions: P46098, gene: HTR3A, swissprot: 5HT3A_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/204447s018lbl.pdf) 5-hydroxytryptamine receptor 7 (Organism: Homo sapiens, class: GPCR, accessions: P34969, gene: HTR7, swissprot: 5HT7R_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/204447s018lbl.pdf) 5-hydroxytryptamine receptor 1D (Organism: Homo sapiens, class: GPCR, accessions: P28221, gene: HTR1D, swissprot: 5HT1D_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/204447s018lbl.pdf) 5-hydroxytryptamine receptor 1B (Organism: Homo sapiens, class: GPCR, accessions: P28222, gene: HTR1B, swissprot: 5HT1B_HUMAN) partial agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/204447s018lbl.pdf) 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/204447s018lbl.pdf) Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/204447s018lbl.pdf) Cytochrome P450 2A6 (Organism: Homo sapiens, class: Enzyme, accessions: P11509, gene: CYP2A6, swissprot: CP2A6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/204447s018lbl.pdf) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/204447s018lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/204447s018lbl.pdf) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/204447s018lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/204447s018lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/204447s018lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/204447s018lbl.pdf) Cytochrome P450 3A5 (Organism: Homo sapiens, class: Enzyme, accessions: P20815, gene: CYP3A5, swissprot: CP3A5_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/204447s018lbl.pdf) Vortioxetine is an antidepressant. The mechanism of the antidepressant effect of vortioxetine is not fully understood, but is thought to be related to its enhancement of serotonergic activity in the CNS through inhibition of the reuptake of serotonin. It also has several other activities including 5-HT3 receptor antagonism and 5-HT1A receptor agonism. The contribution of these activities to vortioxetine’s antidepressant effect has not been established. Vortioxetine binds with high affinity to the human serotonin transporter, but not to the norepinephrine or dopamine transporters. Vortioxetine potently and selectively inhibits reuptake of serotonin. Vortioxetine binds to 5-HT3, 5-HT1A, 5-HT7, 5-HT1D, and 5-HT1B, receptors and is a 5-HT3, 5-HT1D, and 5-HT7 receptor antagonist, 5-HT1B receptor partial agonist, and 5-HT1A receptor agonist. Vortioxetine is indicated for the treatment of major depressive disorder. antidepressant (Code: CHEBI:35469) anxiolytic drug (Code: CHEBI:35474) serotonergic agonist (Code: CHEBI:35941) serotonergic antagonist (Code: CHEBI:48279) Anti-Anxiety Agents (Code: D014151) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Membrane Transport Modulators (Code: D049990) Neurotransmitter Agents (Code: D018377) Neurotransmitter Uptake Inhibitors (Code: D014179) Psychotropic Drugs (Code: D011619) Serotonin 5-HT1 Receptor Agonists (Code: D058825) Serotonin 5-HT1 Receptor Antagonists (Code: D058829) Serotonin 5-HT3 Receptor Antagonists (Code: D058831) Serotonin Agents (Code: D018490) Serotonin Antagonists (Code: D012702) Serotonin Receptor Agonists (Code: D017366) Serotonin Uptake Inhibitors (Code: D017367) Tranquilizing Agents (Code: D014149) 2013-09-30 FDA
Click to view riociguat Guanylate cyclase soluble subunit beta-1 (Organism: Homo sapiens, class: Enzyme, accessions: Q02153, gene: GUCY1B3, swissprot: GCYB1_HUMAN) positive allosteric modulator (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204819s011lbl.pdf) Cytochrome P450 1A1 (Organism: Homo sapiens, class: Enzyme, accessions: P04798, gene: CYP1A1, swissprot: CP1A1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204819s011lbl.pdf) Cytochrome P450 2J2 (Organism: Homo sapiens, class: Enzyme, accessions: P51589, gene: CYP2J2, swissprot: CP2J2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204819s011lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204819s011lbl.pdf) Cytochrome P450 3A5 (Organism: Homo sapiens, class: Enzyme, accessions: P20815, gene: CYP3A5, swissprot: CP3A5_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204819s011lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204819s011lbl.pdf) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204819s011lbl.pdf) Riociguat is a stimulator of guanylate cyclase which causes relaxation of vascular smooth muscle and is used to treat severe pulmonary arterial hypertension. antihypertensive agent (Code: CHEBI:35674) Guanylate Cyclase Stimulators (Code: N0000190484) Soluble Guanylate Cyclase Stimulator (Code: N0000190485) Enzyme Activators (Code: D020536) 2013-10-08 FDA
Click to view sofosbuvir Lysosomal protective protein (Organism: Homo sapiens, class: Enzyme, accessions: P10619, gene: CTSA, swissprot: PPGB_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212480s000lbl.pdf) Liver carboxylesterase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P23141, gene: CES1, swissprot: EST1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212480s000lbl.pdf) Histidine triad nucleotide-binding protein 1 (Organism: Homo sapiens, class: Enzyme, accessions: P49773, gene: HINT1, swissprot: HINT1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212480s000lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212480s000lbl.pdf) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212480s000lbl.pdf) Sofosbuvir is an inhibitor of the HCV NS5B RNA-dependent RNA polymerase, which is essential for viral replication. Sofosbuvir is a nucleotide prodrug that undergoes intracellular metabolism to form the pharmacologically active uridine analog triphosphate (GS-461203), which can be incorporated into HCV RNA by the NS5B polymerase and acts as a chain terminator. Sofosbuvir is indicated for the treatment of adult and pediatric patients with genotype 1, 2, 3 or 4 chronic HCV infection without cirrhosis or with compensated cirrhosis. prodrug (Code: CHEBI:50266) antiviral drug (Code: CHEBI:36044) Hepatitis C Virus Nucleotide Analog NS5B Polymerase Inhibitor (Code: N0000191493) RNA Replicase Inhibitors (Code: N0000191258) Nucleoside Analog (Code: N0000175459) Anti-Infective Agents (Code: D000890) Antiviral Agents (Code: D000998) 2013-12-06 FDA
Click to view simeprevir Genome polyprotein (Organism: Hepatitis C virus genotype 1a (isolate H), class: Polyprotein, accessions: P27958, gene: None, swissprot: POLG_HCVH) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/205123s014lbl.pdf) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/205123s014lbl.pdf) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/205123s014lbl.pdf) Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/205123s014lbl.pdf) Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/205123s014lbl.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/205123s014lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/205123s014lbl.pdf) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/205123s014lbl.pdf) Solute carrier organic anion transporter family member 2B1 (Organism: Homo sapiens, class: Transporter, accessions: O94956, gene: SLCO2B1, swissprot: SO2B1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/205123s014lbl.pdf) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/205123s014lbl.pdf) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/205123s014lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/205123s014lbl.pdf) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/205123s014lbl.pdf) Canalicular multispecific organic anion transporter 1 (Organism: Homo sapiens, class: Transporter, accessions: Q92887, gene: ABCC2, swissprot: MRP2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/205123s014lbl.pdf) Bile salt export pump (Organism: Homo sapiens, class: Transporter, accessions: O95342, gene: ABCB11, swissprot: ABCBB_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/205123s014lbl.pdf) Ileal sodium/bile acid cotransporter (Organism: Homo sapiens, class: Transporter, accessions: Q12908, gene: SLC10A2, swissprot: NTCP2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/205123s014lbl.pdf) Simeprevir is an inhibitor of the HCV NS3/4A protease which is essential for viral replication. It is used in the treatment of chronic hepatitis C genotype 1 infection in adults with compensated liver disease, including cirrhosis. Hepatitis C Virus NS3/4A Protease Inhibitor (Code: N0000182639) HCV NS3/4A Protease Inhibitors (Code: N0000182638) Cytochrome P450 3A4 Inhibitors (Code: N0000182141) P-Glycoprotein Inhibitors (Code: N0000185503) Organic Anion Transporting Polypeptide 1B1 Inhibitors (Code: N0000190107) Organic Anion Transporting Polypeptide 1B3 Inhibitors (Code: N0000190108) Anti-Infective Agents (Code: D000890) Antiviral Agents (Code: D000998) Enzyme Inhibitors (Code: D004791) Protease Inhibitors (Code: D011480) 2013-11-22 FDA 30B
Click to view ipidacrine Acetylcholinesterase (Organism: Homo sapiens, class: Enzyme, accessions: P22303, gene: ACHE, swissprot: ACES_HUMAN) inhibitor (Source: https://onlinelibrary.wiley.com/doi/abs/10.1111/j.1527-3458.1998.tb00067.x) Ipidacrine is a nonselective inhibitor of acetylcholinesterase and butyrilcholinesterase. Ipidacrine has a direct stimulating effect on the conduct of the pulse along the nerve fibers, interneuronal and neuromuscular synapses of the CNS and peripheral nervous system. 1988-07-15 Ministry of Health of the Russian Federation
Click to view macitentan Endothelin-1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P25101, gene: EDNRA, swissprot: EDNRA_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/204410s017lbl.pdf) Endothelin B receptor (Organism: Homo sapiens, class: GPCR, accessions: P24530, gene: EDNRB, swissprot: EDNRB_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/204410s017lbl.pdf) Macitentan is an endothelin receptor antagonist that is used in the therapy of pulmonary arterial hypertension. endothelin receptor antagonist (Code: CHEBI:51451) antihypertensive agent (Code: CHEBI:35674) orphan drug (Code: CHEBI:71031) Endothelin A Receptor Antagonists (Code: D065130) Endothelin B Receptor Antagonists (Code: D065131) Endothelin Receptor Antagonists (Code: D065128) 2013-10-18 FDA
Click to view ibrutinib Tyrosine-protein kinase BTK (Organism: Homo sapiens, class: Kinase, accessions: Q06187, gene: BTK, swissprot: BTK_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/17154430) Tyrosine-protein kinase Blk (Organism: Homo sapiens, class: Kinase, accessions: P51451, gene: BLK, swissprot: BLK_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/26641137) Tyrosine-protein kinase Fgr (Organism: Homo sapiens, class: Kinase, accessions: P09769, gene: FGR, swissprot: FGR_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/26641137) Tyrosine-protein kinase Fyn (Organism: Homo sapiens, class: Kinase, accessions: P06241, gene: FYN, swissprot: FYN_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/26641137) Tyrosine-protein kinase HCK (Organism: Homo sapiens, class: Kinase, accessions: P08631, gene: HCK, swissprot: HCK_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/26641137) Tyrosine-protein kinase Lck (Organism: Homo sapiens, class: Kinase, accessions: P06239, gene: LCK, swissprot: LCK_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/26641137) Proto-oncogene tyrosine-protein kinase Src (Organism: Homo sapiens, class: Kinase, accessions: P12931, gene: SRC, swissprot: SRC_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/26641137) Tyrosine-protein kinase Yes (Organism: Homo sapiens, class: Kinase, accessions: P07947, gene: YES1, swissprot: YES_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/26641137) Tyrosine-protein kinase ITK/TSK (Organism: Homo sapiens, class: Kinase, accessions: Q08881, gene: ITK, swissprot: ITK_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/26641137) Tyrosine-protein kinase Tec (Organism: Homo sapiens, class: Kinase, accessions: P42680, gene: TEC, swissprot: TEC_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/26641137) Tyrosine-protein kinase TXK (Organism: Homo sapiens, class: Kinase, accessions: P42681, gene: TXK, swissprot: TXK_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/26641137) Receptor tyrosine-protein kinase erbB-2 (Organism: Homo sapiens, class: Kinase, accessions: P04626, gene: ERBB2, swissprot: ERBB2_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/26641137) Receptor tyrosine-protein kinase erbB-4 (Organism: Homo sapiens, class: Kinase, accessions: Q15303, gene: ERBB4, swissprot: ERBB4_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/26641137) Tyrosine-protein kinase JAK3 (Organism: Homo sapiens, class: Kinase, accessions: P52333, gene: JAK3, swissprot: JAK3_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/26641137) Ibrutinib is a small-molecule inhibitor of BTK. Ibrutinib forms a covalent bond with a cysteine residue in the BTK active site, leading to inhibition of BTK enzymatic activity. BTK is a signaling molecule of the B-cell antigen receptor (BCR) and cytokine receptor pathways. BTK's role in signaling through the B-cell surface receptors results in activation of pathways necessary for B-cell trafficking, chemotaxis, and adhesion. Nonclinical studies show that ibrutinib inhibits malignant B-cell proliferation and survival in vivo as well as cell migration and substrate adhesion in vitro. antineoplastic agent (Code: CHEBI:35610) Kinase Inhibitor (Code: N0000175605) Protein Kinase Inhibitors (Code: N0000175076) 2013-11-13 FDA 1E8
Click to view dolutegravir Integrase (Organism: Human immunodeficiency virus 1, class: Enzyme, accessions: Q7ZJM1, gene: pol, swissprot: Q7ZJM1_9HIV1) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/210192s000lbl.pdf) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/210192s000lbl.pdf) Multidrug and toxin extrusion protein 1 (Organism: Homo sapiens, class: Transporter, accessions: Q96FL8, gene: SLC47A1, swissprot: S47A1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/210192s000lbl.pdf) Solute carrier family 22 member 6 (Organism: Homo sapiens, class: Transporter, accessions: Q4U2R8, gene: SLC22A6, swissprot: S22A6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/210192s000lbl.pdf) Dolutegravir inhibits HIV integrase by binding to the integrase active site and blocking the strand transfer step of retroviral deoxyribonucleic acid (DNA) integration which is essential for the HIV replication cycle. Human Immunodeficiency Virus Integrase Strand Transfer Inhibitor (Code: N0000175887) Multidrug and Toxin Extrusion Transporter 1 Inhibitors (Code: N0000191423) Organic Cation Transporter 2 Inhibitors (Code: N0000187061) Anti-HIV Agents (Code: D019380) Anti-Infective Agents (Code: D000890) Anti-Retroviral Agents (Code: D044966) Antiviral Agents (Code: D000998) Enzyme Inhibitors (Code: D004791) HIV Integrase Inhibitors (Code: D019428) 2013-08-12 FDA DLU
Click to view dimethyl fumarate Dimethyl fumarate is a fumarate derivative. The mechanism by which dimethyl fumarate (DMF) exerts its therapeutic effect in multiple sclerosis is unknown. DMF have been shown to activate the Nuclear factor (erythroid-derived 2)-like 2 (Nrf2) pathway in vitro and in vivo in animals and humans. The Nrf2 pathway is involved in the cellular response to oxidative stress. Dimethyl fumarate also appears to inhibit the nuclear factor-kappa B (NF-kB)-mediated pathway, modulates the production of certain cytokines and induces apoptosis in certain T-cell subsets. Its radiosensitizing activity is due to this agent's ability to bind to and sequester intracellular GSH, thereby depleting intracellular GSH and preventing its anti-oxidative effects. Dimethyl fumarate is indicated for the treatment of patients with relapsing forms of multiple sclerosis. immunomodulator (Code: CHEBI:50846) antipsoriatic (Code: CHEBI:50748) Dermatologic Agents (Code: D003879) Immunologic Factors (Code: D007155) Immunosuppressive Agents (Code: D007166) Radiation-Sensitizing Agents (Code: D011838) 2013-03-27 FDA
Click to view canagliflozin Sodium/glucose cotransporter 2 (Organism: Homo sapiens, class: Transporter, accessions: P31639, gene: SLC5A2, swissprot: SC5A2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/204353s000lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/204353s000lbl.pdf) A glucoside-derived sodium-glucose transporter 2 inhibitor that stimulates urinary excretion of glucose by suppressing renal glucose reabsorption. It is used to manage blood glucose levels in patients with type 2 diabetes. hypoglycemic agent (Code: CHEBI:35526) Sodium-Glucose Cotransporter 2 Inhibitor (Code: N0000187059) Sodium-Glucose Transporter 2 Inhibitors (Code: N0000187058) P-Glycoprotein Inhibitors (Code: N0000185503) Hypoglycemic Agents (Code: D007004) 2013-03-29 FDA
Click to view glycerol phenylbutyrate Glycerol phenylbutyrate is a nitrogen-binding agent. It is a triglyceride containing 3 molecules of phenylbutyrate linked to a glycerol backbone. Phenylacetate, the major metabolite of phenylbutyrate, is the active moiety of this drug. Phenylacetate conjugates with glutamine (which contains 2 molecules of nitrogen) via acetylation in the liver and kidneys to form phenylacetylglutamine, which is excreted by the kidneys. On a molar basis, phenylacetylglutamine, like urea, contains 2 moles of nitrogen and provides an alternate vehicle for waste nitrogen excretion. Glycerol phenylbutyrate is indicated for use as a nitrogen-binding agent for chronic management of patients with urea cycle disorders (UCDs) who cannot be managed by dietary protein restriction and/or amino acid supplementation alone. (See: phenylbutanoic acid) 2013-02-01 FDA
Click to view pomalidomide Protein cereblon (Organism: Homo sapiens, class: Cytosolic other, accessions: Q96SW2, gene: CRBN, swissprot: CRBN_HUMAN) modulator (Source: http://www.ncbi.nlm.nih.gov/pubmed/26131937) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204026s017lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204026s017lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204026s017lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204026s017lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204026s017lbl.pdf) Prostaglandin G/H synthase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P35354, gene: PTGS2, swissprot: PGH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17308870) Pomalidomide is an analogue of thalidomide with immunomodulatory, antiangiogenic, and antineoplastic properties. Cellular activities of pomalidomide are mediated through its target cereblon, a component of a cullin ring E3 ubiquitin ligase enzyme complex. In vitro, in the presence of drug, substrate proteins (including Aiolos and Ikaros) are targeted for ubiquitination and subsequent degradation leading to direct cytotoxic and immunomodulatory effects. In in vitro cellular assays, pomalidomide inhibited proliferation and induced apoptosis of hematopoietic tumor cells. Additionally, pomalidomide inhibited the proliferation of lenalidomideresistant multiple myeloma cell lines and synergized with dexamethasone in both lenalidomide-sensitive and lenalidomide-resistant cell lines to induce tumor cell apoptosis. Pomalidomide enhanced T cell- and natural killer (NK) cell-mediated immunity and inhibited production of pro-inflammatory cytokines (e.g., TNF-? and IL-6) by monocytes. angiogenesis inhibitor (Code: CHEBI:48422) antineoplastic agent (Code: CHEBI:35610) immunomodulator (Code: CHEBI:50846) Angiogenesis Inhibitors (Code: D020533) Angiogenesis Modulating Agents (Code: D043924) Antineoplastic Agents (Code: D000970) Growth Inhibitors (Code: D006131) Growth Substances (Code: D006133) Immunologic Factors (Code: D007155) Thalidomide Analog (Code: N0000184014) 2013-02-08 FDA Y70
Click to view quifenadine Quifenadine is a quinuclidine derivative and a non-sedating antihistamines, which combines a high selective activity to block histamine type 1 receptors and an ability to block serotonin and to break down histamine directly in tissues. Quifenadine is used for the treatment of different allergic conditions. Histamine Agents (Code: D018494) Histamine Antagonists (Code: D006633) Neurotransmitter Agents (Code: D018377) 2006-02-17 Ministry of Health of the Russian Federation
Click to view ospemifene Estrogen receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P03372, gene: ESR1, swissprot: ESR1_HUMAN) modulator an estrogen agonist/antagonist with tissue selective effects, its biological actions are mediated through binding to estrogen receptors, this binding results in activation of estrogenic pathways in some tissues (agonism) and blockade of estrogenic pathways in others (antagonism) estrogen receptor modulator (Code: CHEBI:50739) antineoplastic agent (Code: CHEBI:35610) anti-inflammatory agent (Code: CHEBI:67079) Estrogen Agonist/Antagonist (Code: N0000175826) Selective Estrogen Receptor Modulators (Code: N0000000168) 2013-02-26 FDA
Click to view cetyl alcohol has been used for eczema, skin irritations; RN given refers to parent cpd; structure 1990-08-02 FDA PL3
Click to view regorafenib Proto-oncogene tyrosine-protein kinase receptor Ret (Organism: Homo sapiens, class: Kinase, accessions: P07949, gene: RET, swissprot: RET_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/204369lbl.pdf) Vascular endothelial growth factor receptor 2 (Organism: Homo sapiens, class: Kinase, accessions: P35968, gene: KDR, swissprot: VGFR2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/204369lbl.pdf) Vascular endothelial growth factor receptor 1 (Organism: Homo sapiens, class: Kinase, accessions: P17948, gene: FLT1, swissprot: VGFR1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/204369lbl.pdf) Vascular endothelial growth factor receptor 3 (Organism: Homo sapiens, class: Kinase, accessions: P35916, gene: FLT4, swissprot: VGFR3_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/204369lbl.pdf) Mast/stem cell growth factor receptor Kit (Organism: Homo sapiens, class: Kinase, accessions: P10721, gene: KIT, swissprot: KIT_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/204369lbl.pdf) Platelet-derived growth factor receptor alpha (Organism: Homo sapiens, class: Kinase, accessions: P16234, gene: PDGFRA, swissprot: PGFRA_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/204369lbl.pdf) Platelet-derived growth factor receptor beta (Organism: Homo sapiens, class: Kinase, accessions: P09619, gene: PDGFRB, swissprot: PGFRB_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/204369lbl.pdf) Fibroblast growth factor receptor 1 (Organism: Homo sapiens, class: Kinase, accessions: P11362, gene: FGFR1, swissprot: FGFR1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/204369lbl.pdf) Fibroblast growth factor receptor 2 (Organism: Homo sapiens, class: Kinase, accessions: P21802, gene: FGFR2, swissprot: FGFR2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/204369lbl.pdf) Angiopoietin-1 receptor (Organism: Homo sapiens, class: Kinase, accessions: Q02763, gene: TEK, swissprot: TIE2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/204369lbl.pdf) Discoidin domain-containing receptor 2 (Organism: Homo sapiens, class: Kinase, accessions: Q16832, gene: DDR2, swissprot: DDR2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/204369lbl.pdf) High affinity nerve growth factor receptor (Organism: Homo sapiens, class: Kinase, accessions: P04629, gene: NTRK1, swissprot: NTRK1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/204369lbl.pdf) RAF proto-oncogene serine/threonine-protein kinase (Organism: Homo sapiens, class: Kinase, accessions: P04049, gene: RAF1, swissprot: RAF1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/204369lbl.pdf) Serine/threonine-protein kinase B-raf (Organism: Homo sapiens, class: Kinase, accessions: P15056, gene: BRAF, swissprot: BRAF_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/204369lbl.pdf) Mitogen-activated protein kinase 11 (Organism: Homo sapiens, class: Kinase, accessions: Q15759, gene: MAPK11, swissprot: MK11_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/204369lbl.pdf) Tyrosine-protein kinase ABL1 (Organism: Homo sapiens, class: Kinase, accessions: P00519, gene: ABL1, swissprot: ABL1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/204369lbl.pdf) Tyrosine-protein kinase FRK (Organism: Homo sapiens, class: Kinase, accessions: P42685, gene: FRK, swissprot: FRK_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/204369lbl.pdf) Ephrin type-A receptor 2 (Organism: Homo sapiens, class: Kinase, accessions: P29317, gene: EPHA2, swissprot: EPHA2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/204369lbl.pdf) Bifunctional epoxide hydrolase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P34913, gene: EPHX2, swissprot: HYES_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23726028) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/204369lbl.pdf) UDP-glucuronosyltransferase 1-9 (Organism: Homo sapiens, class: Enzyme, accessions: O60656, gene: UGT1A9, swissprot: UD19_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/204369lbl.pdf) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/204369lbl.pdf) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/204369lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/204369lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/204369lbl.pdf) UDP-glucuronosyltransferase 1-1 (Organism: Homo sapiens, class: Enzyme, accessions: P22309, gene: UGT1A1, swissprot: UD11_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/204369lbl.pdf) UDP-glucuronosyltransferase 1-9 (Organism: Homo sapiens, class: Enzyme, accessions: O60656, gene: UGT1A9, swissprot: UD19_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/204369lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/204369lbl.pdf) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/204369lbl.pdf) Glycine receptor subunit alpha-1 (Organism: Homo sapiens, class: Ion channel, accessions: P23415, gene: GLRA1, swissprot: GLRA1_HUMAN) potentiator (Source: https://www.ncbi.nlm.nih.gov/pubmed/25790278) Regorafenib is a small molecule inhibitor of multiple membrane-bound and intracellular kinases involved in normal cellular functions and in pathologic processes such as oncogenesis, tumor angiogenesis, and maintenance of the tumor microenvironment. In in vivo models, regorafenib demonstrated anti-angiogenic activity in a rat tumor model, and inhibition of tumor growth as well as anti-metastatic activity in several mouse xenograft models including some for human colorectal carcinoma. Regorafenib is indicated for the treatment of patients with Metastatic colorectal cancer who have been previously treated with fluoropyrimidine-, oxaliplatin- and irinotecan-based chemotherapy, an anti-VEGF therapy, and, if KRAS wild type, an anti-EGFR therapy; Locally advanced, unresectable or metastatic gastrointestinal stromal tumor (GIST) who have been previously treated with imatinib mesylate and sunitinib malate. antineoplastic agent (Code: CHEBI:35610) Kinase Inhibitor (Code: N0000175605) Protein Kinase Inhibitors (Code: N0000175076) Cytochrome P450 2C9 Inhibitors (Code: N0000185504) 2012-09-27 FDA
Click to view tedisamil Potassium voltage-gated channel subfamily A member 7 (Organism: Mus musculus, class: Unclassified, accessions: Q17ST2, gene: Kcna7, swissprot: KCNA7_MOUSE) blocker (Source: ) a multiple potassium channel blocker which blocks the rapid (IKr), slow (IKs) and ultrarapid (IKur) components of the delayed rectifier potassium current, the transient outward potassium current (Ito) and the ATP (IKATP) sensitive and the acetylcholine-activated (IKACH) potassium currents Anti-Arrhythmia Agents (Code: D000889) Cardiotonic Agents (Code: D002316) Cardiovascular Agents (Code: D002317) Protective Agents (Code: D020011) 2008-05-21 UK Medicines and Healthcare Products Regulatory Agency (MHRA)
Click to view metabutethamine Metabutethamine is a local anesthetic used in dentistry to produce infiltration and nerve block anesthesia. Anesthetics (Code: D000777)
Click to view metamizole Transient receptor potential cation channel subfamily A member 1 (Organism: Homo sapiens, class: Ion channel, accessions: O75762, gene: TRPA1, swissprot: TRPA1_HUMAN) blocker (Source: http://www.ncbi.nlm.nih.gov/pubmed/25765567) Glucose-6-phosphate 1-dehydrogenase (Organism: Homo sapiens, class: Enzyme, accessions: P11413, gene: G6PD, swissprot: G6PD_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11440730) Metamizole has a role as a non-steroidal anti-inflammatory drug, a non-narcotic analgesic, an antirheumatic drug, a peripheral nervous system drug, an antipyretic, a prodrug and a cyclooxygenase 3 inhibitor. It was withdrawn from US market in 1977 on the basis of reports of agranulocytosis. Withdrawn from the Canadian market in 1963. prodrug (Code: CHEBI:50266) non-narcotic analgesic (Code: CHEBI:35481) antirheumatic drug (Code: CHEBI:35842) peripheral nervous system drug (Code: CHEBI:49110) antipyretic (Code: CHEBI:35493) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antipyretics (Code: D058633) Antirheumatic Agents (Code: D018501) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1949-05-10 Swissmedic (Switzerland)
Click to view methylatropine Methylatropine is a quaternary salt of atropine. It was used for relieving pyloric spasm in infants. The drug has the same action as atropine and antagonizes muscarinic acetylcholine receptors. Autonomic Agents (Code: D001337) Parasympatholytics (Code: D010276) Peripheral Nervous System Agents (Code: D018373)
Click to view creatine Creatine is a glycine derivative having methyl and amidino groups attached to the nitrogen. Creatine is an endogenous amino acid derivative produced by vertebrate animals and occurring primarily in muscle cells. Creatine is important for energy storage; it is phosphorylated to creatine phosphate, which serves as a phosphate donor in the conversion of ADP to ATP and supplies energy necessary for muscle contraction. Dietary supplementation with creatine may improve muscle wasting associated with cancer and other chronic diseases. CRN
Click to view benzoin Benzoin is a ketone that consists of acetophenone bearing hydroxy and phenyl substituents at the alpha-position. The parent of the class of benzoins. Benzoin was first reported in 1832 by Justus von Liebig and Friedrich Woehler during their research on oil of bitter almond, which is benzaldehyde with traces of hydrocyanic acid. This should not be confused with benzoin gum from STYRAX.
Click to view octinoxate a UV filter compound 1992-12-07 FDA
Click to view avobenzone Tyrosinase (Organism: Homo sapiens, class: Enzyme, accessions: P14679, gene: TYR, swissprot: TYRO_HUMAN) inhibitor causes allergic or photoallergic contact dermatitis; structure given in first source Cosmetics (Code: D003358) Dermatologic Agents (Code: D003879) Protective Agents (Code: D020011) Radiation-Protective Agents (Code: D011837) Sunscreening Agents (Code: D013473) 1992-12-07 FDA
Click to view methyl salicylate Methyl salicylate is an organic ester naturally produced by many species of plants, particularly wintergreens. Methyl salicylate is used as a rubefacient and analgesic in deep heating liniments for acute joint and muscular pain. It is used as a flavoring agent in chewing gums and mints in small concentrations and added as antiseptic in mouthwash solutions. flavouring agent (Code: CHEBI:35617) insect attractant (Code: CHEBI:24850) Antirheumatic Agents (Code: D018501) Fixatives (Code: D005404) 2008-02-20 FDA
Click to view tafluprost Prostaglandin F2-alpha receptor (Organism: Homo sapiens, class: GPCR, accessions: P43088, gene: PTGFR, swissprot: PF2R_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/202514s003s004lbl.pdf) Prostaglandin G/H synthase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P35354, gene: PTGS2, swissprot: PGH2_HUMAN) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/22910791) Tafluprost is a prostaglandin analog is a selective FP prostanoid receptor agonist which is believed to reduce intraocular pressure by increasing uveoscleral outflow. Tafluprost is indicated for reducing elevated intraocular pressure in patients with open-angle glaucoma or ocular hypertension. Prostaglandin Analog (Code: N0000175454) Prostaglandin Receptor Agonists (Code: N0000000106) Increased Prostaglandin Activity (Code: N0000009526) Prostaglandins (Code: N0000007706) 2012-02-10 FDA
Click to view Ioflupane I-123 a radiopharmaceutical indicated for striatal dopamine transporter visualization using single photon emission computed tomography (SPECT) brain imaging to assist in the evaluation of adult patients with suspected Parkinsonian syndromes (PS) radiopharmaceutical (Code: CHEBI:35232) Radioactive Diagnostic Agent (Code: N0000177914) Radiopharmaceutical Activity (Code: N0000000205) 2011-01-14 FDA
Click to view telbivudine Telbivudine is a synthetic thymidine nucleoside analogue with activity against HBV DNA polymerase. It is phosphorylated by cellular kinases to the active triphosphate form. Telbivudine 5'-triphosphate inhibits HBV DNA polymerase (reverse transcriptase) by competing with the natural substrate, thymidine 5'-triphosphate. Incorporation of telbivudine 5'-triphosphate into viral DNA causes DNA chain termination. antiviral drug (Code: CHEBI:36044) Hepatitis B Virus Nucleoside Analog Reverse Transcriptase Inhibitor (Code: N0000175656) Nucleoside Analog (Code: N0000175459) Nucleoside Reverse Transcriptase Inhibitors (Code: N0000009947) Anti-Infective Agents (Code: D000890) Antiviral Agents (Code: D000998) Enzyme Inhibitors (Code: D004791) Nucleic Acid Synthesis Inhibitors (Code: D019384) 2006-10-25 FDA LLT
Click to view formaldehyde Formaldehyde is a colorless poisonous gas synthesized by the oxidation of methanol and used as an antiseptic, disinfectant, histologic fixative, and general-purpose chemical reagent for laboratory applications. Formaldehyde is readily soluble in water and is commonly distributed as a 37% solution in water; formalin, a 10% solution of formaldehyde in water, is used as a disinfectant and to preserve biological specimens. Environmentally, formaldehyde may be found in the atmosphere, smoke from fires, automobile exhaust and cigarette smoke. Small amounts are produced during normal metabolic processes in most organisms, including humans. Formaldehyde vapors are toxic, upon entry formaldehyde reacts readily with macromolecules, including DNA to form DNA-protein and DNA-DNA cross-links. Anti-Infective Agents (Code: D000890) Disinfectants (Code: D004202) Fixatives (Code: D005404) Standardized Chemical Allergen (Code: N0000185508) Increased Histamine Release (Code: N0000175629) Cell-mediated Immunity (Code: N0000184306) Allergens (Code: N0000171131) FDA FOR
Click to view mequinol Tyrosinase (Organism: Homo sapiens, class: Enzyme, accessions: P14679, gene: TYR, swissprot: TYRO_HUMAN) substrate (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020922s006lbl.pdf) Mequinol is 4-hydroxyanisole. The mechanism of action of mequinol is unknown. Although mequinol is a substrate for the enzyme tyrosinase and acts as a competitive inhibitor of the formation of melanin precursors, the clinical significance of these findings is unknown. Mequinol is a skin lightening agent. Mequinol is used in combination with tretinoin as an adjunct to a comprehensive skin care and sun avoidance program where the patient should primarily either avoid the sun or use protective clothing. Antineoplastic Agents (Code: D000970) Antioxidants (Code: D000975) Protective Agents (Code: D020011) Depigmenting Activity (Code: N0000175851) Melanin Synthesis Inhibitors (Code: N0000175850) Skin Lightening Agent (Code: N0000175855) 1999-12-10 FDA 4KS
Click to view vilazodone Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) inhibitor (Source: ) 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) agonist (Source: ) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) agonist (Source: ) Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) agonist (Source: ) 5-hydroxytryptamine receptor 4 (Organism: Homo sapiens, class: GPCR, accessions: Q13639, gene: HTR4, swissprot: 5HT4R_HUMAN) agonist (Source: ) D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) agonist (Source: ) 5-hydroxytryptamine receptor 7 (Organism: Rattus norvegicus, class: GPCR, accessions: P32305, gene: Htr7, swissprot: 5HT7R_RAT D(3) dopamine receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P19020, gene: Drd3, swissprot: DRD3_RAT Serotonin 3 (5-HT3) receptor (Organism: Rattus norvegicus, class: Ion channel, accessions: P35563|Q9JJ16, gene: Htr3a|Htr3b, swissprot: 5HT3A_RAT|5HT3B_RAT 5-hydroxytryptamine receptor 2C (Organism: Rattus norvegicus, class: GPCR, accessions: P08909, gene: Htr2c, swissprot: 5HT2C_RAT 5-hydroxytryptamine receptor 2A (Organism: Rattus norvegicus, class: GPCR, accessions: P14842, gene: Htr2a, swissprot: 5HT2A_RAT Sodium-dependent serotonin transporter (Organism: Rattus norvegicus, class: Transporter, accessions: P31652, gene: Slc6a4, swissprot: SC6A4_RAT D(4) dopamine receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P30729, gene: Drd4, swissprot: DRD4_RAT 5-hydroxytryptamine receptor 6 (Organism: Rattus norvegicus, class: GPCR, accessions: P31388, gene: Htr6, swissprot: 5HT6R_RAT 5-hydroxytryptamine receptor 1B (Organism: Rattus norvegicus, class: GPCR, accessions: P28564, gene: Htr1b, swissprot: 5HT1B_RAT 5-hydroxytryptamine receptor 1A (Organism: Rattus norvegicus, class: GPCR, accessions: P19327, gene: Htr1a, swissprot: 5HT1A_RAT 5-hydroxytryptamine receptor 1D (Organism: Rattus norvegicus, class: GPCR, accessions: P28565, gene: Htr1d, swissprot: 5HT1D_RAT Adrenergic receptor alpha-2 (Organism: Homo sapiens, class: GPCR, accessions: P08913|P18089|P18825, gene: ADRA2A|ADRA2B|ADRA2C, swissprot: ADA2A_HUMAN|ADA2B_HUMAN|ADA2C_HUMAN Adrenergic receptor alpha-1 (Organism: Homo sapiens, class: GPCR, accessions: P25100|P35348|P35368, gene: ADRA1A|ADRA1B|ADRA1D, swissprot: ADA1A_HUMAN|ADA1B_HUMAN|ADA1D_HUMAN 5-hydroxytryptamine receptor 4 (Organism: Rattus norvegicus, class: GPCR, accessions: Q62758, gene: Htr4, swissprot: 5HT4R_RAT D(2) dopamine receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P61169, gene: Drd2, swissprot: DRD2_RAT A benzofuran, indole, and piperazine derivative that functions as a SEROTONIN UPTAKE INHIBITOR and partial SEROTONIN 5-HT1 RECEPTOR AGONIST. It is used as an ANTIDEPRESSIVE AGENT. antidepressant (Code: CHEBI:35469) serotonergic agonist (Code: CHEBI:35941) serotonin uptake inhibitor (Code: CHEBI:50949) Antidepressive Agents (Code: D000928) Central Nervous System Agents (Code: D002491) Membrane Transport Modulators (Code: D049990) Neurotransmitter Agents (Code: D018377) Neurotransmitter Uptake Inhibitors (Code: D014179) Psychotropic Drugs (Code: D011619) Serotonin 5-HT1 Receptor Agonists (Code: D058825) Serotonin Agents (Code: D018490) Serotonin Receptor Agonists (Code: D017366) Serotonin Uptake Inhibitors (Code: D017367) 2011-01-21 FDA
Click to view pirfenidone Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022535s012,208780s002lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022535s012,208780s002lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022535s012,208780s002lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022535s012,208780s002lbl.pdf) Cytochrome P450 2E1 (Organism: Homo sapiens, class: Enzyme, accessions: P05181, gene: CYP2E1, swissprot: CP2E1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022535s012,208780s002lbl.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022535s012,208780s002lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022535s012,208780s002lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022535s012,208780s002lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022535s012,208780s002lbl.pdf) Cytochrome P450 2E1 (Organism: Homo sapiens, class: Enzyme, accessions: P05181, gene: CYP2E1, swissprot: CP2E1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022535s012,208780s002lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022535s012,208780s002lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022535s012,208780s002lbl.pdf) Pirfenidone is an immunosuppresant. It is used for the treatment of idiopathic pulmonary fibrosis. It has a role as a non-narcotic analgesic, a non-steroidal anti-inflammatory drug and an antipyretic. non-narcotic analgesic (Code: CHEBI:35481) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) antipyretic (Code: CHEBI:35493) Pyridone (Code: N0000191420) Pyridones (Code: N0000007575) Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antineoplastic Agents (Code: D000970) Antirheumatic Agents (Code: D018501) Central Nervous System Agents (Code: D002491) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 2008-09-16 PMDA
Click to view axitinib Vascular endothelial growth factor receptor 1 (Organism: Homo sapiens, class: Kinase, accessions: P17948, gene: FLT1, swissprot: VGFR1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/202324s008lbl.pdf) Vascular endothelial growth factor receptor 2 (Organism: Homo sapiens, class: Kinase, accessions: P35968, gene: KDR, swissprot: VGFR2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/202324s008lbl.pdf) Vascular endothelial growth factor receptor 3 (Organism: Homo sapiens, class: Kinase, accessions: P35916, gene: FLT4, swissprot: VGFR3_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/202324s008lbl.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/202324s008lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/202324s008lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/202324s008lbl.pdf) Cytochrome P450 3A5 (Organism: Homo sapiens, class: Enzyme, accessions: P20815, gene: CYP3A5, swissprot: CP3A5_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/202324s008lbl.pdf) UDP-glucuronosyltransferase 1-1 (Organism: Homo sapiens, class: Enzyme, accessions: P22309, gene: UGT1A1, swissprot: UD11_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/202324s008lbl.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/202324s008lbl.pdf) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/202324s008lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/202324s008lbl.pdf) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/24398510) Axitinib is an indazole derivative and a second generation tyrosine kinase inhibitor that works by selectively inhibiting vascular endothelial growth factor receptors (VEGFR-1, VEGFR-2, VEGFR-3). Through this mechanism of action, axitinib blocks angiogenesis, tumour growth and metastases. It is reported to exhibit potency that is 50-450 times higher than that of the first generation VEGFR inhibitors. Axitinib is indicated for the treatment of advanced renal cell carcinoma after failure of one prior systemic therapy. antineoplastic agent (Code: CHEBI:35610) Kinase Inhibitor (Code: N0000175605) Receptor Tyrosine Kinase Inhibitors (Code: N0000020000) Enzyme Inhibitors (Code: D004791) Protein Kinase Inhibitors (Code: D047428) 2012-01-27 FDA AXI
Click to view ingenol mebutate Protein kinase C delta type (Organism: Homo sapiens, class: Kinase, accessions: Q05655, gene: PRKCD, swissprot: KPCD_HUMAN) activator (Source: http://www.ncbi.nlm.nih.gov/pubmed/15126366) Protein kinase C alpha type (Organism: Homo sapiens, class: Kinase, accessions: P17252, gene: PRKCA, swissprot: KPCA_HUMAN) Protein kinase C beta type (Organism: Homo sapiens, class: Kinase, accessions: P05771, gene: PRKCB, swissprot: KPCB_HUMAN) Protein kinase C epsilon type (Organism: Homo sapiens, class: Kinase, accessions: Q02156, gene: PRKCE, swissprot: KPCE_HUMAN) Serine/threonine-protein kinase D1 (Organism: Homo sapiens, class: Kinase, accessions: Q15139, gene: PRKD1, swissprot: KPCD1_HUMAN) Protein kinase C gamma type (Organism: Homo sapiens, class: Kinase, accessions: P05129, gene: PRKCG, swissprot: KPCG_HUMAN) activator (Source: ) protein kinase C agonist and antineoplastic antineoplastic agent (Code: CHEBI:35610) Cell Death Inducer (Code: N0000184015) Increased Cellular Death (Code: N0000009176) 2012-01-23 FDA
Click to view icatibant B2 bradykinin receptor (Organism: Homo sapiens, class: GPCR, accessions: P30411, gene: BDKRB2, swissprot: BKRB2_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/022150s000lbl.pdf) Aminopeptidase N (Organism: Homo sapiens, class: Enzyme, accessions: P15144, gene: ANPEP, swissprot: AMPN_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17026984) B1 bradykinin receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P97583, gene: Bdkrb1, swissprot: BKRB1_RAT) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10422787) B1 bradykinin receptor (Organism: Homo sapiens, class: GPCR, accessions: P46663, gene: BDKRB1, swissprot: BKRB1_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10422787) Icatibant is a competitive antagonist selective for the bradykinin B2 receptor, with an affinity similar to bradykinin. Hereditary angioedema is caused by an absence or dysfunction of C1-esterase-inhibitor, a key regulator of the Factor XII/kallikrein proteolytic cascade that leads to bradykinin production. Bradykinin is a vasodilator which is thought to be responsible for the characteristic HAE symptoms of localized swelling, inflammation, and pain. Icatibant inhibits bradykinin from binding the B2 receptor and thereby treats the clinical symptoms of an acute, episodic attack of HAE. beta-adrenergic antagonist (Code: CHEBI:35530) Bradykinin B2 Receptor Antagonist (Code: N0000182965) Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Bradykinin B2 Receptor Antagonists (Code: D065094) Bradykinin Receptor Antagonists (Code: D065168) Complement Inactivating Agents (Code: D051056) Immunologic Factors (Code: D007155) Immunosuppressive Agents (Code: D007166) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 2008-07-11 EMA
Click to view crizotinib Hepatocyte growth factor receptor (Organism: Homo sapiens, class: Kinase, accessions: P08581, gene: MET, swissprot: MET_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/202570s027lbl.pdf) Proto-oncogene tyrosine-protein kinase ROS (Organism: Homo sapiens, class: Kinase, accessions: P08922, gene: ROS1, swissprot: ROS1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/202570s027lbl.pdf) Macrophage-stimulating protein receptor (Organism: Homo sapiens, class: Kinase, accessions: Q04912, gene: MST1R, swissprot: RON_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/202570s027lbl.pdf) ALK tyrosine kinase receptor (Organism: Homo sapiens, class: Kinase, accessions: Q9UM73, gene: ALK, swissprot: ALK_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/202570s027lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23686600) Cytochrome P450 3A5 (Organism: Homo sapiens, class: Enzyme, accessions: P20815, gene: CYP3A5, swissprot: CP3A5_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23686600) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23686600) Insulin receptor (Organism: Homo sapiens, class: Kinase, accessions: P06213, gene: INSR, swissprot: INSR_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21708465) Crizotinib is an inhibitor of receptor tyrosine kinases including ALK, Hepatocyte Growth Factor Receptor (HGFR, c-Met), ROS1 (c-ros), and Recepteur d'Origine Nantais (RON). Translocations can affect the ALK gene resulting in the expression of oncogenic fusion proteins. The formation of ALK fusion proteins results in activation and dysregulation of the gene's expression and signaling which can contribute to increased cell proliferation and survival in tumors expressing these proteins. Crizotinib demonstrated concentration-dependent inhibition of ALK, ROS1, and c-Met phosphorylation in cell-based assays using tumor cell lines and demonstrated antitumor activity in mice bearing tumor xenografts that expressed echinoderm microtubule-associated protein-like 4 (EML4)- or nucleophosmin (NPM)-ALK fusion proteins or c-Met. antineoplastic agent (Code: CHEBI:35610) biomarker (Code: CHEBI:59163) Kinase Inhibitor (Code: N0000175605) Cytochrome P450 3A Inhibitors (Code: N0000190114) Receptor Tyrosine Kinase Inhibitors (Code: N0000020000) Cytochrome P450 2B6 Inhibitors (Code: N0000182139) P-Glycoprotein Inhibitors (Code: N0000185503) Organic Cation Transporter 1 Inhibitors (Code: N0000191265) Organic Cation Transporter 2 Inhibitors (Code: N0000187061) Enzyme Inhibitors (Code: D004791) Protein Kinase Inhibitors (Code: D047428) 2011-08-26 FDA VGH
Click to view deferiprone iron (Organism: None, class: Inorganic material, accessions: None, gene: None, swissprot: None) chelating agent (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/021825s003lbl.pdf) UDP-glucuronosyltransferase 1-6 (Organism: Homo sapiens, class: Enzyme, accessions: P19224, gene: UGT1A6, swissprot: UD16_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021825s004lbl.pdf) Deferiprone is a chelating agent with an affinity for ferric ion (iron III). Deferiprone binds with ferric ions to form neutral 3:1 (deferiprone:iron) complexes that are stable over a wide range of pH values. Deferiprone has a lower binding affinity for other metals such as copper, aluminum and zinc than for iron. Deferiprone is indicated for the treatment of patients with transfusional iron overload due to thalassemia syndromes when current chelation therapy is inadequate. protective agent (Code: CHEBI:50267) Iron Chelating Activity (Code: N0000000144) Iron Chelator (Code: N0000175522) Chelating Agents (Code: D002614) Iron Chelating Agents (Code: D007502) Sequestering Agents (Code: D064449) 2011-10-14 FDA
Click to view hydroxyprogesterone caproate Progesterone receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P06401, gene: PGR, swissprot: PRGR_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/18060946) Hydroxyprogesterone caproate is a synthetic progestin. It is an ester derivative of 17alpha-hydroxyprogesterone formed from caproic acid (hexanoic acid). Mimicking the action of progesterone, hydroxyprogesterone caporate binds to and activates nuclear progesterone receptors in the reproductive system and causes the ligand-receptor complex to be translocated to the nucleus where it binds to and promotes expression of target genes. Hydroxyprogesterone caproate is used as a contraceptive and to reduce the risk of preterm birth in women with a singleton pregnancy who have a history of singleton spontaneous preterm birth. Progesterone Congeners (Code: N0000011301) Progestin (Code: N0000175602) Estrogen Antagonists (Code: D004965) Hormone Antagonists (Code: D006727) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Progestins (Code: D011372) 1974-12-26 FDA
Click to view talbutal Talbutal is a short to intermediate-acting barbiturate. Talbutal has been used as a sedative and hypnotic, but then this usage was discontinued. 1954-09-21 FDA
Click to view ethanol Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15285839) Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/12824820) Cytochrome P450 1A1 (Organism: Homo sapiens, class: Enzyme, accessions: P04798, gene: CYP1A1, swissprot: CP1A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9929510) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9929510) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9929510) Kir3.1/Kir3.4 (Organism: Homo sapiens, class: Ion channel, accessions: P48544|P48549, gene: KCNJ3|KCNJ5, swissprot: KCNJ3_HUMAN|KCNJ5_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/10570486) Glycine receptor subunit alpha-1 (Organism: Homo sapiens, class: Ion channel, accessions: P23415, gene: GLRA1, swissprot: GLRA1_HUMAN) potentiator (Source: https://www.ncbi.nlm.nih.gov/pubmed/8700149) Glycine receptor subunit alpha-2 (Organism: Homo sapiens, class: Ion channel, accessions: P23416, gene: GLRA2, swissprot: GLRA2_HUMAN) potentiator (Source: https://www.ncbi.nlm.nih.gov/pubmed/8700149) Gamma-aminobutyric acid receptor subunit delta (Organism: Homo sapiens, class: Ion channel, accessions: O14764, gene: GABRD, swissprot: GBRD_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/17591544) Ethanol is a primary alcohol that is ethane in which one of the hydrogens is substituted by a hydroxy group. Ethanol affects the brain’s neurons in several ways. It alters their membranes as well as their ion channels, enzymes, and receptors. Alcohol also binds directly to the receptors for acetylcholine, serotonin, GABA, and the NMDA receptors for glutamate. The sedative effects of ethanol are mediated through binding to GABA receptors and glycine receptors (alpha 1 and alpha 2 subunits). It also inhibits NMDA receptor functioning. In its role as an anti-infective, ethanol acts as an osmolyte or dehydrating agent that disrupts the osmotic balance across cell membranes. It has bactericidal activity and is used often as a topical disinfectant. It is widely used as a solvent and preservative in pharmaceutical preparations as well as serving as the primary ingredient in alcoholic beverages. antiseptic drug (Code: CHEBI:48218) polar solvent (Code: CHEBI:48354) central nervous system depressant (Code: CHEBI:35488) Anti-Infective Agents (Code: D000890) Anti-Infective Agents, Local (Code: D000891) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Solvents (Code: D012997) 1946-01-17 FDA EOH
Click to view guanidine Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12089365) Solute carrier family 22 member 3 (Organism: Homo sapiens, class: Transporter, accessions: O75751, gene: SLC22A3, swissprot: S22A3_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/9632645) Solute carrier family 22 member 5 (Organism: Homo sapiens, class: Transporter, accessions: O76082, gene: SLC22A5, swissprot: S22A5_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/9618255) Solute carrier family 22 member 4 (Organism: Homo sapiens, class: Transporter, accessions: Q9H015, gene: SLC22A4, swissprot: S22A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10215651) Multidrug and toxin extrusion protein 1 (Organism: Homo sapiens, class: Transporter, accessions: Q96FL8, gene: SLC47A1, swissprot: S47A1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/17509534) Multidrug and toxin extrusion protein 2 (Organism: Homo sapiens, class: Transporter, accessions: Q86VL8, gene: SLC47A2, swissprot: S47A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/17509534) Potassium voltage-gated channel subfamily A member 2 (Organism: Oncorhynchus mykiss, class: Ion channel, accessions: Q9I830, gene: kcna2, swissprot: KCNA2_ONCMY) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21926190) Guanidine is a small basic compound. It is found in the urine as a normal product of protein metabolism. It is also used in laboratory research as a protein denaturant. Guanidine stimulates the neuromuscular junction presynaptically by inhibiting voltage-gated potassium channels, leading to the enhanced release of acetylcholine in the synaptic cleft. This stimulatory effect of guanidine underlies its use in the therapy for the neuromuscular diseases. The hydrochloride salt of guanidine was approved for the reduction of the symptoms of muscle weakness and easy fatigability associated with the myasthenic syndrome of Eaton-Lambert. Acetylcholine Releasing Agent (Code: N0000175772) Increased Acetylcholine Activity (Code: N0000009079) 1939-10-02 FDA GAI
Click to view corticorelin ovine used in diagnosis of adrenocortical insufficiency & Cushing's syndrome; AA sequence given in first source; MF C205-H339-N59-O63-S; RN given refers to triflutate salt; RN for parent cpd not avail 3/94 diagnostic agent (Code: CHEBI:33295) 1996-05-23 FDA
Click to view vinyl ether Vinyl ether is a clear, nearly colorless, volatile liquid which was used as an inhalation anesthetic. Vinyl ether's only strengths compared to ethyl ether are favorable induction and recovery. During anesthesia vinyl ether has no particularly wonderful properties and is harder to control than other agents. Therefore, vinyl ether was commonly used as a preliminary anesthetic before administration of diethyl ether. Additionally, vinyl ether was only used for short operations or analgesia, e.g. dentistry and obstetrics. Vinyl ether was used infrequently for long operations because of toxicity, cost, and superior alternatives. Anesthetics (Code: D000777) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492)
Click to view propiolactone Propiolactone (beta-propiolactone) is disinfectant which was used in vapor form to sterilize vaccines, grafts, etc. It is no longer used for medical disinfection. Dermal exposure to beta-propiolactone causes the burning or blistering of the skin, and ingestion of this substance burns the mouth and stomach while exposure to its vapors causes severe irritation of the eyes, throat and respiratory tract. This substance is reasonably anticipated to be a human carcinogen. Anti-Infective Agents (Code: D000890) Disinfectants (Code: D004202) 1959-06-12 FDA
Click to view ethyl chloride Ethyl chloride is the simplest and least toxic member of the class of chloroethanes, that is ethane in which a single hydrogen is substituted by a chlorine. A colourless gas at room temperature and pressure (boiling point 12?), it is used as a mild topical anaesthetic to numb the skin prior to ear piercing, skin biopsies, etc., and is also used in the treatment of sports injuries. It was formerly used in the production of tetraethyllead. It is still used in the treatment of cellulose to make ethylcellulose for commercial products. Also ethyl chloride is used as a diagnostic tool to detect a dead tooth with nonviable pulp. Anesthetics (Code: D000777) Anesthetics, Local (Code: D000779) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1965-07-01 Spanish Agency of Medicines and Medical Products (AEMPS) MCE
Click to view glycine Glycine N-acyltransferase (Organism: Homo sapiens, class: Transporter, accessions: Q6IB77, gene: GLYAT, swissprot: GLYAT_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/22475485) Glycine amidinotransferase, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P50440, gene: GATM, swissprot: GATM_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/3800397) Glycine receptor (alpha-1/beta) (Organism: Homo sapiens, class: Ion channel, accessions: P23415|P48167, gene: GLRA1|GLRB, swissprot: GLRA1_HUMAN|GLRB_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/14551753) Glycine receptor subunit alpha-1 (Organism: Homo sapiens, class: Ion channel, accessions: P23415, gene: GLRA1, swissprot: GLRA1_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/14551753) Sodium-coupled neutral amino acid transporter 2 (Organism: Homo sapiens, class: Transporter, accessions: Q96QD8, gene: SLC38A21, swissprot: S38A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10930503) Sodium-coupled neutral amino acid transporter 1 (Organism: Homo sapiens, class: Transporter, accessions: Q9H2H9, gene: SLC38A1, swissprot: S38A1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11342143) Sodium-coupled neutral amino acid transporter 5 (Organism: Homo sapiens, class: Transporter, accessions: Q8WUX1, gene: SLC38A5, swissprot: S38A5_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11243884) Glycine (Gly) is a natural amino acid neurotransmitter that acts as a co-agonist at Glutamate receptors in the brain and is an activator of glycine receptors, GLRA1-3, GLRB. The abnormal Gly levels have been implicated in neuropsychiatric disorders. Alterations in Gly levels are implicated in several diseases of the central nervous system. Glycine is a component of a nutrients mixture for peripheral administration to well-nourished mildly catabolic adult patients who require only short-term parenteral nutrition. nutraceutical (Code: CHEBI:50733) hepatoprotective agent (Code: CHEBI:62868) NMDA receptor agonist (Code: CHEBI:64571) Glycine Agents (Code: D018684) Neurotransmitter Agents (Code: D018377) 1976-05-25 FDA GLY
Click to view acetohydroxamic acid Urease (Organism: Sporosarcina pasteurii, class: Enzyme, accessions: P41020|P41021|P41022, gene: ureC|ureB|ureA, swissprot: URE1_SPOPA|URE2_SPOPA|URE3_SPOPA) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/29913313) Acetohydroxamic Acid, a synthetic drug derived from hydroxylamine and ethyl acetate, is similar in structure to urea. In the urine, it acts as an antagonist of the bacterial enzyme urease. This inhibits the hydrolysis of urea and production of ammonia in urine infected with urea-splitting organisms, leading to a decrease in pH and ammonia levels. As antimicrobial agents are more effective in such conditions, the effectiveness of these agents is amplified, resulting in a higher cure rate. Acetohydroxamic Acid has no direct antimicrobial action and does not acidify urine directly. It is used, in addition to antibiotics or medical procedures, to treat chronic urea-splitting urinary infections. Urease Inhibitor (Code: N0000175611) Urease Inhibitors (Code: N0000175087) Enzyme Inhibitors (Code: D004791) 1983-05-31 FDA HAE
Click to view hydroxycarbamide Carbonic anhydrase 5A, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P35218, gene: CA5A, swissprot: CAH5A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16759856) Carbonic anhydrase 9 (Organism: Homo sapiens, class: Enzyme, accessions: Q16790, gene: CA9, swissprot: CAH9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16759856) Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16759856) Ribonucleoside-diphosphate reductase subunit M2 (Organism: Homo sapiens, class: Enzyme, accessions: P31350, gene: RRM2, swissprot: RIR2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15670581) Ribonucleoside-diphosphate reductase large subunit (Organism: Homo sapiens, class: Enzyme, accessions: P23921, gene: RRM1, swissprot: RIR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15670581) Hydroxyurea is an antimetabolite. The precise mechanism by which hydroxyurea produces its antineoplastic effects cannot, at present, be described. The reports of various studies in tissue culture in rats and humans lend support to the hypothesis that hydroxyurea causes an immediate inhibition of DNA synthesis by acting as a ribonucleotide reductase inhibitor, without interfering with the synthesis of ribonucleic acid or of protein. This hypothesis explains why, under certain conditions, hydroxyurea may induce teratogenic effects. Hydroxyurea is indicated for the treatment of resistant chronic myeloid leukemia or locally advanced squamous cell carcinomas of the head and neck (excluding the lip) in combination with chemoradiation. antineoplastic agent (Code: CHEBI:35610) immunomodulator (Code: CHEBI:50846) Antimetabolite (Code: N0000180853) Urea (Code: N0000006999) Antineoplastic Agents (Code: D000970) Antisickling Agents (Code: D000986) Enzyme Inhibitors (Code: D004791) Hematologic Agents (Code: D006401) Nucleic Acid Synthesis Inhibitors (Code: D019384) 1967-12-07 FDA NHY
Click to view propylene glycol Propylene glycol (1, 2-propanediol) is an organic compound (a diol alcohol), usually a tasteless, odorless, and colorless clear oily liquid that is hygroscopic and miscible with water, acetone, and chloroform. Propylene glycol is used as a solvent for intravenous, oral, and topical pharmaceutical preparations It is generally considered safe. However in large doses it can be toxic, especially if given over a short period of time. Propylene glycol is metabolized by the liver to form lactate, acetate, and pyruvate. Propylene glycol toxicity includes development of serum hyperosmolality, lactic acidosis, and kidney failure. It has been suggested that proximal tubular necrosis is the cause of acute kidney injury from propylene glycol. Propylene glycol induced intoxication can also mimic sepsis or systemic inflammatory response syndrome (SIRS). Propylene glycol also is used for the temporary relief of burning and irritation due to dryness of the eye. protic solvent (Code: CHEBI:48356) Pharmaceutic Aids (Code: D010592) Pharmaceutical Vehicles (Code: D014677) Solvents (Code: D012997) PGO
PGR
Click to view mercaptamine cystine (Organism: None, class: Unnatural amino acid, accessions: None, gene: None, swissprot: None) cleavage (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/200740s000lbl.pdf) Myeloperoxidase (Organism: Homo sapiens, class: Enzyme, accessions: P05164, gene: MPO, swissprot: PERM_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/2829860) Mercaptamine (cysteamine) is a cystine-depleting agent which lowers the cystine content of cells in patients with cystinosis. Cysteamine acts as a cystine-depleting agent by converting cystine to cysteine and cysteine-cysteamine mixed disulfides and reduces corneal cystine crystal accumulation. Mercaptamine indicated for the treatment of corneal cystine crystal accumulation in patients with cystinosis. Cystine Depleting Agents (Code: D065104) Cystine Depleting Agent (Code: N0000187051) Cystine Disulfide Reduction (Code: N0000175549) 1994-08-15 FDA DHL
Click to view dimethyl sulfoxide Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11159803) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11159803) Cytochrome P450 2E1 (Organism: Homo sapiens, class: Enzyme, accessions: P05181, gene: CYP2E1, swissprot: CP2E1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11159803) Dimethyl sulfoxide (DMSO) is a highly polar organic liquid, that is used widely as a chemical solvent. Because of its ability to penetrate biological membranes, it is used as a vehicle for topical application of pharmaceuticals. It is also used to protect tissue during cryopreservation. The mechanism of dimethyl sulfoxide's actions is not well understood. Dimethyl sulfoxide shows a range of pharmacological activity including analgesia and anti-inflammation. Dimethyl sulfoxide is indicated for the symptomatic relief of patients with interstitial cystitis. polar aprotic solvent (Code: CHEBI:48358) non-narcotic analgesic (Code: CHEBI:35481) antidote (Code: CHEBI:50247) Antioxidants (Code: D000975) Cryoprotective Agents (Code: D003451) Free Radical Scavengers (Code: D016166) Protective Agents (Code: D020011) Solvents (Code: D012997) 1978-04-04 FDA DMS
Click to view fomepizole Alcohol dehydrogenase (Organism: Homo sapiens, class: Enzyme, accessions: P00325|P07327|P00326, gene: ADH1A|ADH1B|ADH1C, swissprot: ADH1A_HUMAN|ADH1B_HUMAN|ADH1G_HUMAN) inhibitor (Source: https://pdf.hres.ca/dpd_pm/00041975.PDF) Fomepizole is a competitive inhibitor of alcohol dehydrogenase, the enzyme that catalyzes the initial steps in the metabolism of ethylene glycol and methanol to their toxic metabolites. Fomepizole is indicated as an antidote for ethylene glycol (such as antifreeze) or methanol poisoning, or for use in suspected ethylene glycol or methanol ingestion, either alone or in combination with hemodialysis. antidote (Code: CHEBI:50247) protective agent (Code: CHEBI:50267) Antidotes (Code: D000931) Protective Agents (Code: D020011) 1997-12-04 FDA 4PZ
Click to view piperazine Piperazine is a cyclic organic compound possessing two nitrogen atoms in opposite positions within a 6-member heterocyclic ring that serves as a backbone for piperazine derivatives and acts as a gamma-amino-butyric acid (GABA) receptor agonist in nematodes, with potential anti-helminthic activity. Upon administration, piperazine binds to the GABA inhibitory receptors in susceptible nematodes, thereby inducing chloride channel opening and hyperpolarization. This results in paralysis of the worm musculature and allows normal peristalsis to dislodge the worm from the intestinal lumen, which causes the worm to be expelled from the body. Unlike vertebrates where GABA is restricted to the central nervous system (CNS), the GABA receptors in helminths are also expressed in the peripheral nervous system. Piperazine was first introduced as an anthelmintic in 1953. Piperazine has been withdrawn from use on the grounds that other more effective and less toxic drugs are now available. Anthelmintics (Code: D000871) Anti-Infective Agents (Code: D000890) Antinematodal Agents (Code: D000969) Antiparasitic Agents (Code: D000977) 1954-07-12 FDA PZE
Click to view cyverine Cyverine is an antispasmodic drugs. It is used for the treatment of gastric ulcer.
Click to view deanol Deanol (dimethylaminoethanol (DMAE) or dimethylethanolamine (DMEA)) holds tertiary amine and primary alcohol groups as functional groups. Deanol has been used in the treatment of attention deficit-hyperactivity disorder (ADHD), Alzheimer's disease, autism, and tardive dyskinesia. It has been also used as an ingredient in skin care, and in cognitive function- and mood-enhancing products. The mechanism of action is not well understood. Now deanol is used for the treatment of general fatigue (asthenia). curing agent (Code: CHEBI:75358) Anti-Dyskinesia Agents (Code: D018726) Antidepressive Agents (Code: D000928) Central Nervous System Agents (Code: D002491) Psychotropic Drugs (Code: D011619) 1972-09-01 Spanish Agency of Medicines and Medical Products (AEMPS)
Click to view benzyl alcohol Benzyl Alcohol is a colorless liquid with a sharp burning taste and slight odor. Benzyl Alcohol is an aromatic alcohol used in a wide variety of cosmetic formulations as a fragrance component, preservative, solvent, and viscosity-decreasing agent. Benzyl Alcohol is metabolized to Benzoic Acid, which reacts with glycine and excreted as hippuric acid in the human body. Acceptable daily intakes were established by the World Health Organization at 5 mg/kg for Benzyl Alcohol. It is used as a local anesthetic and to reduce pain associated with Lidocaine injection. Also, it is used in the manufacture of other benzyl compounds, as a pharmaceutical aid, and in perfumery and flavoring. Benzyl alcohol is approved for the treatment of head lice. The drug acts on head lice by inhibiting them from closing their respiratory spiracles, allowing the vehicle to obstruct the spiracles and causing the lice to asphyxiate. solvent (Code: CHEBI:46787) fragrance (Code: CHEBI:48318) Pediculicide (Code: N0000181811) Anesthetics (Code: D000777) Anesthetics, Local (Code: D000779) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 2009-04-09 FDA 010
Click to view lactic acid Lactic Acid is the racemic isomer of lactic acid, the biologically active isoform in humans. Lactic acid or lactate is produced during fermentation from pyruvate by lactate dehydrogenase. This reaction, in addition to producing lactic acid, also produces nicotinamide adenine dinucleotide (NAD) that is then used in glycolysis to produce energy source adenosine triphosphate (ATP). Lactic Acid is primarily indicated as a source of bicarbonate for prevention or control of mild to moderate metabolic acidosis in patients with restricted oral intake whose oxidative processes are not seriously impaired. Sodium Lactate is most commonly associated with an E number of “E325” Sodium Lactate blends are commonly used in meat and poultry products to extend shelf life and increase food safety. 2006-10-25 FDA LAC
2OP
Click to view glycerol Cytochrome P450 2E1 (Organism: Homo sapiens, class: Enzyme, accessions: P05181, gene: CYP2E1, swissprot: CP2E1_HUMAN) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/9113273) Glycerol is a triol with a structure of propane substituted at positions 1, 2 and 3 by hydroxy groups. Glycerol is commonly classified as an osmotic laxative but may act additionally or alternatively through its local irritant effects; it may also have lubricating and fecal softening actions. When administered rectally, glycerol exerts a hygroscopic and/or local irritant action, drawing water from the tissues into the feces and reflexively stimulating evacuation. Glycerol decreases intraocular pressure by creating an osmotic gradient between the blood and intraocular fluid, causing fluid to move out of the aqueous and vitreous humors into the bloodstream. It is used as a solvent, emollient, pharmaceutical agent, and sweetening agent. solvent (Code: CHEBI:46787) detergent (Code: CHEBI:27780) Non-Standardized Chemical Allergen (Code: N0000185370) Increased Histamine Release (Code: N0000175629) Cell-mediated Immunity (Code: N0000184306) Increased IgG Production (Code: N0000185001) Allergens (Code: N0000171131) Glycerol (Code: N0000006566) Cryoprotective Agents (Code: D003451) Protective Agents (Code: D020011) Solvents (Code: D012997) 1979-01-31 ANSM (French National Agency for Medicines and Health Products Safety) GOL
Click to view methylpentynol Methylpentynol is a tertiary hexanol with hypnotic, sedative and anticonvulsant effects. It was used for the treatment of insomnia and as sedaive agent, but its use was quickly phased out in response to newer drugs with more favorable safety profiles. Methylpentynol is no longer available.
Click to view secretin porcine stimulate pancreatic ductal cells to secrete pancreas fluid in large volumes that contain bicarbonate 2002-04-04 FDA
Click to view loxoprofen Prostaglandin G/H synthase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P23219, gene: PTGS1, swissprot: PGH1_HUMAN) inhibitor (Source: ) Prostaglandin G/H synthase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P35354, gene: PTGS2, swissprot: PGH2_HUMAN) inhibitor (Source: ) Loxoprofen is a propionic acid derivative and a non-steroidal anti-inflammatory drug. After oral administration loxoprofen sodium hydrate is absorbed from the gastrointestinal tract as an unchanged compound with only a modest gastric-mucosal irritation. It is then rapidly biotransformed into the active metabolite trans-OH form (SRS coordination) with a potent inhibitory effect on prostaglandin biosynthesis to exert its pharmacologic effects. It is used to treat rheumatoid arthritis, osteoarthritis, to reduce pain and inflammation after surgery, wounds and tooth removal. Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) non-narcotic analgesic (Code: CHEBI:35481) antipyretic (Code: CHEBI:35493) prodrug (Code: CHEBI:50266) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 2005-12-22 PMDA
Click to view aminopicoline Nitric oxide synthase, brain (Organism: Homo sapiens, class: Enzyme, accessions: P29475, gene: NOS1, swissprot: NOS1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/8937711) Nitric oxide synthase, endothelial (Organism: Homo sapiens, class: Enzyme, accessions: P29474, gene: NOS3, swissprot: NOS3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/8937711) Nitric oxide synthase, inducible (Organism: Homo sapiens, class: Enzyme, accessions: P35228, gene: NOS2, swissprot: NOS2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/8937711) Nitric oxide synthase, inducible (Organism: Mus musculus, class: Enzyme, accessions: P29477, gene: Nos2, swissprot: NOS2_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/8937711) Aminopicoline (2-Amino-4-methylpyridine) acts as ligand and forms methoxo-bridged copper(II) complexes. Aminopicoline is potent inhibitor of inducible nitric oxide synthase (iNOS) in vitro. Aminopicoline is used in the synthesis of 2-amino-4-methyl­pyridinium 2-hy­droxy­benzoate. BVF
Click to view glutaral Glutaral (glutaraldehyde) is used as an antimicrobial agent in sugar mills and as a fixing agent in the immobilisation of glucose isomerase enzyme preparations for use in the manufacture of high fructose corn syrup A polymerized isomer of glutaraldehyde known as polycycloglutaracetal is a fertilizer for aquatic plants. It is claimed that it provides a bioavailable source of carbon for higher plants that is not available to algae. Though not marketed as such due to federal regulations, the biocidal effect of glutaraldehyde kills most algae at concentrations of 0. 5 - 5. 0 ppm. These levels are not harmful to most aquatic fauna and flora. Adverse reactions have been observed by some aquarists at these concentrations in some aquatic mosses, liverworts, and vascular plants. Glutaraldehyde is a colorless liquid with a pungent odor used to disinfect medical and dental equipment. It is also used for industrial water treatment and as a chemical preservative. It is used as a tissue fixative in electron microscopy. It is employed as an embalming fluid, is a component of leather tanning solutions, and occurs as an intermediate in the production of certain industrial chemicals. Glutaraldehyde is frequently used in biochemistry applications as an amine-reactive homobifunctional crosslinker. The oligomeric state of proteins can be examined through this application. However, it is toxic, causing severe eye, nose, throat and lung irritation, along with headaches, drowsiness and dizziness. It is a main source of occupational asthma among health care providers. cross-linking reagent (Code: CHEBI:50684) Anti-Infective Agents (Code: D000890) Cross-Linking Reagents (Code: D003432) Disinfectants (Code: D004202) Fixatives (Code: D005404) Indicators and Reagents (Code: D007202) 1984-08-01 PMDA PTD
Click to view cycloserine Alanine racemase (Organism: Mycobacterium tuberculosis (strain ATCC 25618 / H37Rv), class: Enzyme, accessions: P9WQA9, gene: alr, swissprot: ALR_MYCTU) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12499203) D-alanine--D-alanine ligase (Organism: Mycobacterium tuberculosis (strain ATCC 25618 / H37Rv), class: Enzyme, accessions: P9WP31, gene: ddl, swissprot: DDL_MYCTU) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12499203) Glutamate NMDA receptor (Organism: Rattus norvegicus, class: Ion channel, accessions: P35439|Q00959|Q00960|Q00961|Q62645|Q9R1M7|Q8VHN2, gene: Grin1|Grin2a|Grin2b|Grin2c|Grin2d|Grin3a|Grin3b, swissprot: NMDZ1_RAT|NMDE1_RAT|NMDE2_RAT|NMDE3_RAT|NMDE4_RAT|NMD3A_RAT|NMD3B_RAT) partial agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/2157524) Cycloserine is a 4-amino-1,2-oxazolidin-3-one that has R configuration. It is an antibiotic produced by Streptomyces garyphalus or S. orchidaceus. Cycloserine suppresses the synthesis of bacterial wall by inhibitin two enzymes: alanine racemase and d-alanine ligase. Cycloserine is used as part of a multi-drug regimen for the treatment of tuberculosis when resistance to, or toxicity from, primary drugs has developed. NMDA receptor agonist (Code: CHEBI:64571) antiinfective agent (Code: CHEBI:35441) antitubercular agent (Code: CHEBI:33231) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Anti-Infective Agents, Urinary (Code: D000892) Antibiotics, Antitubercular (Code: D000904) Antimetabolites (Code: D000963) Antitubercular Agents (Code: D000995) Noxae (Code: D009676) Renal Agents (Code: D012076) 1964-06-29 FDA 4AX
Click to view gamma-aminobutyric acid Gamma-aminobutyric acid receptor subunit rho-1 (Organism: Homo sapiens, class: Ion channel, accessions: P24046, gene: GABRR1, swissprot: GBRR1_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/23294161) GABA-A receptor alpha-1/beta-2/gamma-2 (Organism: Homo sapiens, class: Ion channel, accessions: P14867|P47870|P18507, gene: GABRA1|GABRB2|GABRG2, swissprot: GBRA1_HUMAN|GBRB2_HUMAN|GBRG2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/23294161) GABA-A receptor alpha-2/beta-2/gamma-2 (Organism: Homo sapiens, class: Ion channel, accessions: P47869|P47870|P18507, gene: GABRA2|GABRB2|GABRG2, swissprot: GBRA1_HUMAN|GBRB2_HUMAN|GBRG2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/23294161) Aminobutyric acid (GABA), a naturally occurring substance, which is a product of decarboxylation of the amino acid glutamate mediated by the synthesizing enzyme glutamic acid decarboxylase. GABA is a major inhibitory neurotransmitter of the brain and acts mainly through the GABAA receptor. GABA is locally produced by the pancreatic beta cells. GABAARs are also expressed in various immune cells, including T-cells, peripheral blood mononuclear cells, and exerted immune-inhibitory effects. GABA is sold as a dietary supplement. GABA Agents (Code: D018682) Neurotransmitter Agents (Code: D018377) FDA ABU
Click to view choline Choline O-acetyltransferase (Organism: Homo sapiens, class: Enzyme, accessions: P28329, gene: CHAT, swissprot: CLAT_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/17144655) Choline/ethanolamine kinase (Organism: Homo sapiens, class: Kinase, accessions: Q9Y259, gene: CHKB, swissprot: CHKB_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/19915674) Choline kinase alpha (Organism: Homo sapiens, class: Kinase, accessions: P35790, gene: CHKA, swissprot: CHKA_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/19915674) Solute carrier family 22 member 1 (Organism: Homo sapiens, class: Transporter, accessions: O15245, gene: SLC22A1, swissprot: S22A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12089365) Solute carrier family 22 member 1 (Organism: Homo sapiens, class: Transporter, accessions: O15245, gene: SLC22A1, swissprot: S22A1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10385678) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10385678) Solute carrier family 22 member 3 (Organism: Homo sapiens, class: Transporter, accessions: O75751, gene: SLC22A3, swissprot: S22A3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9632645) Solute carrier family 22 member 5 (Organism: Homo sapiens, class: Transporter, accessions: O76082, gene: SLC22A5, swissprot: S22A5_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9618255) Solute carrier family 22 member 4 (Organism: Homo sapiens, class: Transporter, accessions: Q9H015, gene: SLC22A4, swissprot: S22A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10215651) Choline transporter-like protein 1 (Organism: Homo sapiens, class: Transporter, accessions: Q8WWI5, gene: SLC44A1, swissprot: CTL1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/16319125) Vesicular acetylcholine transporter (Organism: Rattus norvegicus, class: Transporter, accessions: Q62666, gene: Slc18a3, swissprot: VACHT_RAT) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15485505) Choline is a major part of the polar head group of phosphatidylcholine. Phosphatidylcholine's role in the maintenance of cell membrane integrity is vital to all of the basic biological processes: information flow, intracellular communication and bioenergetics. Inadequate choline intake would negatively affect all these processes. Choline is also a major part of sphingomyelin also important for the maintenance of cell structure and function. Choline deficiency in cell culture causes apoptosis or programmed cell death. This appears to be due to abnormalities in cell membrane phosphatidylcholine content and an increase in ceramide, a precursor, as well as a metabolite, of sphingomyelin. Ceramide accumulation, which is caused by choline deficiency, appears to activate Caspase that mediates apoptosis. Betaine or trimethylglycine is derived from choline via an oxidation reaction. Choline is a precursor to acetylcholine. Choline is also needed for gallbladder regulation, liver function and lecithin (a key lipid) formation. Adequate acetylcholine levels in the brain are believed to be protective against certain types of dementia, including Alzheimer's disease. Choline is used for nutritional supplementation, also for treating dietary shortage or imbalance. Antimetabolites (Code: D000963) Central Nervous System Agents (Code: D002491) Gastrointestinal Agents (Code: D005765) Hypolipidemic Agents (Code: D000960) Lipid Regulating Agents (Code: D057847) Lipotropic Agents (Code: D008082) Nootropic Agents (Code: D018697) CHT
Click to view nicotinyl alcohol Nicotinyl alcohol is an alcohol analog of nicotinic acid which is a direct-acting peripheral vasodilator that causes flushing and may decrease blood pressure. Nicotinyl alcohol (pyridylcarbinol) is rapidly oxidized to nicotinic acid. Nicotinyl alcohol is used as a vasodilator agent and an antilipemic drug. (See: nicotinic acid) Cardiovascular Agents (Code: D002317) Vasodilator Agents (Code: D014665) 1964 CDSCO (INDIA) PYF
Click to view resorcinol Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18501600) Prostaglandin G/H synthase 1 (Organism: Ovis aries, class: Enzyme, accessions: P05979, gene: PTGS1, swissprot: PGH1_SHEEP) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15568761) Carbonic anhydrase 14 (Organism: Homo sapiens, class: Enzyme, accessions: Q9ULX7, gene: CA14, swissprot: CAH14_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18579385) Carbonic anhydrase 5A, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P35218, gene: CA5A, swissprot: CAH5A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18579385) Carbonic anhydrase 13 (Organism: Mus musculus, class: Enzyme, accessions: Q9D6N1, gene: Ca13, swissprot: CAH13_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18579385) Carbonic anhydrase 9 (Organism: Homo sapiens, class: Enzyme, accessions: Q16790, gene: CA9, swissprot: CAH9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18579385) Carbonic anhydrase 12 (Organism: Homo sapiens, class: Enzyme, accessions: O43570, gene: CA12, swissprot: CAH12_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18579385) Carbonic anhydrase (Organism: Dicentrarchus labrax, class: Unclassified, accessions: Q2PCB5, gene: ca, swissprot: Q2PCB5_DICLA) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21669522) Carbonic anhydrase 5B, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: Q9Y2D0, gene: CA5B, swissprot: CAH5B_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18579385) Resorcinol is a benzenediol that is benzene dihydroxylated at positions 1 and 3. It is used as an antiseptic and disinfectant in topical pharmaceutical products in the treatment of skin disorders and infections such as acne, seborrheic dermatitis, eczema, psoriasis, corns, calluses, and warts. 1956-02-01 Spanish Agency of Medicines and Medical Products (AEMPS) RCO
Click to view hydroquinone Carbonic anhydrase 14 (Organism: Homo sapiens, class: Enzyme, accessions: Q9ULX7, gene: CA14, swissprot: CAH14_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18579385) Carbonic anhydrase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P22748, gene: CA4, swissprot: CAH4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18579385) Carbonic anhydrase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P00915, gene: CA1, swissprot: CAH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18579385) Carbonic anhydrase 5A, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P35218, gene: CA5A, swissprot: CAH5A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18579385) Carbonic anhydrase 13 (Organism: Mus musculus, class: Enzyme, accessions: Q9D6N1, gene: Ca13, swissprot: CAH13_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18579385) Carbonic anhydrase 9 (Organism: Homo sapiens, class: Enzyme, accessions: Q16790, gene: CA9, swissprot: CAH9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18579385) Carbonic anhydrase 12 (Organism: Homo sapiens, class: Enzyme, accessions: O43570, gene: CA12, swissprot: CAH12_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18579385) Carbonic anhydrase (Organism: Dicentrarchus labrax, class: Unclassified, accessions: Q2PCB5, gene: ca, swissprot: Q2PCB5_DICLA) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18579385) Carbonic anhydrase 5B, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: Q9Y2D0, gene: CA5B, swissprot: CAH5B_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18579385) Carbonic anhydrase 3 (Organism: Homo sapiens, class: Enzyme, accessions: P07451, gene: CA3, swissprot: CAH3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18579385) Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18579385) Carbonic anhydrase 15 (Organism: Mus musculus, class: Enzyme, accessions: Q99N23, gene: Ca15, swissprot: CAH15_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18501600) Polyphenol oxidase 2 (Organism: Agaricus bisporus, class: Enzyme, accessions: O42713, gene: PPO2, swissprot: PPO2_AGABI) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19181523) Hydroquinone is a melanin synthesis inhibitor. It is prepared from the reduction of p-benzoquinone with sodium bisulfite. Hydroquinone is used as a topical application in skin whitening to reduce the color of skin.The FDA stated that hydroquinone cannot be ruled out as a potential carcinogen. skin lightening agent (Code: CHEBI:85046) Antioxidants (Code: D000975) Mutagens (Code: D009153) Noxae (Code: D009676) Protective Agents (Code: D020011) Radiation-Protective Agents (Code: D011837) Depigmenting Activity (Code: N0000175851) Melanin Synthesis Inhibitor (Code: N0000175854) Melanin Synthesis Inhibitors (Code: N0000175850) 2002-01-18 FDA HQE
Click to view histamine Histamine H4 receptor (Organism: Homo sapiens, class: GPCR, accessions: Q9H3N8, gene: HRH4, swissprot: HRH4_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/21044842) Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12626648) Histamine H2 receptor (Organism: Homo sapiens, class: GPCR, accessions: P25021, gene: HRH2, swissprot: HRH2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/21044842) Histamine H3 receptor (Organism: Homo sapiens, class: GPCR, accessions: Q9Y5N1, gene: HRH3, swissprot: HRH3_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/21044842) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12089365) Histamine is a depressor amine derived by enzymatic decarboxylation of histidine. Histamine physiological functions are mediated by four 7-transmembrane G protein-coupled receptors (H1R, H2R, H3R, H4R) that are all targets of pharmacological intervention. It is a powerful stimulant of gastric secretion, a constrictor of bronchial smooth muscle, a vasodilator, and a centrally acting neurotransmitter. Phosphate salt of histamine was used as a diagnostic aid for evaluation of gastric acid secretory function. In addition, this compound is used as a positive control in evaluation of allergenic (immediate hypersensitivity or "Type I") skin testing. Histamine Agents (Code: D018494) Histamine Agonists (Code: D017442) Neurotransmitter Agents (Code: D018377) 1939-04-25 FDA HSM
Click to view betazole Betazole is a histamine H2 receptor agonist with diagnostic application. Betazole selectively targets and binds to the H2 receptor, thereby mimicking the effect of histamine on these receptors. This may lead to an increase in gastric secretions. Betazole can be used in gastric function tests. histamine agonist (Code: CHEBI:35678) diagnostic agent (Code: CHEBI:33295) gastrointestinal drug (Code: CHEBI:55324) Gastrointestinal Agents (Code: D005765) Histamine Agents (Code: D018494) Histamine Agonists (Code: D017442) Neurotransmitter Agents (Code: D018377) 1982-01-01 FDA
Click to view thiamazole Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9172960) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9172960) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9172960) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9172960) Thyroid peroxidase (Organism: Sus scrofa, class: Enzyme, accessions: P09933, gene: TPO, swissprot: PERT_PIG) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10365684) Thiamazole is a thionamide antithyroid agent that inhibits the synthesis of thyroid hormones. Thiamazole is indicated for the treatment of hyperthyroidism; for the amelioration of hyperthyroid symptoms in preparation for thyroidectomy or radioactive iodine therapy. antithyroid drug (Code: CHEBI:50671) Antithyroid Agents (Code: D013956) Hormone Antagonists (Code: D006727) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Thyroid Hormone Synthesis Inhibitor (Code: N0000175918) Thyroid Hormone Synthesis Inhibitors (Code: N0000175917) 1950-06-21 FDA MMZ
Click to view tuaminoheptane Tuaminoheptane is a vasoconstrictor and a sympathomimetic amine. Tuaminoheptane acts similarly to ephedrine. Tuaminoheptane is used as a nasal decongestant in combination with other drugs. 1983-04-22 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view methylhexaneamine Methylhexaneamine is an amphetamine derivative. It was used as a nasal decongestant. Now methylhexaneamine is used as a dietary supplement with stimulant properties.
Click to view cacodylic acid Cacodylic acid (dimethylarsinic acid) is classified as a member of the Pentaorganoarsanes. Cacodylic acid induces an organ-specific lesion-single strand breaks in DNA. Mechanistic studies have suggested that this damage is due mainly to the peroxyl radical of cacodylic acid and production of active oxygen species by pulmonary tissues. Multi-organ initiation-promotion studies have demonstrated that cacodylic acid acts as a promotor of urinary bladder, kidney, liver and thyroid gland cancers in rats and as a promotor of lung tumors in mice. Cacodylic acid is used as a buffering agent in the preparation and fixation of biological samples for electron microscopy. Also cacodylic acid is used as a non-selective herbicide and defoliant for general weed control. Herbicides (Code: D006540) Pesticides (Code: D010575) CAC
CAD
Click to view fumaric acid Carbonic anhydrase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P00915, gene: CA1, swissprot: CAH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19962903) Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19962903) Carbonic anhydrase 5A, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P35218, gene: CA5A, swissprot: CAH5A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19962903) Carbonic anhydrase 5B, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: Q9Y2D0, gene: CA5B, swissprot: CAH5B_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19962903) Transmembrane prolyl 4-hydroxylase (Organism: Homo sapiens, class: Enzyme, accessions: Q9NXG6, gene: P4HTM, swissprot: P4HTM_HUMAN) inhbiitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17182618) Fumaric acid, naturally found in organisms, is a well-known intermediate of the citric acid cycle. Fumaric acid has been identified as an oncometabolite or an endogenous, cancer causing metabolite. High levels of this organic acid can be found in tumors or biofluids surrounding tumors. Oncogenic action of fumarate appears to due to its ability to inhibit prolyl hydroxylase-containing enzymes. Fumaric acid is found to be associated with fumarase deficiency, which is an inborn error of metabolism. food acidity regulator (Code: CHEBI:64049) FUM
Click to view succinic acid Succinate receptor 1 (Organism: Homo sapiens, class: GPCR, accessions: Q9BXA5, gene: SUCNR1, swissprot: SUCR1_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/15141213) Solute carrier family 22 member 8 (Organism: Homo sapiens, class: Transporter, accessions: Q8TCC7, gene: SLC22A8, swissprot: S22A8_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11306713) Succinic acid is a dicarboxylic acid, which has multiple biological roles as a metabolic intermediate being converted into fumarate by the enzyme succinate dehydrogenase in complex 2 of the electron transport chain which is involved in making ATP, and as a signaling molecule reflecting the cellular metabolic state. Succinate is generated in mitochondria via the tricarboxylic acid cycle (TCA), an energy-yielding process shared by all organisms. Succinate can exit the mitochondrial matrix and function in the cytoplasm as well as the extracellular space, changing gene expression patterns, modulating epigenetic landscape or demonstrating hormone-like signaling. Dysregulation of succinate synthesis, and therefore ATP synthesis, happens in some genetic mitochondrial diseases, such as Leigh's disease, and Mela's disease and degradation can lead to pathological conditions, such as malignant transformation, inflammation and tissue injury. Succinic acid is a precursor to some polyesters and a component of some alkyd resins. Succinic acid is used primarily as an acidity regulator in the food and beverage industry. anti-ulcer drug (Code: CHEBI:49201) nutraceutical (Code: CHEBI:50733) 1971-11-16 FDA SIN
Click to view betaine Betaine is a naturally occurring compound that has been of interest for its role in osmoregulation. Betaine acts as a methyl group donor in the remethylation of homocysteine to methionine in patients with homocystinuria. Betaine occurs naturally in the body. It is a metabolite of choline and is present in small amounts in foods such as beets, spinach, cereals, and seafood. Betaine is indicated for the treatment of homocystinuria to decrease elevated homocysteine blood concentrations. Included within the category of homocystinuria are cystathionine beta-synthase (CBS) deficiency, 5,10-methylenetetrahydrofolate reductase (MTHFR) deficiency, cobalamin cofactor metabolism (cbl) defect. Antimetabolites (Code: D000963) Gastrointestinal Agents (Code: D005765) Hypolipidemic Agents (Code: D000960) Lipid Regulating Agents (Code: D057847) Lipotropic Agents (Code: D008082) Methylating Activity (Code: N0000175804) Methylating Agent (Code: N0000175805) 1996-10-25 FDA BET
Click to view aminohydroxybutyric acid Gamma-aminobutyric acid receptor subunit rho-1 (Organism: Homo sapiens, class: Ion channel, accessions: P24046, gene: GABRR1, swissprot: GBRR1_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/23019493) Aminohydroxybutyric acid (or gamma-Amino-beta-hydroxybutyric acid) is an endogenous ligand found in the central nervous system in mammals. Aminohydroxybutyric acid is a derivative of the neurotransmitter GABA. Aminohydroxybutyric acid is used for the treatment of stress and anxiety, for improvement learning and boost memory function. anticonvulsant (Code: CHEBI:35623) Anti-epileptic Agent (Code: N0000175753) Anticonvulsants (Code: D000927) 1961-06-27 Italian Medicines Agency (AIFA)
Click to view oxymethurea Oxymethurea is an antiseptic included in multi-ingredient preparations intended for the topical treatment of ear infections.
Click to view noxytiolin Noxythiolin is local antibacterial agent that probably acts by releasing formaldehyde in aqueous solutions. It is used for irrigation of infected body cavities - bladder, peritoneum, etc. and as a spray for burns. Anti-Infective Agents (Code: D000890) Anti-Infective Agents, Local (Code: D000891) 1977-02-03 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view trometamol Trometamol is a proton acceptor with a pK of 7.8, it is an effective buffer that can be used to maintain the pH of body fluids. Trometamol is indicated for the prevention and correction of metabolic acidosis. Trometamol also acts as an osmotic diuretic, increasing urine flow, urinary pH, and excretion of fixed acids, carbon dioxide and electrolytes. Buffers (Code: D002021) Excipients (Code: D005079) Pharmaceutic Aids (Code: D010592) Pharmaceutical Vehicles (Code: D014677) 1965-12-16 FDA TRS
Click to view cysteine Cysteine is a non-essential sulfur-containing amino acid in humans, related to cystine, Cysteine is important for protein synthesis, detoxification, and diverse metabolic functions. Found in beta-keratin, the main protein in nails, skin, and hair, Cysteine is important in collagen production, as well as skin elasticity and texture. Also required in the manufacture of amino acid taurine, Cysteine is a component of the antioxidant glutathione, and plays a role in the metabolism of essential biochemicals such as coenzyme A, heparin, and biotin. Amino Acid (Code: N0000175780) Amino Acids (Code: N0000006806) 1986-10-22 FDA CYS
DCY
Click to view nicotinamide Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15081432) Cytochrome P450 2E1 (Organism: Homo sapiens, class: Enzyme, accessions: P05181, gene: CYP2E1, swissprot: CP2E1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15081432) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15081432) NAD-dependent protein deacetylase sirtuin-2 (Organism: Homo sapiens, class: Enzyme, accessions: Q8IXJ6, gene: SIRT2, swissprot: SIR2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17149860) NAD-dependent deacetylase sirtuin 3 (Organism: Homo sapiens, class: Enzyme, accessions: Q9NTG7, gene: SIRT3, swissprot: SIR3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19700324) NAD-dependent protein deacetylase sirtuin-1 (Organism: Homo sapiens, class: Enzyme, accessions: Q96EB6, gene: SIRT1, swissprot: SIR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19700324) NAD-dependent protein deacylase sirtuin-5, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: Q9NXA8, gene: SIRT5, swissprot: SIR5_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/24900427) Nicotinamide ia an important compound functioning as a component of the coenzyme NAD. Its primary significance is in the prevention and/or cure of blacktongue and pellagra. Most animals cannot manufacture this compound in amounts sufficient to prevent nutritional deficiency and it therefore must be supplemented through dietary intake. neuroprotective agent (Code: CHEBI:63726) anti-inflammatory agent (Code: CHEBI:67079) Growth Substances (Code: D006133) Micronutrients (Code: D018977) Vitamins (Code: D014815) Vitamin B Complex (Code: D014803) 1953-02-20 FDA NCA
Click to view nicotinic acid Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15081432) Solute carrier organic anion transporter family member 2B1 (Organism: Homo sapiens, class: Transporter, accessions: O94956, gene: SLCO2B1, swissprot: SO2B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12724351) Monocarboxylate transporter 1 (Organism: Rattus norvegicus, class: Transporter, accessions: P53987, gene: Slc16a1, swissprot: MOT1_RAT) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10579682) Hydroxycarboxylic acid receptor 2 (Organism: Homo sapiens, class: GPCR, accessions: Q8TDS4, gene: HCAR2, swissprot: HCAR2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/17358052) Hydroxycarboxylic acid receptor 2 (Organism: Rattus norvegicus, class: GPCR, accessions: Q80Z39, gene: Hcar2, swissprot: HCAR2_RAT) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/19309152) Nicotinic acid (niacin) is a water-soluble vitamin of the B complex occurring in various animal and plant tissues. It is required by the body for the formation of coenzymes NAD and NADP. It has pellagra-curative, vasodilating, and antilipemic properties. Niacin in gram doses reduces LDL-C, Apo B, Lp(a), TG, and TC, and increases HDL-C. The mechanism by which niacin alters lipid profiles is not completely understood and may involve several actions, including partial inhibition of release of free fatty acids from adipose tissue, and increased lipoprotein lipase activity. Niacin decreases the rate of hepatic synthesis of VLDL-C and LDL-C, and does not appear to affect fecal excretion of fats, sterols, or bile acids. Nicotinic acid is indicated to reduce elevated TC, LDL-C, Apo B and TG, and to increase HDL-C in patients with primary hyperlipidemia and mixed dyslipidemia, to reduce the risk of recurrent nonfatal myocardial infarction in patients with a history of myocardial infarction and hyperlipidemia. In combination with a bile acid binding resin nicotinic acid slows progression or promotes regression of atherosclerotic disease in patients with a history of coronary artery disease and hyperlipidemia. Nicotinic acid also indicated to reduce TG in adult patients with severe hypertriglyceridemia. B vitamin (Code: CHEBI:75769) vasodilator agent (Code: CHEBI:35620) antidote (Code: CHEBI:50247) antilipemic drug (Code: CHEBI:35679) Nicotinic Acid (Code: N0000175594) Nicotinic Acids (Code: N0000007641) Antimetabolites (Code: D000963) Cardiovascular Agents (Code: D002317) Growth Substances (Code: D006133) Hypolipidemic Agents (Code: D000960) Lipid Regulating Agents (Code: D057847) Micronutrients (Code: D018977) Vitamins (Code: D014815) Vasodilator Agents (Code: D014665) Vitamin B Complex (Code: D014803) 1957-07-24 FDA NIO
Click to view mecysteine Mecysteine is known as a mucolytic agent. Mecysteine works by breaking some of the chemical bonds between the molecules in mucus. Mecysteine is used as an adjunct in the management of conditions such as chronic obstructive pulmonary disease, when characterised by thick viscid or glutinous mucus, including the symptomatic relief of cough with sputum. Expectorants (Code: D005100) Respiratory System Agents (Code: D019141) 2006-02-24 UK Medicines and Healthcare Products Regulatory Agency (MHRA) CMT
Click to view pyrazinamide Aldehyde oxidase 1 (Organism: Rattus norvegicus, class: Enzyme, accessions: Q9Z0U5, gene: Aox1, swissprot: AOXA_RAT) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/8216357) Probable fatty acid synthase Fas (Fatty acid synthetase) (Organism: Mycobacterium tuberculosis (strain ATCC 25618 / H37Rv), class: Enzyme, accessions: P95029, gene: fas, swissprot: P95029_MYCTU) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17485499) Pyrazinamide is a synthetic pyrazinoic acid amide derivative with bactericidal property. Pyrazinamide is indicated for the initial treatment of active tuberculosis in adults and children. antitubercular agent (Code: CHEBI:33231) prodrug (Code: CHEBI:50266) Antimycobacterial (Code: N0000175483) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Antitubercular Agents (Code: D000995) 1971-06-03 FDA PZA
Click to view guaiacol Carbonic anhydrase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P00915, gene: CA1, swissprot: CAH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19231207) Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19231207) Guaiacol is a naturally occurring organic compound. Although it is biosynthesized by a variety of organisms, this yellowish aromatic oil is usually derived from guaiacum or wood creosote. Guaiacol is used as a reducing co-substrate for COX reactions. It is mainly used as expectorant, antiseptic. expectorant (Code: CHEBI:77035) 2006-10-27 UK Medicines and Healthcare Products Regulatory Agency (MHRA) JZ3
Click to view dimercaprol arsenic (Organism: None, class: Inorganic material, accessions: None, gene: None, swissprot: None) chelating agent (Source: https://www.ncbi.nlm.nih.gov/pubmed/20717537) cadmium (Organism: None, class: Inorganic material, accessions: None, gene: None, swissprot: None) chelating agent (Source: https://www.ncbi.nlm.nih.gov/pubmed/20717537) mercury (Organism: None, class: Inorganic material, accessions: None, gene: None, swissprot: None) chelating agent (Source: https://www.ncbi.nlm.nih.gov/pubmed/20717537) Dimercaprol is an anti-gas warfare agent that is effective against Lewisite (dichloro(2-chlorovinyl)arsine) and formerly known as British Anti-Lewisite or BAL. It acts as a chelating agent and is used in the treatment of arsenic, gold, and other heavy metal poisoning. Metal Chelating Activity (Code: N0000175472) Metal Chelator (Code: N0000175473) Chelating Agents (Code: D002614) Sequestering Agents (Code: D064449) 1946-05-06 FDA 9DC
Click to view foscarnet DNA polymerase catalytic subunit (Organism: Human herpesvirus 1 (strain 17), class: Enzyme, accessions: P04293, gene: None, swissprot: DPOL_HHV11) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020068s023lbl.pdf) Reverse transcriptase/RNaseH (Organism: Human immunodeficiency virus 1, class: Enzyme, accessions: Q72549, gene: pol, swissprot: Q72549_9HIV1) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15189038) Carbonic anhydrase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P00915, gene: CA1, swissprot: CAH1_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/15745821) Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15745821) Carbonic anhydrase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P22748, gene: CA4, swissprot: CAH4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15745821) Carbonic anhydrase 5A, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P35218, gene: CA5A, swissprot: CAH5A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15745821) Carbonic anhydrase 5B, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: Q9Y2D0, gene: CA5B, swissprot: CAH5B_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15745821) Carbonic anhydrase 9 (Organism: Homo sapiens, class: Enzyme, accessions: Q16790, gene: CA9, swissprot: CAH9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15745821) Foscarnet is a phosphonoformic acid. Foscarnet is an antiviral agent used in the treatment of cytomegalovirus retinitis. Foscarnet exerts its antiviral activity by a selective inhibition at the pyrophosphate binding site on virus-specific DNA polymerases at concentrations that do not affect cellular DNA polymerases. Foscarnet does not require activation (phosphorylation) by thymidine kinase or other kinases. Foscarnet also shows activity against human herpesviruses and HIV. antiviral drug (Code: CHEBI:36044) DNA Polymerase Inhibitors (Code: N0000020060) Pyrophosphate Analog (Code: N0000175469) Pyrophosphate Analog DNA Polymerase Inhibitor (Code: N0000175470) Chelating Activity (Code: N0000000087) Anti-Infective Agents (Code: D000890) Anti-Retroviral Agents (Code: D044966) Antiviral Agents (Code: D000998) Enzyme Inhibitors (Code: D004791) Nucleic Acid Synthesis Inhibitors (Code: D019384) Reverse Transcriptase Inhibitors (Code: D018894) 1991-09-27 FDA PPF
Click to view fluroxene Fluroxene, is a volatile, inhalational anesthetic. It was voluntarily withdrawn from the market in 1974 due to its potential flammability and accumulating evidence that it could cause organ toxicity.
Click to view phloroglucinol Prostaglandin G/H synthase 1 (Organism: Ovis aries, class: Enzyme, accessions: P05979, gene: PTGS1, swissprot: PGH1_SHEEP) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16252923) Beta-secretase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P56817, gene: BACE1, swissprot: BACE1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20462757) Phloroglucinol is a phenol derivative with antispasmodic properties that is used primarily as a laboratory reagent. The mechanism of action is most likely based on the direct inhibition of the voltage-dependent calcium channels of smooth muscle; however, the modulation of prostaglandin or nitric oxide release has also been suggested. Although it has long been used in clinical practice as an antispasmodic for painful urogenital and gastrointestinal conditions, in an early study on anesthetized rats, phloroglucinol was found to be inactive toward the contraction of the duodenum, ileum and colon. However in Irritable bowel syndrome (IBS) patients iv phloroglucinol effectively reduced postprandial rectosigmoid motility increases after a test meal, compared to placebo. Phloroglucinol is indicated for the treatment of pain in the intestine, bile ducts, bladder and uterus caused by spasm. Indicators and Reagents (Code: D007202) 2007-10-30 ANSM (French National Agency for Medicines and Health Products Safety) 13X
Click to view orazamide Orazamide is composed of one molecule of 5-aminoimidazole-4-carboxamide (AICA), one molecule of orotic acid and two molecules of water. The nucleoside of AICA is internalized and becomes phosphorylated by adenosine kinase to form AICAR mono-phosphate, an intermediate in the late steps of de novo purine biosynthesis. In hepatocytes, AICA can inhibit the fatty acid synthesis, sterol synthesis, and gluconeogenesis. Orazamide is used clinically for the treatment of hepatitis and cirrhosis. 1971 YEAR INTRODUCED 5AC
Click to view chloral hydrate GABA-A receptor alpha-2/beta-1 (Organism: Homo sapiens, class: Ion channel, accessions: P47869|P18505, gene: GABRA2|GABRB1, swissprot: GBRA1_HUMAN|GBRB1_HUMAN) positive allosteric modulator (Source: https://www.ncbi.nlm.nih.gov/pubmed/10683198) Glycine receptor subunit alpha-1 (Organism: Homo sapiens, class: Ion channel, accessions: P23415, gene: GLRA1, swissprot: GLRA1_HUMAN) positive allosteric modulator (Source: https://www.ncbi.nlm.nih.gov/pubmed/10683198) Chloral Hydrate is a synthetic monohydrate of chloral with sedative, hypnotic, and anticonvulsive properties. Chloral hydrate is converted to the active compound trichloroethanol by hepatic alcohol dehydrogenase. The agent interacts with various neurotransmitter-operated ion channels, thereby enhancing gamma-aminobutyric acid (GABA)-A receptor mediated chloride currents and inhibiting amino acid receptor-activated ion currents. In addition, chloral hydrate enhances the agonistic effects of glycine receptors, inhibits AMPA-induced calcium influx in cortical neurons, and facilitates 5-HT 3 receptor-mediated currents in ganglionic neurons. Overall, this results in a depressive effect on the central nervous system. Chloral Hydrate is used in the treatment of insomnia. The safety margin is too narrow for chloral hydrate to be used as a general anesthetic in humans, but it is commonly used for that purpose in animal experiments. It is no longer considered useful as an anti-anxiety medication. sedative (Code: CHEBI:35717) general anaesthetic (Code: CHEBI:38869) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Hypnotics and Sedatives (Code: D006993) 1840-01-01 YEAR INTRODUCED
Click to view pyrithione Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22365761) Carbonic anhydrase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P22748, gene: CA4, swissprot: CAH4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22365761) Carbonic anhydrase 5A, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P35218, gene: CA5A, swissprot: CAH5A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22365761) Carbonic anhydrase 5B, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: Q9Y2D0, gene: CA5B, swissprot: CAH5B_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22365761) Carbonic anhydrase 7 (Organism: Homo sapiens, class: Enzyme, accessions: P43166, gene: CA7, swissprot: CAH7_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22365761) Carbonic anhydrase 6 (Organism: Homo sapiens, class: Enzyme, accessions: P23280, gene: CA6, swissprot: CAH6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22365761) Pyrithione is the common name of an organosulfur compound with molecular formula C5H5NOS. It exists as a pair of tautomers, the major form being the thione 1-hydroxy-2(1H)-pyridinethione and the minor form being the thiol 2-mercaptopyridine N-oxide. It is used to prepare zinc pyrithione, which is used primarily to treat dandruff and seborrhoeic dermatitis in medicated shampoos. (See: pyrithione zinc) Anti-Infective Agents (Code: D000890) Antifungal Agents (Code: D000935)
Click to view thiouracil Nitric oxide synthase, brain (Organism: Rattus norvegicus, class: Enzyme, accessions: P29476, gene: Nos1, swissprot: NOS1_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11094150) Thiouracil is a sulfur-containing uracil. Thiouracil occurs in seeds of Brassica and Crucifera species. An established antithyroid drug and highly selective inhibitor of nitric oxide synthase (NOS), thiouracil also covalently binds to dopaquinone, produced by tyrosinase catalyzed oxidation of tyrosine, thereby selectively accumulating in de novo-synthesized melanin in overactive melanin-producing cells and providing a means to localize melanoma cells. It is known to cause blood dyscrasias and suspected of terato- and carcinogenesis. Antithyroid Agents (Code: D013956) Cardiovascular Agents (Code: D002317) Hormone Antagonists (Code: D006727) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Vasodilator Agents (Code: D014665) 3CJ
Click to view dichloroacetic acid [Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 1, mitochondrial (Organism: Rattus norvegicus, class: Kinase, accessions: Q63065, gene: Pdk1, swissprot: PDK1_RAT) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/9405293) [Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 2, mitochondrial (Organism: Rattus norvegicus, class: Kinase, accessions: Q64536, gene: Pdk2, swissprot: PDK2_RAT) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/9405293) [Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 3, mitochondrial (Organism: Homo sapiens, class: Kinase, accessions: Q15120, gene: PDK3, swissprot: PDK3_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/9405293) [Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 4, mitochondrial (Organism: Rattus norvegicus, class: Kinase, accessions: O54937, gene: Pdk4, swissprot: PDK4_RAT) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/9405293) Dichloroacetic acid (dichloroacetate) is an acid analog of acetic acid. Salts of dichloroacetate are used as drugs since they inhibit the enzyme pyruvate dehydrogenase kinase. Dichloroacetate is a noncompetitive inhibitor of the endoplasmic reticulum enzyme HMG CoA reductase, which catalyzes the rate limiting step in cholesterol biosynthesis. dichloroacetate has been researched in adults, children, animals, and cells as a monotherapy as well as in combination with other therapies for the treatment of severe metabolic disorders including diabetes and hypercholesterolemia, lactic acidosis, certain heart conditions, and cancer. TF4
Click to view flucytosine Cytosine deaminase (Organism: Candida albicans, class: Enzyme, accessions: P78594, gene: FCA1, swissprot: FCA1_CANAX) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/017001s033lbl.pdf) Flucytosine is a fluorinated cytosine analog that is used as an antifungal agent. Inside the fungal cell, flucytosine is rapidly converted to fluorouracil by the enzyme cytosine deaminase. Fluorouracil exerts its antifungal activity through the subsequent conversion into several active metabolites, which inhibit protein synthesis by being falsely incorporated into fungal RNA or interfere with the biosynthesis of fungal DNA through the inhibition of the enzyme thymidylate synthetase. Flucytosine has been shown to be active against most strains of Candida albicans and Cryptococcus neoformans. Flucytosine is indicated only in the treatment of serious infections caused by susceptible strains of Candida and/or Cryptococcus. prodrug (Code: CHEBI:50266) Nucleoside Analog (Code: N0000175459) Nucleoside Analog Antifungal (Code: N0000175467) Anti-Infective Agents (Code: D000890) Antifungal Agents (Code: D000935) Antimetabolites (Code: D000963) Noxae (Code: D009676) 1971-11-26 FDA 1LD
Click to view vigabatrin 4-aminobutyrate aminotransferase, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P80404, gene: ABAT, swissprot: GABT_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020427s020,022006s022lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inducer (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020427s020,022006s022lbl.pdf) Vigabatrin is a gamma-amino acid having a gamma-vinyl GABA structure.The precise mechanism of vigabatrin's anti-seizure effect is unknown, but it is believed to be the result of its action as an irreversible inhibitor of gamma-aminobutyric acid transaminase (GABA-T), the enzyme responsible for the metabolism of the inhibitory neurotransmitter GABA. This action results in increased levels of GABA in the central nervous system. Vigabatrin is indicated for the treatment of refractory complex partial seizures as adjunctive therapy and infantile spasms -monotherapy in infants 1 month to 2 years of age for whom the potential benefits outweigh the potential risk of vision loss. anticonvulsant (Code: CHEBI:35623) Anti-epileptic Agent (Code: N0000175753) Anticonvulsants (Code: D000927) Central Nervous System Agents (Code: D002491) Enzyme Inhibitors (Code: D004791) GABA Agents (Code: D018682) Neurotransmitter Agents (Code: D018377) 2009-08-21 FDA
Click to view metformin 5'-AMP-activated protein kinase subunit beta-1 (Organism: Homo sapiens, class: Kinase, accessions: Q9Y478, gene: PRKAB1, swissprot: AAKB1_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/14871885) Mitochondrial complex I (NADH dehydrogenase) (Organism: Homo sapiens, class: Enzyme, accessions: None, gene: None, swissprot: None) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22117616) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/23435786) Multidrug and toxin extrusion protein 1 (Organism: Homo sapiens, class: Transporter, accessions: Q96FL8, gene: SLC47A1, swissprot: S47A1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/23435786) Multidrug and toxin extrusion protein 2 (Organism: Homo sapiens, class: Transporter, accessions: Q86VL8, gene: SLC47A2, swissprot: S47A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/23435786) Dipeptidyl peptidase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P27487, gene: DPP4, swissprot: DPP4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15842525) Metformin is an antihyperglycemic agent which improves glucose tolerance in patients with type 2 diabetes mellitus, lowering both basal and postprandial plasma glucose. Metformin decreases hepatic glucose production, decreases intestinal absorption of glucose, and improves insulin sensitivity by increasing peripheral glucose uptake and utilization. With metformin therapy, insulin secretion remains unchanged while fasting insulin levels and day-long plasma insulin response may decrease. hypoglycemic agent (Code: CHEBI:35526) Biguanide (Code: N0000175565) Biguanides (Code: N0000007698) Hypoglycemic Agents (Code: D007004) 1995-03-03 FDA MF8
Click to view octodrine Octodrine is a stimulant that is structurally similar to amphetamine and is included in several so-called “pre-workout” and “fat-burning” supplements. Originally developed as a remedy to nasal congestion and as a possible anti-tumor drug, Octodrine has resurfaced as a key ingredient in dietary supplements for its stimulant and thermogenic benefits.
Click to view oxiniacic acid Oxiniacic acid is a nicotinic acid derivative and an antihyperlipidemic agent.
Click to view fluorouracil Solute carrier family 22 member 7 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y694, gene: SLC22A7, swissprot: S22A7_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15901346) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/18820913) Solute carrier family 22 member 8 (Organism: Mus musculus, class: Transporter, accessions: O88909, gene: Slc22a8, swissprot: S22A8_MOUSE) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15100168) Fluorouracil is an antimetabolite fluoropyrimidine analog of the nucleoside pyrimidine with antineoplastic activity. Fluorouracil and its metabolites possess a number of different mechanisms of action. In vivo, fluoruracil is converted to the active metabolite 5-fluoroxyuridine monophosphate (F-UMP); replacing uracil, F-UMP incorporates into RNA and inhibits RNA processing, thereby inhibiting cell growth. Another active metabolite, 5-5-fluoro-2'-deoxyuridine-5'-O-monophosphate (F-dUMP), inhibits thymidylate synthase, resulting in the depletion of thymidine triphosphate (TTP), one of the four nucleotide triphosphates used in the in vivo synthesis of DNA. Other fluorouracil metabolites incorporate into both RNA and DNA; incorporation into RNA results in major effects on both RNA processing and functions. Fluorouracil is used for the topical treatment of multiple actinic or solar keratoses, superficial basal cell carcinomas, for palliative management of some types of cancer, including colon, esophageal, gastric, rectum, breast, biliary tract, stomach, head and neck, cervical, pancreas, renal cell, and carcinoid. radiosensitizing agent (Code: CHEBI:132992) antineoplastic agent (Code: CHEBI:35610) immunosuppressive agent (Code: CHEBI:35705) Nucleic Acid Synthesis Inhibitors (Code: N0000000233) Nucleoside Metabolic Inhibitor (Code: N0000175595) Antimetabolites (Code: D000963) Antimetabolites, Antineoplastic (Code: D000964) Antineoplastic Agents (Code: D000970) Immunologic Factors (Code: D007155) Immunosuppressive Agents (Code: D007166) Noxae (Code: D009676) 1962-04-25 FDA URF
Click to view aminolevulinic acid Solute carrier family 15 member 1 (Organism: Homo sapiens, class: Transporter, accessions: P46059, gene: SLC15A1, swissprot: S15A1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/9637710) Solute carrier family 15 member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q16348, gene: SLC15A2, swissprot: S15A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/9637710) Aminolevulinic acid is a porphyrin precursor. Photoactivation following topical application occurs when aminolevulinic acid (prodrug) is metabolized to protoporphyrin IX (PpIX), a photoactive compound which accumulates in the skin. When exposed to red light of a suitable wavelength and energy, PpIX is activated resulting in an excited state of porphyrin molecules. In the presence of oxygen, reactive oxygen species are formed which causes damage to cellular components, and eventually destroys the cells. Aminolevulinic acid is indicated for the lesion-directed and field-directed treatment of actinic keratoses of mild-to-moderate severity on the face and scalp. antineoplastic agent (Code: CHEBI:35610) photosensitizing agent (Code: CHEBI:47868) dermatologic drug (Code: CHEBI:50177) prodrug (Code: CHEBI:50266) Porphyrin Precursor (Code: N0000175846) Porphyrinogens (Code: N0000171207) Dermatologic Agents (Code: D003879) Photosensitizing Agents (Code: D017319) Radiation-Sensitizing Agents (Code: D011838) 1999-12-03 FDA FVT
Click to view leucine Large neutral amino acids transporter small subunit 3 (Organism: Homo sapiens, class: Transporter, accessions: O75387, gene: SLC43A1, swissprot: LAT3_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12930836) Large neutral amino acids transporter small subunit 1 (Organism: Homo sapiens, class: Transporter, accessions: Q01650, gene: SLC7A5, swissprot: LAT1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12930836) Sodium-coupled neutral amino acid transporter 2 (Organism: Homo sapiens, class: Transporter, accessions: Q96QD8, gene: SLC38A2, swissprot: S38A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10930503) Sodium-coupled neutral amino acid transporter 4 (Organism: Homo sapiens, class: Transporter, accessions: Q969I6, gene: SLC38A4, swissprot: S38A4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11342143) Leucine is an alpha-amino acid used in the biosynthesis of proteins. Leucine is an essential hydrophobic amino acid. Leucine is an mTOR activator. It is a dietary amino acid with the capacity to directly stimulate muscle protein synthesis. As a dietary supplement, leucine has been found to slow the degradation of muscle tissue by increasing the synthesis of muscle proteins in aged rats. Long-term leucine supplementation does not increase muscle mass or strength in healthy elderly men. Leucine potently activates the mammalian target of rapamycin kinase that regulates cell growth. Infusion of leucine into the rat brain has been shown to decrease food intake and body weight via activation of the mTOR pathway. Leucine is also found in fish, meat, and poultry. In the pharmaceutical industry, L-leucine is used for parenteral and enteral nutrition and feeding, and is also used as a flavoring product and tablet lubricant in manufacturing. 1971-09-24 FDA LEU
DLE
Click to view aminocaproic acid Tissue-type plasminogen activator (Organism: Homo sapiens, class: Enzyme, accessions: P00750, gene: PLAT, swissprot: TPA_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2008/015197s043,015230s035lbl.pdf) Aminocaproic acid is an antifibrinolytic agent that acts by inhibiting plasminogen activators which have fibrinolytic properties. Aminocaproic acid is useful in enhancing hemostasis when fibrinolysis contributes to bleeding. antifibrinolytic drug (Code: CHEBI:48675) hematologic agent (Code: CHEBI:50248) Antifibrinolytic Agent (Code: N0000175634) Decreased Fibrinolysis (Code: N0000175632) Antifibrinolytic Agents (Code: D000933) Coagulants (Code: D003029) Fibrin Modulating Agents (Code: D050299) Hematologic Agents (Code: D006401) Hemostatics (Code: D006490) 1964-06-03 FDA ACA
Click to view paraldehyde Paraldehyde is a hypnotic and sedative with anticonvulsant effects. It is believed to depress many levels of the central nervous system (CNS), including the ascending reticular activating system to cause an imbalance between inhibitory and facilitatory mechanisms. In sub-hypnotic doses, paraldehyde has anticonvulsant actions, although the dose margin between the anticonvulsant and hypnotic effects is small. At sub-anaesthetic doses, it is not an analgesic and may produce excitement or delirium in the presence of pain. Paraldehyde has been used as a sedative and hypnotic in a variety of clinical situations, although it has been largely replaced by safer and/ or more effective agents. It may also be used in the treatment of convulsive episodes arising from tetanus, status epilepticus and poisoning by convulsive drugs, when other agents are inappropriate or ineffective. Paraldehyde may be effective in reducing the anxiety associated with withdrawal from drugs such as narcotics or barbiturates, as well as in the management of acute agitation or delirium tremens due to alcohol withdrawal. Paraldehyde is only recommended for use in these conditions when other treatments are ineffective or deemed inappropriate. sedative (Code: CHEBI:35717) Anticonvulsants (Code: D000927) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Hypnotics and Sedatives (Code: D006993) 2009-08-31 Therapeutic Goods Administration (TGA)
Click to view ornithine G-protein coupled receptor family C group 6 member A (Organism: Homo sapiens, class: GPCR, accessions: Q5T6X5, gene: GPRC6A, swissprot: GPC6A_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/15576628) Ornithine is a non-essential and nonprotein amino acid, ornithine is critical for the production of the body's proteins, enzymes and muscle tissue. Ornithine plays a central role in the urea cycle and is important for the disposal of excess nitrogen (ammonia). Ornithine is the starting point for the synthesis of many polyamines such as putrescine and spermine. Ornithine supplements are claimed to enhance the release of growth hormone and to burn excess body fat. Ornithine is necessary for proper immune function and good liver function. Ornithine is a naturally occurring amino acid found in meat, fish, dairy and eggs. Ornithine is also a precursor of citrulline and arginine. Ornithine is used for nutritional supplementation, also for treating dietary shortage or imbalance. It has been claimed that ornithine improves athletic performance, has anabolic effects, has wound-healing effects, and is immuno-enhancing. 1979-11-16 ANSM (French National Agency for Medicines and Health Products Safety) ORN
ORD
Click to view prenderol Prenderol ia an anticonvulsant drug and it has a depressant action on multisynaptic reflexes. Prenderol has been used as a drug to relieve anxiety in patients with mental disorders. It has also been used to treat absence crisis. anticonvulsant (Code: CHEBI:35623)
Click to view aspartic acid Glutamate NMDA receptor (Organism: Rattus norvegicus, class: Ion channel, accessions: P35439|Q00959|Q00960|Q00961|Q62645|Q9R1M7|Q8VHN2, gene: Grin1|Grin2a|Grin2b|Grin2c|Grin2d|Grin3a|Grin3b, swissprot: NMDZ1_RAT|NMDE1_RAT|NMDE2_RAT|NMDE3_RAT|NMDE4_RAT|NMD3A_RAT|NMD3B_RAT) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/15703381) Aspartate aminotransferase, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P00505, gene: GOT2, swissprot: AATM_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/26902786) Aspartic acid (aspartate) is a non-essential alpha-amino acid that is used in the biosynthesis of proteins. Aspartic acid acts as a neurotransmitter by stimulation of the NMDA receptors. In medicine, aspartic acid was studied as an activator of brain L-asparaginase to treat opiate abstinence syndrom. Supplements of aspartic acid was shown to improve condition of newborns with jaundice due to inhibition of beta-glucuronidase. L-aspartate is formed by the transamination of the Krebs cycle intermediate oxaloacetate. The amino acid serves as a precursor for synthesis of proteins, oligopeptides, purines, pyrimidines, nucleic acids and L-arginine. L-aspartate is a glycogenic amino acid, and it can also promote energy production via its metabolism in the Krebs cycle. These latter activities were the rationale for the claim that supplemental aspartate has an anti-fatigue effect on skeletal muscle, a claim that was never confirmed. FDA ASP
IAS
Click to view timonacic Timonacic (4-Thiazolidinecarboxylic acid) is the product of condensation between cysteine and formaldehyde. Dietary timonacic slows the aging process in mammals and prolongs their life span. It exerts antioxidant and antineoplastic actions however its mechanism of action is elusive. Timonacic is hydrolyzed in the licer to N-formyl-cysteine which contains the free -SH group. Timonacic is used for the treatment of liver diseases. hepatoprotective agent (Code: CHEBI:62868) antidote (Code: CHEBI:50247) 1993-05-24 Office for Registration of Medicinal Products, Medical Devices and Biocidal Products (Poland) PRS
Click to view tranylcypromine Amine oxidase [flavin-containing] B (Organism: Homo sapiens, class: Enzyme, accessions: P27338, gene: MAOB, swissprot: AOFB_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/012342s064lbl.pdf) Amine oxidase [flavin-containing] A (Organism: Homo sapiens, class: Enzyme, accessions: P21397, gene: MAOA, swissprot: AOFA_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/012342s064lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15049511) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15049511) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15049511) Cytochrome P450 2A6 (Organism: Homo sapiens, class: Enzyme, accessions: P11509, gene: CYP2A6, swissprot: CP2A6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11181487) Cytochrome P450 2E1 (Organism: Homo sapiens, class: Enzyme, accessions: P05181, gene: CYP2E1, swissprot: CP2E1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11181487) Tranylcypromine is a nonhydrazine monamine oxidase inhibitor. The mechanism of action of tranylcypromine as an antidepressant is not fully understood, but is presumed to be linked to potentiation of monoamine neurotransmitter activity in the central nervous system. Tranylcypromine is indicated for the treatment of major depressive disorder. antidepressant (Code: CHEBI:35469) anxiolytic drug (Code: CHEBI:35474) Monoamine Oxidase Inhibitor (Code: N0000175744) Anti-Anxiety Agents (Code: D014151) Antidepressive Agents (Code: D000928) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Enzyme Inhibitors (Code: D004791) Monoamine Oxidase Inhibitors (Code: D008996) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149) 1961-02-21 FDA GJZ
Click to view adenine Xanthine dehydrogenase/oxidase (Organism: Homo sapiens, class: Enzyme, accessions: P47989, gene: XDH, swissprot: XDH_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17379526) Adenine is a purine base. Adenine is found in both DNA and RNA. Adenine is a fundamental component of adenine nucleotides. Adenine forms adenosine, a nucleoside, when attached to ribose, and deoxyadenosine when attached to deoxyribose; it forms adenosine triphosphate (ATP), a nucleotide, when three phosphate groups are added to adenosine. Adenosine triphosphate is used in cellular metabolism as one of the basic methods of transferring chemical energy between chemical reactions. Adenine is used for nutritional supplementation, also for treating dietary shortage or imbalance. 1980-06-11 FDA ADE
Click to view acetanilide Acetanilide is a fever-reducing drug. Acetanilide exhibited an unacceptable profile of toxic effects, the most alarming being cyanosis due to methemoglobinemia. Acetanilide is no longer used as a drug in its own right, although its primary metabolite, paracetamol, has been widely succesful. analgesic (Code: CHEBI:35480)
Click to view amfetamine Sodium-dependent dopamine transporter (Organism: Homo sapiens, class: Transporter, accessions: Q01959, gene: SLC6A3, swissprot: SC6A3_HUMAN) inhibitor (Source: https://pdf.hres.ca/dpd_pm/00043799.PDF) Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) inhibitor (Source: https://pdf.hres.ca/dpd_pm/00043799.PDF) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://pdf.hres.ca/dpd_pm/00043799.PDF) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://pdf.hres.ca/dpd_pm/00043799.PDF) Carbonic anhydrase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P22748, gene: CA4, swissprot: CAH4_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/28936885) Carbonic anhydrase 7 (Organism: Homo sapiens, class: Enzyme, accessions: P43166, gene: CA7, swissprot: CAH7_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/28936885) Carbonic anhydrase 12 (Organism: Homo sapiens, class: Enzyme, accessions: O43570, gene: CA12, swissprot: CAH12_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/28936885) Carbonic anhydrase 14 (Organism: Homo sapiens, class: Enzyme, accessions: Q9ULX7, gene: CA14, swissprot: CAH14_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/28936885) Carbonic anhydrase 5A, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P35218, gene: CA5A, swissprot: CAH5A_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/28936885) Carbonic anhydrase 5B, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: Q9Y2D0, gene: CA5B, swissprot: CAH5B_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/28936885) Solute carrier family 22 member 3 (Organism: Homo sapiens, class: Transporter, accessions: O75751, gene: SLC22A3, swissprot: S22A3_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/9830022) Solute carrier family 22 member 5 (Organism: Homo sapiens, class: Transporter, accessions: O76082, gene: SLC22A5, swissprot: S22A5_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/9618255) Trace amine-associated receptor 1 (Organism: Homo sapiens, class: GPCR, accessions: Q96RJ0, gene: TAAR1, swissprot: TAAR1_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/22037049) Amphetamine is a powerful central nervous system stimulant and sympathomimetic. Amphetamine has multiple mechanisms of action including blocking uptake of adrenergics and dopamine, stimulation of release of monamines, and inhibiting monoamine oxidase. Amphetamine is also a drug of abuse and a psychotomimetic. The l-form (levamfetamine) has less central nervous system activity but stronger cardiovascular effects. L-Amphetamine succinate was sold between 1952 and 1955 under the brand name Cydril. Amphetamine is used in the treatment of attention deficit hyperactivity disorder (ADHD), narcolepsy, and obesity. Amphetamine is one of the more restricted controlled drugs. sympathomimetic agent (Code: CHEBI:35524) dopaminergic agent (Code: CHEBI:48560) adrenergic agent (Code: CHEBI:37962) dopamine uptake inhibitor (Code: CHEBI:51039) adrenergic uptake inhibitor (Code: CHEBI:35640) bronchodilator agent (Code: CHEBI:35523) Central Nervous System Stimulant (Code: N0000175739) Central Nervous System Stimulation (Code: N0000175729) Adrenergic Agents (Code: D018663) Adrenergic Uptake Inhibitors (Code: D018759) Autonomic Agents (Code: D001337) Central Nervous System Agents (Code: D002491) Central Nervous System Stimulants (Code: D000697) Dopamine Agents (Code: D015259) Dopamine Uptake Inhibitors (Code: D018765) Membrane Transport Modulators (Code: D049990) Neurotransmitter Agents (Code: D018377) Neurotransmitter Uptake Inhibitors (Code: D014179) Peripheral Nervous System Agents (Code: D018373) Sympathomimetics (Code: D013566) 1955-09-09 FDA FRD
1WE
Click to view allopurinol Xanthine dehydrogenase/oxidase (Organism: Homo sapiens, class: Enzyme, accessions: P47989, gene: XDH, swissprot: XDH_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/016084s044lbl.pdf) Solute carrier family 22 member 8 (Organism: Mus musculus, class: Transporter, accessions: O88909, gene: Slc22a8, swissprot: S22A8_MOUSE) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15100168) Solute carrier family 22 member 7 (Organism: Mus musculus, class: Transporter, accessions: Q91WU2, gene: Slc22a7, swissprot: S22A7_MOUSE) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12065749) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/29342419) Allopurinol is a structural analogue of the natural purine base, hypoxanthine. It is an inhibitor of xanthine oxidase, the enzyme responsible for the conversion of hypoxanthine to xanthine and of xanthine to uric acid, the end product of purine metabolism in man. Allopurinol is metabolized to the corresponding xanthine analogue, oxipurinol (alloxanthine), which also is an inhibitor of xanthine oxidase. Allopurinol is indicated in the management of patients with signs and symptoms of primary or secondary gout (acute attacks, tophi, joint destruction, uric acid lithiasis, and/or nephropathy), in the management of patients with leukemia, lymphoma and malignancies who are receiving cancer therapy which causes elevations of serum and urinary uric acid levels and in the management of patients with recurrent calcium oxalate calculi. gout suppressant (Code: CHEBI:35845) Antimetabolites (Code: D000963) Antioxidants (Code: D000975) Antirheumatic Agents (Code: D018501) Enzyme Inhibitors (Code: D004791) Free Radical Scavengers (Code: D016166) Gout Suppressants (Code: D006074) Noxae (Code: D009676) Xanthine Oxidase Inhibitor (Code: N0000175698) Xanthine Oxidase Inhibitors (Code: N0000000206) 1966-08-19 FDA
Click to view pentaerythritol Pentaerythritol is a white crystalline polyhydric alcohol containing four primary hydroxyl groups. Pentaerythritol causes hyperhydration of the intestinal contents. Pentaerythritol is osmotically acting laxatives. It was used for treatment of constipation. 1991-07-01 ANSM (French National Agency for Medicines and Health Products Safety) 3SY
Click to view phenylpropanol Phenylpropanol (1-phenyl-1-propanol) is a choleretic agent.
Click to view phenelzine Amine oxidase [flavin-containing] B (Organism: Homo sapiens, class: Enzyme, accessions: P27338, gene: MAOB, swissprot: AOFB_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/020682s010lbl.pdf) Amine oxidase [flavin-containing] A (Organism: Homo sapiens, class: Enzyme, accessions: P21397, gene: MAOA, swissprot: AOFA_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/020682s010lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16669850) Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16669850) Membrane primary amine oxidase (Organism: Homo sapiens, class: Enzyme, accessions: Q16853, gene: AOC3, swissprot: AOC3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20690686) Phenelzine is a hydrazine derivative. Phenelzine is a potent inhibitor of monoamine oxidase by phenelzine relieves depressive symptoms by causing an increase in the levels of serotonin, norepinephrine, and dopamine in the neuron. Phenelzine is used in depressed patients clinically characterized as “atypical,” “nonendogenous,” or “neurotic.” These patients often have mixed anxiety and depression and phobic or hypochondriacal features. Monoamine Oxidase Inhibitor (Code: N0000175744) Antidepressive Agents (Code: D000928) Central Nervous System Agents (Code: D002491) Enzyme Inhibitors (Code: D004791) Monoamine Oxidase Inhibitors (Code: D008996) Psychotropic Drugs (Code: D011619) 1961-06-09 FDA
Click to view betahistine Histamine H3 receptor (Organism: Homo sapiens, class: GPCR, accessions: Q9Y5N1, gene: HRH3, swissprot: HRH3_HUMAN) antagonist (Source: https://pdf.hres.ca/dpd_pm/00045254.PDF) Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) partial agonist (Source: https://pdf.hres.ca/dpd_pm/00045254.PDF) Amine oxidase [flavin-containing] A (Organism: Homo sapiens, class: Enzyme, accessions: P21397, gene: MAOA, swissprot: AOFA_HUMAN) substrate (Source: https://pdf.hres.ca/dpd_pm/00045254.PDF) Amine oxidase [flavin-containing] B (Organism: Homo sapiens, class: Enzyme, accessions: P27338, gene: MAOB, swissprot: AOFB_HUMAN) substrate (Source: https://pdf.hres.ca/dpd_pm/00045254.PDF) Betahistine is is an antivertigo drug first used for treating vertigo assosicated with Meniere's disease. It is also commonly used for patients with balance disorders. Betahistine primarily acts as a histamine H1-agonist with 0. 07 times the activity of histamine. Stimulating the H1-receptors in the inner ear causes a vasodilatory effect and increased permeability in the blood vessels which results in reduced endolymphatic pressure. Betahistine is believed to act by reducing the asymmetrical functioning of sensory vestibular organs as well as by increasing vestibulocochlear blood flow. Doing so aids in decreasing symptoms of vertigo and balance disorders. Betahistine also acts as a histamine H3-receptor antagonist which causes an increased output of histamine from histaminergic nerve endings which can further increase the direct H1-agonist activity. Furthermore, H3-receptor antagonism increases the levels of neurotransmitters such as serotonin in the brainstem, which inhibits the activity of vestibular nuclei, helping to restore proper balance and decrease in vertigo symptoms. H1-receptor agonist (Code: CHEBI:71173) vasodilator agent (Code: CHEBI:35620) Cardiovascular Agents (Code: D002317) Histamine Agents (Code: D018494) Histamine Agonists (Code: D017442) Neurotransmitter Agents (Code: D018377) Vasodilator Agents (Code: D014665) 1970-06-08 Ministry of Health, Welfare and Sport (Netherlands)
Click to view isopromethazine Isopromethazine is an impurity of promethazine, an antihistamine used as an central nervous system depressant.
Click to view homonicotinic acid Hydroxycarboxylic acid receptor 2 (Organism: Homo sapiens, class: GPCR, accessions: Q8TDS4, gene: HCAR2, swissprot: HCAR2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12522134) Homonicotinic acid is a breakdown product of nicotine (and other tobacco alkaloids). Homonicotinic acid acid is an analog of nicotinic acid and used as a hypolipidemic agent. Italian Medicines Agency (AIFA)
Click to view bethanechol Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9224827) Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9224827) Muscarinic acetylcholine receptor M4 (Organism: Homo sapiens, class: GPCR, accessions: P08173, gene: CHRM4, swissprot: ACM4_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9224827) Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9224827) Bethanechol is a synthetic cholinergic agent with is structurally and pharmacologically related to acetylcholine. Bethanechol is a slowly hydrolysed muscarinic agonist with no nicotinic effects, it is used as its chloride salt to increase smooth muscle tone, as in the gastrointestinal tract following abdominal surgery, treatment of gastro-oesophageal reflux disease, and as an alternative to catheterisation in the treatment of non-obstructive urinary retention. muscarinic agonist (Code: CHEBI:38325) Cholinergic Muscarinic Agonist (Code: N0000175840) Cholinergic Muscarinic Agonists (Code: N0000000104) Autonomic Agents (Code: D001337) Cholinergic Agents (Code: D018678) Cholinergic Agonists (Code: D018679) Muscarinic Agonists (Code: D018721) Neurotransmitter Agents (Code: D018377) Parasympathomimetics (Code: D010277) Peripheral Nervous System Agents (Code: D018373) 1948-10-12 FDA
Click to view methyl nicotinate Methyl nicotinate is the methyl ester of niacin. Methyl nicotinate is present in guava fruit, papaya, strawberry, soursop (Annona muricata), beer, grape brandy, coffee, roasted filbert, roasted peanut and Bourbon vanill. The action of methyl nicotinate as a rubefacient is thought to involve peripheral vasodilation. Methyl nicotinate is used in combination with other drugs for the symptomatic treatment of muscle stiffness, muscular rheumatism, lumbago, sciatica, fibrositis, sprains and chilblains. 1983-12-29 UK Medicines and Healthcare Products Regulatory Agency (MHRA)
Click to view salicylamide Salicylamide is a non-prescription drug with analgesic and antipyretic properties. It has similar medicinal uses to aspirin. Salicylamide blocks cyclooxygenase, breaks the metabolism of arachidonic acid, reduces the amount of prostaglandins both in the inflammation focus and in healthy tissues, suppresses the exudative and proliferative phase of inflammation. Reduces the permeability of capillaries; stabilizes the lysosomal membranes; inhibits the production of macroergers (primarily ATP) in the processes of oxidative phosphorylation; inhibits synthesis or inactivates mediators of inflammation, incl. histamine, bradykinin, lymphokines, complement factor and other nonspecific endogenous "damaging factors". It blocks the interaction of bradykinin with tissue receptors, restores disturbed microcirculation and reduces pain sensitivity in the inflammatory focus. Salicylamide is used in combination with both aspirin and caffeine in the over-the-counter pain remedies. non-narcotic analgesic (Code: CHEBI:35481) antirheumatic drug (Code: CHEBI:35842) Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1964-04-30 Ministry of Health of the Russian Federation OHB
Click to view aminobenzoic acid Acetylcholinesterase (Organism: Homo sapiens, class: Enzyme, accessions: P22303, gene: ACHE, swissprot: ACES_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22172310) Carbonic anhydrase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P00915, gene: CA1, swissprot: CAH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21402476) Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21402476) Carbonic anhydrase (Organism: Candida albicans (strain SC5314 / ATCC MYA-2876), class: Enzyme, accessions: Q5AJ71, gene: NCE103, swissprot: CAN_CANAL) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21402476) Aminobenzoic acid is an intermediate in the synthesis of folate by bacteria, plants, and fungi. Many bacteria, including those found in the human intestinal tract such as E. coli, generate Aminobenzoic acid from chorismate by the combined action of the enzymes 4-amino-4-deoxychorismate synthase and 4-amino-4-deoxychorismate lyase. Plants produce Aminobenzoic acid in their chloroplasts, and store it as a glucose ester (pABA-Glc) in their tissues. Humans lack the enzymes to convert Aminobenzoic acid to folate, so require folate from dietary sources such as green leafy vegetables. In humans, Aminobenzoic acid is considered nonessential and, although it has been referred to historically as "vitamin Bx", is no longer recognized as a vitamin, because most people have colon bacteria that generate Aminobenzoic acid. It used to be common in sunscreening agents until found to also be a sensitizer. The potassium salt is used therapeutically in fibrotic skin disorders. Vitamin B Complex Compounds (Code: N0000175715) Vitamin B Complex Member (Code: N0000175714) 1987-02-26 ANSM (French National Agency for Medicines and Health Products Safety) PAB
Click to view isoniazid Myeloperoxidase (Organism: Homo sapiens, class: Enzyme, accessions: P05164, gene: MPO, swissprot: PERM_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/28197313) Enoyl-[acyl-carrier-protein] reductase [NADH] (Organism: Mycobacterium tuberculosis (strain ATCC 25618 / H37Rv), class: Enzyme, accessions: P9WGR1, gene: inhA, swissprot: INHA_MYCTU) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15908576) Antibacterial agent used primarily as a tuberculostatic, inhibits the synthesis of mycoloic acids, an essential component of the bacterial cell wall. It remains the treatment of choice for tuberculosis. drug allergen (Code: CHEBI:88188) antitubercular agent (Code: CHEBI:33231) Antimycobacterial (Code: N0000175483) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Antimetabolites (Code: D000963) Antitubercular Agents (Code: D000995) Fatty Acid Synthesis Inhibitors (Code: D054872) Hypolipidemic Agents (Code: D000960) 1952-09-29 FDA NIZ
Click to view dimetofrine proposed cardiovascular stimulant; minor descriptor (75-85); on-line & Index Medicus search ETHANOLAMINES (75-85); RN given refers to parent cpd without isomeric designation
Click to view pralidoxime Acetylcholinesterase (Organism: Homo sapiens, class: Enzyme, accessions: P22303, gene: ACHE, swissprot: ACES_HUMAN) activator (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021983s023lbl.pdf) Cholinesterase (Organism: Homo sapiens, class: Enzyme, accessions: P06276, gene: BCHE, swissprot: CHLE_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/24571195) Pralidoxime is an antidote to organophosphate pesticides and chemicals. If given within 24 hours, after organophosphate exposure, pralidoxime reactivates the enzyme cholinesterase by cleaving the phosphate-ester bond formed between the organophosphate and acetylcholinesterase. Pralidoxime in combination with atropine or alone is indicated for the treatment of poisoning by organophosphorus nerve agents as well as organophosphorus insecticides. cholinergic drug (Code: CHEBI:38323) antidote to organophosphate poisoning (Code: CHEBI:90753) antidote to sarin poisoning (Code: CHEBI:136860) Cholinesterase Reactivator (Code: N0000175742) Antidotes (Code: D000931) Cholinergic Agents (Code: D018678) Cholinesterase Reactivators (Code: D002801) Enzyme Reactivators (Code: D004793) Neurotransmitter Agents (Code: D018377) Protective Agents (Code: D020011) 1964-03-11 FDA
Click to view phenylethanolamine Phenylethanolamine is the simplest member of the class of phenylethanolamines that is 2-aminoethanol bearing a phenyl substituent at the 1-position. It has a role as a human metabolite in the brain. Its derivatives are adrenergic agonists and antagonists. It can be used as a modulator of sympathetic functions.
Click to view tyramine Trace amine-associated receptor 1 (Organism: Homo sapiens, class: GPCR, accessions: Q96RJ0, gene: TAAR1, swissprot: TAAR1_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/18602830) Equilibrative nucleoside transporter 4 (Organism: Homo sapiens, class: Transporter, accessions: Q7RTT9, gene: SLC29A4, swissprot: S29A4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/16099839) Tyramine is a monoamine compound derived from the amino acid tyrosine. Foods containing considerable amounts of tyramine include fish, chocolate, alcoholic beverages, cheese, soy sauce, sauerkraut, and processed meat. A large dietary intake of tyramine can cause an increase in systolic blood pressure of 30 mmHg or more. Tyramine acts as a neurotransmitter via a G protein-coupled receptor with high affinity for tyramine called TA1. The TA1 receptor is found in the brain as well as peripheral tissues including the kidney. An indirect sympathomimetic, Tyramine can also serve as a substrate for adrenergic uptake systems and monoamine oxidase so it prolongs the actions of adrenergic transmitters. It also provokes transmitter release from adrenergic terminals. Tyramine is a biomarker for the consumption of cheese. Adrenergic Agents (Code: D018663) Adrenergic Uptake Inhibitors (Code: D018759) Autonomic Agents (Code: D001337) Membrane Transport Modulators (Code: D049990) Neurotransmitter Agents (Code: D018377) Neurotransmitter Uptake Inhibitors (Code: D014179) Peripheral Nervous System Agents (Code: D018373) Sympathomimetics (Code: D013566) AEF
Click to view isaxonine Isaxonine (isopropyl-amino-2-pyrimidinephosphate) is a neurotropic agent. Isaxonine is believed to have a positive effect on nerve regeneration by increasing the axonal transport, enhancing polymerization of tubuline in the peripheral nerves and stimulating axonal sprouting. Isaxonine is activated cytochromes P-450 into a reactive metabolite that is conjugated with glutathione or covalently binds to hepatic proteins. Isaxonine was used for the treatment of peripheral neuropathie. Also isaxonine was used for protection against the neurotoxic side-effect of vincristine. It is no longer commercially available due to its severe hepatotoxicity. 1981 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view fosfomycin UDP-N-acetylglucosamine 1-carboxyvinyltransferase 1 (Organism: Enterococcus faecalis (strain ATCC 700802 / V583), class: Enzyme, accessions: Q836E5, gene: murA1, swissprot: MURA1_ENTFA) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/050717s009lbl.pdf) UDP-N-acetylglucosamine 1-carboxyvinyltransferase 2 (Organism: Enterococcus faecalis (strain ATCC 700802 / V583), class: Enzyme, accessions: Q831A8, gene: murA2, swissprot: MURA2_ENTFA) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/050717s009lbl.pdf) UDP-N-acetylglucosamine 1-carboxyvinyltransferase (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P0A749, gene: murA, swissprot: MURA_ECOLI) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/050717s009lbl.pdf) UDP-N-acetylglucosamine 1-carboxyvinyltransferase (Organism: Pseudomonas aeruginosa (strain ATCC 15692 / PAO1 / 1C / PRS 101 / LMG 12228), class: Unclassified, accessions: Q9HVW7, gene: murA, swissprot: MURA_PSEAE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16945528) Fosfomycin is an antibiotic produced by Streptomyces fradiae. Fosfomycin has in vitro activity against a broad range of gram-positive and gram-negative aerobic microorganisms which are associated with uncomplicated urinary tract infections. Fosfomycin is bactericidal in urine at therapeutic doses. The bactericidal action of fosfomycin is due to its inactivation of the enzyme enolpyruvyl transferase, thereby irreversibly blocking the condensation of uridine diphosphate-N-acetylglucosamine with p-enolpyruvate, one of the first steps in bacterial cell wall synthesis. It also reduces adherence of bacteria to uroepithelial cells. There is generally no cross-resistance between fosfomycin and other classes of antibacterial agents such as beta-lactams and aminoglycosides. Fosfomycin has been shown to be active in clinical infections against Enterococcus faecalis and Escherichia coli. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) 1996-12-19 FDA FCN
Click to view salicylic acid High mobility group protein B1 (Organism: Homo sapiens, class: Unclassified protein, accessions: P09429, gene: HMGB1, swissprot: HMGB1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/26101955) Aldo-keto reductase family 1 member C1 (Organism: Homo sapiens, class: Enzyme, accessions: Q04828, gene: AKR1C1, swissprot: AK1C1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18045204) Solute carrier family 22 member 6 (Organism: Homo sapiens, class: Transporter, accessions: Q4U2R8, gene: SLC22A6, swissprot: S22A6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10049739) Solute carrier family 22 member 19 (Organism: Mus musculus, class: Transporter, accessions: Q8VCA0, gene: Slc22a19, swissprot: S22AJ_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15068970) Solute carrier family 22 member 8 (Organism: Homo sapiens, class: Transporter, accessions: Q8TCC7, gene: SLC22A8, swissprot: S22A8_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11306713) Monocarboxylate transporter 1 (Organism: Rattus norvegicus, class: Transporter, accessions: P53987, gene: Slc16a1, swissprot: MOT1_RAT) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10579682) Solute carrier organic anion transporter family member 2B1 (Organism: Homo sapiens, class: Transporter, accessions: O94956, gene: SLCO2B1, swissprot: SO2B1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15640378) Solute carrier family 22 member 7 (Organism: Mus musculus, class: Transporter, accessions: Q91WU2, gene: Slc22a7, swissprot: S22A7_MOUSE) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12065749) Carbonic anhydrase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P22748, gene: CA4, swissprot: CAH4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18579385) Carbonic anhydrase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P00915, gene: CA1, swissprot: CAH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18579385) Carbonic anhydrase 12 (Organism: Homo sapiens, class: Enzyme, accessions: O43570, gene: CA12, swissprot: CAH12_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18579385) Carbonic anhydrase 6 (Organism: Homo sapiens, class: Enzyme, accessions: P23280, gene: CA6, swissprot: CAH6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18579385) Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18579385) Solute carrier family 22 member 20 (Organism: Mus musculus, class: Transporter, accessions: Q80UJ1, gene: Slc22a20, swissprot: S22AK_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17553798) Solute carrier family 22 member 6 (Organism: Mus musculus, class: Transporter, accessions: Q8VC69, gene: Slc22a6, swissprot: S22A6_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17553798) Salicylic acid is a compound obtained from the bark of the white willow and wintergreen leaves, and also prepared synthetically. It has bacteriostatic, fungicidal, and keratolytic actions. Its salts, the salicylates, are used as analgesics. Salicylic acid directly irreversibly inhibits COX-1 and COX-2 to decrease conversion of arachidonic acid to precursors of prostaglandins and thromboxanes. Salicylic acid competitively inhibits oxidation of uridine-5-diphosphoglucose (UDPG) with nicotinamide adenosine dinucleotide (NAD) and noncompetitively with UDPG. It also competitively inhibits the transferring of the glucuronyl group of uridine-5-phosphoglucuronic acid (UDPGA) to a phenolic acceptor. Inhibition of mucopoly saccharide synthesis is likely responsible for the slowing of wound healing with salicylates. Salicylic acid is a key additive in many skin-care products for the treatment of acne, psoriasis, callouses, corns, keratosis pilaris and warts. antiinfective agent (Code: CHEBI:35441) keratolytic drug (Code: CHEBI:50176) Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Infective Agents (Code: D000890) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antifungal Agents (Code: D000935) Antirheumatic Agents (Code: D018501) Cyclooxygenase Inhibitors (Code: D016861) Dermatologic Agents (Code: D003879) Enzyme Inhibitors (Code: D004791) Keratolytic Agents (Code: D007641) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1898-01-01 YEAR INTRODUCED SAL
Click to view phenoxyethanol Phenoxyethanol is a glycol ether used as a insect repellent, antiseptic, solvent, preservative, and also as an anesthetic in fish aquaculture. Phenoxyethanol is used as an antimicrobial and preservative. Also it is used in vaccines and shown to inactivate bacteria, and several types of yeast. antiinfective agent (Code: CHEBI:35441) central nervous system depressant (Code: CHEBI:35488) Anesthetics (Code: D000777) Anti-Infective Agents (Code: D000890) Anti-Infective Agents, Local (Code: D000891) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) FDA 268
Click to view pentetrazol GABA-A receptor alpha-1/beta-2/gamma-2 (Organism: Homo sapiens, class: Ion channel, accessions: P14867|P47870|P18507, gene: GABRA1|GABRB2|GABRG2, swissprot: GBRA1_HUMAN|GBRB2_HUMAN|GBRG2_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/11504794) Pentetrazol is a pharmaceutical agent that displays activity as a central nervous system and respiratory stimulant. It is considered a non-competitive gamma-aminobutyric acid (GABA) antagonist. Pentetrazol has been used experimentally to study seizure phenomenon and to identify pharmaceuticals that may control seizure susceptibility. GABA is thought to play a role in promoting sleep and its function is believed to be elevated in idiopathic hypersomnia. By blocking GABA’s function, pentetrazo is expected to reduce excessive daytime sleepiness. Pentetrazole in combination with dihydrocodeine rhodanate is used as cough suppressant. Central Nervous System Agents (Code: D002491) Central Nervous System Stimulants (Code: D000697) Convulsants (Code: D003292) GABA Agents (Code: D018682) GABA Antagonists (Code: D018756) Neurotransmitter Agents (Code: D018377) 1969-08-12 Italian Medicines Agency (AIFA)
Click to view methazolamide Carbonic anhydrase 5A, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P35218, gene: CA5A, swissprot: CAH5A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18167490) Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18167490) Carbonic anhydrase 14 (Organism: Homo sapiens, class: Enzyme, accessions: Q9ULX7, gene: CA14, swissprot: CAH14_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18167490) Carbonic anhydrase 7 (Organism: Homo sapiens, class: Enzyme, accessions: P43166, gene: CA7, swissprot: CAH7_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18167490) Carbonic anhydrase 13 (Organism: Mus musculus, class: Enzyme, accessions: Q9D6N1, gene: Ca13, swissprot: CAH13_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18167490) Carbonic anhydrase 12 (Organism: Homo sapiens, class: Enzyme, accessions: O43570, gene: CA12, swissprot: CAH12_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18167490) Carbonic anhydrase 9 (Organism: Homo sapiens, class: Enzyme, accessions: Q16790, gene: CA9, swissprot: CAH9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18167490) Carbonic anhydrase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P22748, gene: CA4, swissprot: CAH4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18167490) Carbonic anhydrase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P00915, gene: CA1, swissprot: CAH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18167490) Carbonic anhydrase 5B, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: Q9Y2D0, gene: CA5B, swissprot: CAH5B_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18167490) Carbonic anhydrase 3 (Organism: Homo sapiens, class: Enzyme, accessions: P07451, gene: CA3, swissprot: CAH3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18167490) Carbonic anhydrase 6 (Organism: Homo sapiens, class: Enzyme, accessions: P23280, gene: CA6, swissprot: CAH6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18167490) Solute carrier family 22 member 6 (Organism: Rattus norvegicus, class: Transporter, accessions: O35956, gene: Slc22a6, swissprot: S22A6_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10991988) Carbonic anhydrase 13 (Organism: Homo sapiens, class: Enzyme, accessions: Q8N1Q1, gene: CA13, swissprot: CAH13_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21620713) Carbonic anhydrase 2 (Organism: Cryptococcus neoformans var. grubii, class: Unclassified, accessions: Q3I4V7, gene: CAN2, swissprot: Q3I4V7_CRYNV) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19450983) Carbonic anhydrase (Organism: Candida albicans (strain SC5314 / ATCC MYA-2876), class: Enzyme, accessions: Q5AJ71, gene: NCE103, swissprot: CAN_CANAL) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19450983) Carbonic anhydrase (Organism: Methanosarcina thermophila, class: Enzyme, accessions: P40881, gene: None, swissprot: CAH_METTE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15546717) Carbonic anhydrase 2 (Organism: Mycobacterium tuberculosis (strain ATCC 25618 / H37Rv), class: Enzyme, accessions: P9WPJ9, gene: mtcA2, swissprot: MTCA2_MYCTU) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19846301) Beta-carbonic anhydrase 1 (Organism: Mycobacterium tuberculosis (strain ATCC 25618 / H37Rv), class: Enzyme, accessions: P9WPJ7, gene: mtcA1, swissprot: MTCA1_MYCTU) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19450983) Methazolamide is a sulfonamide derivative and a potent inhibitor of the enzyme carbonic anhydrase. The oral administration of the drug inhibits ocular carbonic anhydrase therefore decreasing formation of aqueous humor and intraocular pressure. Methazolamide does have a weak transient diuretic effect. Methazolamide is indicated for adjunctive treatment of chronic simple (open-angle) glaucoma, secondary glaucoma and preoperatively in acute angle closure glaucoma, where delay of surgery is desired in order to lower intraocular pressure. Carbonic Anhydrase Inhibitors (Code: D002257) Diuretics (Code: D004232) Enzyme Inhibitors (Code: D004791) Natriuretic Agents (Code: D045283) 1959-01-26 FDA MZM
Click to view irofulven Serine/threonine-protein kinase Chk2 (Organism: Homo sapiens, class: Kinase, accessions: O96017, gene: CHEK2, swissprot: CHK2_HUMAN) Irofulven is a semisynthetic sesquiterpene derivative of illudin S, a natural toxin isolated from the fungus Omphalotus illudens. Irofulven alkylates DNA and protein macromolecules, forms adducts, and arrests cells in the S-phase of the cell cycle. This agent requires NADPH-dependent metabolism by alkenal/one oxidoreductase for activity. Irofulven is more active in vitro against tumor cells of epithelial origin and is more resistant to deactivation by p53 loss and MDR1 than other alkylating agents. Alkylating Agents (Code: D000477) Antineoplastic Agents (Code: D000970) Antineoplastic Agents, Alkylating (Code: D018906) Noxae (Code: D009676) Radiation-Sensitizing Agents (Code: D011838)
Click to view methenamine Methenamine is a heterocyclic organic compound with antibiotic activity. Methenamine most commonly used in the treatment of urinary tract infections. Its anti-infective action derives from the slow release of formaldehyde by hydrolysis at acidic pH. (From Martindale, The Extra Pharmacopoeia, 30th ed, p173) Anti-Infective Agents (Code: D000890) Anti-Infective Agents, Urinary (Code: D000892) Renal Agents (Code: D012076) 1967-07-05 FDA
Click to view furtrethonium Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9224827) Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9224827) Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9224827) Muscarinic acetylcholine receptor M4 (Organism: Homo sapiens, class: GPCR, accessions: P08173, gene: CHRM4, swissprot: ACM4_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9224827) Furtrethonium is an cholinergic agent. Furtrethonium iodide is used for the treatment of glaucoma. Cholinergic Agents (Code: D018678) Cholinergic Agonists (Code: D018679) Neurotransmitter Agents (Code: D018377)
Click to view ethosuximide Voltage-dependent T-type calcium channel subunit alpha-1G (Organism: Homo sapiens, class: Ion channel, accessions: O43497, gene: CACNA1G, swissprot: CAC1G_HUMAN) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/11641441) Voltage-dependent T-type calcium channel subunit alpha-1H (Organism: Homo sapiens, class: Ion channel, accessions: O95180, gene: CACNA1H, swissprot: CAC1H_HUMAN) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/11641441) Voltage-dependent T-type calcium channel subunit alpha-1I (Organism: Homo sapiens, class: Ion channel, accessions: Q9P0X4, gene: CACNA1I, swissprot: CAC1I_HUMAN) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/11641441) Cytochrome P450 2E1 (Organism: Homo sapiens, class: Enzyme, accessions: P05181, gene: CYP2E1, swissprot: CP2E1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12637244) Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12637244) Ethosuximide is a succinimide anticonvulsant. Ethosuximide suppresses the paroxysmal three cycle per second spike and wave activity associated with lapses of consciousness which is common in absence (petit mal) seizures. The frequency of epileptiform attacks is reduced, apparently by depression of the motor cortex and elevation of the threshold of the central nervous system to convulsive stimuli. Ethosuximide is on the World Health Organization's List of Essential Medicines. Ethosuximide is indicated for the control of absence (petit mal) epilepsy. anticonvulsant (Code: CHEBI:35623) Anti-epileptic Agent (Code: N0000175753) Decreased Central Nervous System Disorganized Electrical Activity (Code: N0000008486) Anticonvulsants (Code: D000927) Central Nervous System Agents (Code: D002491) 1960-11-02 FDA
Click to view isometheptene Isometheptene is a sympathomimetic drug which causes vasoconstriction. Isometheptene's vasoconstricting properties arise through activation of the sympathetic nervous system via epinephrine and norepinephrine. It is used for treating migraines and tension headaches. FDA
Click to view cyclopentamine Cyclopentamine is a sympathomimetic alkylamine, classified as a vasoconstrictor. Cyclopentamine acts as a releasing agent of the catecholamine neurotransmitters norepinephrine (noradrenaline), epinephrine (adrenaline), and dopamine. Cyclopentamine was indicated in the past as a nasal decongestant, but has now been largely discontinued.
Click to view metyrapone Cytochrome P450 11B1, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P15538, gene: CYP11B1, swissprot: C11B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25874338) Cytochrome P450 11B2, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P19099, gene: CYP11B2, swissprot: C11B2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25874338) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11465421) Metopirone is an inhibitor of endogenous adrenal corticosteroid synthesis. The pharmacological effect of Metopirone is to reduce cortisol and corticosterone production by inhibiting the 11-betahydroxylation reaction in the adrenal cortex. Metopirone is used as a diagnostic test, with urinary 17-hydroxycorticosteroids measured as an index of pituitary adrenocorticotropic hormone responsiveness. Metopirone may also suppress biosynthesis of aldosterone, resulting in a mild natriuresis. diagnostic agent (Code: CHEBI:33295) Antimetabolites (Code: D000963) Enzyme Inhibitors (Code: D004791) Noxae (Code: D009676) Adrenal Steroid Synthesis Inhibitor (Code: N0000175928) Adrenal Steroid Synthesis Inhibitors (Code: N0000175921) 1961-12-04 FDA MYT
Click to view kojic acid Polyphenol oxidase (Organism: Agaricus bisporus, class: Enzyme, accessions: Q00024|O42713|C7FF04|C7FF05, gene: PPO1|PPO2|PPO3|PPO4, swissprot: PPO1_AGABI|PPO2_AGABI|PPO3_AGABI|PPO4_AGABI) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16513349) D-amino-acid oxidase (Organism: Homo sapiens, class: Enzyme, accessions: P14920, gene: DAO, swissprot: OXDA_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23683589) Kojic acid is a pyranone that has been isolated from the fungus Aspergillus oryzae. It has a role as a NF-kappaB inhibitor, an Aspergillus metabolite, a skin lightening agent, an catechol oxidase inhibitor, an laccase inhibitor, an quercetin 2,3-dioxygenase inhibitor, an tyrosinase inhibitor and an D-amino-acid oxidase inhibitor. it is used to treat skin diseases like melasma. Kojic acid also has antibacterial and antifungal properties. skin lightening agent (Code: CHEBI:85046) Antioxidants (Code: D000975) Protective Agents (Code: D020011) KOJ
Click to view piracetam Piracetam is a nootropic drug in the racetams group, with chemical name 2-oxo-1-pyrrolidine acetamide. It shares the same 2-oxo-pyrrolidone base structure with pyroglutamic acid and is a cyclic derivative of the neurotransmitter gamma-aminobutyric acid (GABA). However its mechanism of action differ from that of endogenous GABA.Piracetam has neuroprotective and anticonvulsant properties and is reported to improve neural plasticity. Its efficacy is documented in cognitive disorders and dementia, vertigo, cortical myoclonus, dyslexia, and sickle cell anemia although the clinical application in these conditions is not yet established. Piracetam has effects on the vascular system by reduce erythrocyte adhesion to vascular endothelium, hinder vasospasm and facilitate microcirculation. Piracetam is indicated in adult patients suffering from myoclonus of cortical origin, irrespective of aetiology, and should be used in combination with other antimyoclonic therapies. Central Nervous System Agents (Code: D002491) Neuroprotective Agents (Code: D018696) Nootropic Agents (Code: D018697) Protective Agents (Code: D020011) 1975-06-01 Spanish Agency of Medicines and Medical Products (AEMPS) PZI
Click to view methylthiouracil Methylthiouracil is a thiourea antithyroid agent that inhibits the synthesis of thyroid hormone. Methylthiouracil was introduced for the treatment of hyperthyroidism. Methylthiouracil is no longer in clinical use in most countries. Methylthiouracil is possibly carcinogenic to humans. Antithyroid Agents (Code: D013956) Hormone Antagonists (Code: D006727) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) 1958 YEAR INTRODUCED
Click to view mesna Mesna is a sulfhydryl compound that is used to reduce the incidence of hemorrhagic cystitis associated with certain chemotherapeutic agents. Mesna is converted to a free thiol compound in the kidney, where it binds to and inactivates acrolein and other urotoxic metabolites of ifosfamide and cyclophosphamide, thereby reducing their toxic effects on the urinary tract during urinary excretion. Protective Agents (Code: D020011) 1988-12-30 FDA COM
Click to view trimethadione Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/14651673) Cytochrome P450 2E1 (Organism: Homo sapiens, class: Enzyme, accessions: P05181, gene: CYP2E1, swissprot: CP2E1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/14651673) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/14651673) Trimethadione is an oxazolidinedione compound and an antiepileptic agent. Trimethadione has been shown to prevent pentylenetetrazol-induced and thujone-induced seizures in experimental animals. Unlike the hydantoins and antiepileptic barbiturates, trimethadione does not modify the maximal seizure pattern in patients undergoing electroconvulsive therapy. Trimethadione is rapidly absorbed from the gastrointestinal tract. It is demethylated by liver microsomes to the active metabolite, dimethadione. Trimethadione is indicated for the control of petit mal seizures that are refractory to treatment with other drugs. Anti-epileptic Agent (Code: N0000175753) Decreased Central Nervous System Disorganized Electrical Activity (Code: N0000008486) Anticonvulsants (Code: D000927) Central Nervous System Agents (Code: D002491) 1946-01-25 FDA
Click to view valpromide Valpromide is a derivative of valproic acid. Valpromide has been shown to decrease aggressivity in stress-induced animals, to regulate anxious induced behaviours, as well as to potentiate central sedative compounds. It produces a significant increase of cognitive functions. Valpromide is indicated for the treatment of bipolar disorder (manic episodes). Anticonvulsants (Code: D000927) Central Nervous System Agents (Code: D002491) 1999-12-23 Italian Medicines Agency (AIFA) VPR
Click to view valnoctamide Valnoctamide is a valproic acid derivative associated with a decreased risk for congenital abnormalities and developed for treatment mania. Valnoctamide has been marketed as an anxiolytic and sedative. It is no longer available. Italian Medicines Agency (AIFA)
Click to view betanaphthol Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15916432) Betanaphthol is a monatomic phenol occurring in coal-tar, but usually prepared artificially from naphthalene. Betanaphthol is antiseptic, antifermentative, deodorant, and may also be considered a disinfectant. Its action closely resembles that of phenol, but is less poisonous. Betanaphthol (in combination with salicylic acid) is used for the treatment of skin dermatomycosis of sleek skin and hairy parts of the head. 2010-10-22 Bulgarian Drug Agency (BDA) 03V
Click to view trichloroacetic acid Trichloroacetic acid (TCA; also known as trichloroethanoic acid) is an analogue of acetic acid. In clinical chemistry and biochemistry, it is used as a precipitant of macromolecules including proteins, DNA and RNA. Trichloroacetate is also found in cosmetic treatments and topical formulations as a cauterant, which removes condyloma or warts on the skin. Caustics (Code: D002424) Noxae (Code: D009676) 1993-12-01 Italian Medicines Agency (AIFA)
Click to view octanoic acid Solute carrier family 22 member 6 (Organism: Homo sapiens, class: Transporter, accessions: Q4U2R8, gene: SLC22A6, swissprot: S22A6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11669456) Solute carrier family 22 member 8 (Organism: Homo sapiens, class: Transporter, accessions: Q8TCC7, gene: SLC22A8, swissprot: S22A8_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11669456) Solute carrier family 22 member 6 (Organism: Homo sapiens, class: Transporter, accessions: Q4U2R8, gene: SLC22A6, swissprot: S22A6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11669456) Solute carrier family 22 member 8 (Organism: Homo sapiens, class: Transporter, accessions: Q8TCC7, gene: SLC22A8, swissprot: S22A8_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11669456) Solute carrier family 22 member 11 (Organism: Homo sapiens, class: Transporter, accessions: Q9NSA0, gene: SLC22A11, swissprot: S22AB_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12063169) Octanoic acid (caprylic acid) is a saturated medium-chain fatty acid with an 8-carbon backbone. Octanoic acid is found naturally in the milk of various mammals and is a minor component of coconut oil and palm kernel oil. Octanoic acid is an antimicrobial pesticide used as a disinfectant agent. OCA
Click to view valproic acid Histone deacetylase 1 (Organism: Homo sapiens, class: Enzyme, accessions: Q13547, gene: HDAC1, swissprot: HDAC1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21874153) Histone deacetylase 2 (Organism: Homo sapiens, class: Enzyme, accessions: Q92769, gene: HDAC2, swissprot: HDAC2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21874153) Histone deacetylase 3 (Organism: Homo sapiens, class: Enzyme, accessions: O15379, gene: HDAC3, swissprot: HDAC3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21874153) Histone deacetylase 8 (Organism: Homo sapiens, class: Enzyme, accessions: Q9BY41, gene: HDAC8, swissprot: HDAC8_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21874153) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/20602621) UDP-glucuronosyltransferase 2B7 (Organism: Homo sapiens, class: Enzyme, accessions: P16662, gene: UGT2B7, swissprot: UD2B7_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/18838507) UDP-glucuronosyltransferase 1-4 (Organism: Homo sapiens, class: Enzyme, accessions: P22310, gene: UGT1A4, swissprot: UD14_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/18838507) UDP-glucuronosyltransferase 1-8 (Organism: Homo sapiens, class: Enzyme, accessions: Q9HAW9, gene: UGT1A8, swissprot: UD18_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/18838507) UDP-glucuronosyltransferase 1-10 (Organism: Homo sapiens, class: Enzyme, accessions: Q9HAW8, gene: UGT1A10, swissprot: UD110_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/18838507) Solute carrier family 22 member 6 (Organism: Rattus norvegicus, class: Transporter, accessions: O35956, gene: Slc22a6, swissprot: S22A6_RAT) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/9228014) Solute carrier family 22 member 5 (Organism: Homo sapiens, class: Transporter, accessions: O76082, gene: SLC22A5, swissprot: S22A5_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10525100) Monocarboxylate transporter 1 (Organism: Rattus norvegicus, class: Transporter, accessions: P53987, gene: Slc16a1, swissprot: MOT1_RAT) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10579682) Solute carrier organic anion transporter family member 2B1 (Organism: Homo sapiens, class: Transporter, accessions: O94956, gene: SLCO2B1, swissprot: SO2B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22541068) Valproic acid is a carboxylic acid designated as 2-propylpentanoic acid. It is also known as dipropylacetic acid. Valproic acid dissociates to the valproate ion in the gastrointestinal tract. The mechanisms by which valproate exerts its therapeutic effects have not been established. It has been suggested that its activity in epilepsy is related to increased brain concentrations of gamma-aminobutyric acid (GABA). Valproic acid is indicated as monotherapy and adjunctive therapy in the treatment of patients with complex partial seizures that occur either in isolation or in association with other types of seizures. Valproic acid also is indicated for use as sole and adjunctive therapy in the treatment of simple and complex absence seizures, and adjunctively in patients with multiple seizure types which include absence seizures. GABA agent (Code: CHEBI:51374) anticonvulsant (Code: CHEBI:35623) psychotropic drug (Code: CHEBI:35471) neuroprotective agent (Code: CHEBI:63726) antimanic drug (Code: CHEBI:35477) Anti-epileptic Agent (Code: N0000175753) Decreased Central Nervous System Disorganized Electrical Activity (Code: N0000008486) Mood Stabilizer (Code: N0000175751) Anticonvulsants (Code: D000927) Antimanic Agents (Code: D018692) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Enzyme Inhibitors (Code: D004791) GABA Agents (Code: D018682) Neurotransmitter Agents (Code: D018377) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149) 1978-02-28 FDA 2PP
Click to view octamoxin Octamoxin (2-octylhydrazine) is both an irreversible and nonselective monoamine oxidase enzyme inhibitor (MAOI) of the hydrazine chemical class. This drug was used in the past as an antidepressant agent in the 1960s, however, has since been discontinued.
Click to view ethchlorvynol Ethchlorvynol is a sedative and hypnotic drug. Ethchlorvynol is a schedule IV (USA) controlled substance. It produces cerebral depression, however the exact mechanism of action is not known. Ethchlorvynol appears to depress the central nervous system in a manner similar to that of barbiturates. It has been used to treat insomnia, but has been largely superseded and is only offered where an intolerance or allergy to other drugs exists. sedative (Code: CHEBI:35717) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Hypnotics and Sedatives (Code: D006993) 1961-05-10 FDA
Click to view methyl aminolevulinate Methyl aminolevulinate is the methyl ester of 5-aminolevulinic acid. Methyl aminolevulinate is a prodrug, it is metabolised to protoporphyrin IX, a photosensitizer. Topical application (often as the hydrochloride salt) results in an accumulation of protoporphyrin IX in the skin lesions to which the cream has been applied. Subsequent illumination with red light results in the generation of toxic singlet oxygen that destroys cell membranes and thereby kills the tumour cells. Methyl aminolevulinate is used in the photodynamic treatment of non-melanoma skin cancer (including basal cell carcinoma). Methyl aminolevulinate is also used for the treatment of thin and moderately thick, non-hyperkeratotic, non-pigmented actinic keratoses of the face and scalp in immunocompetent patients when used in conjunction with lesion preparation in the physician’s office when other therapies are considered medically less appropriate. antineoplastic agent (Code: CHEBI:35610) photosensitizing agent (Code: CHEBI:47868) prodrug (Code: CHEBI:50266) dermatologic drug (Code: CHEBI:50177) Porphyrin Precursor (Code: N0000175846) Porphyrinogens (Code: N0000171207) 2004-07-27 FDA
Click to view camphor Methionine aminopeptidase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P50579, gene: METAP2, swissprot: MAP2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20621724) Methionine aminopeptidase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P53582, gene: METAP1, swissprot: MAP11_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20621724) Methionine aminopeptidase (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P0AE18, gene: map, swissprot: MAP1_ECOLI) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20621724) Catechol O-methyltransferase (Organism: Rattus norvegicus, class: Enzyme, accessions: P22734, gene: Comt, swissprot: COMT_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/817025) Camphor is an antiseptic with mild fungistatic, bacteriostatic, anthelmintic, and amebicidal action. It is also used as a reagent and metal chelator, as a carrier for radio-indium for diagnostic purposes, and its halogenated derivatives are used in addition as topical anti-infective agents and oral antiamebics. antiseptic drug (Code: CHEBI:48218) antifungal agrochemical (Code: CHEBI:86328) 1964-04-30 Ministry of Health of the Russian Federation HQY
Click to view emylcamate Emylcamate is an anxiolytic and muscle relaxant. It is used for the treatment of anxiety and tension. It is no longer prescribed.
Click to view heptaminol Heptaminol is an amino alcohol that has been used as a myocardial stimulant and vasodilator and to relieve bronchospasm. Its most common therapeutic use is in orthostatic hypotension. The mechanism of heptaminol's therapeutic actions is not well understood although it has been suggested to affect catecholamine release or calcium metabolism.
Click to view trioxsalen Trioxsalen (trimethylpsoralen, trioxysalen or trisoralen) is a furanocoumarin and a psoralen derivative. It is obtained from several plants, mainly Psoralea corylifolia. Like other psoralens it causes photosensitization of the skin. The photoactivated form produces interstrand linkages in DNA resulting in cell apoptosis. It is administered either topically or orally in conjunction with UV-A (the least damaging form of ultraviolet light) for phototherapy treatment of vitiligo and hand eczema. dermatologic drug (Code: CHEBI:50177) photosensitizing agent (Code: CHEBI:47868) Psoralen (Code: N0000175879) Psoralens (Code: N0000007909) Dermatologic Agents (Code: D003879) Photosensitizing Agents (Code: D017319) Radiation-Sensitizing Agents (Code: D011838) 1964-07-24 FDA
Click to view gimeracil Dihydropyrimidine dehydrogenase [NADP(+)] (Organism: Homo sapiens, class: Enzyme, accessions: Q12882, gene: DPYD, swissprot: DPYD_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/21668582) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inducer (Source: https://www.ema.europa.eu/documents/product-information/teysuno-epar-product-information_en.pdf) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) inducer (Source: https://www.ema.europa.eu/documents/product-information/teysuno-epar-product-information_en.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inducer (Source: https://www.ema.europa.eu/documents/product-information/teysuno-epar-product-information_en.pdf) Cytochrome P450 3A5 (Organism: Homo sapiens, class: Enzyme, accessions: P20815, gene: CYP3A5, swissprot: CP3A5_HUMAN) inducer (Source: https://www.ema.europa.eu/documents/product-information/teysuno-epar-product-information_en.pdf) Gimeracil is a dihydropyrimidine dehydrogenase (DPD) inhibitor which used to prevent degradation of 5-fluorouracil (5-FU) by the body. Gimeracil inhibits the metabolism of 5-FU by reversibly and selectively inhibiting DPD, the primary metabolic enzyme for 5-FU, so that higher plasma concentrations of 5-FU are achieved with the administration of a lower dose of tegafur. Gimeracil is indicated in combination with tegaflur and oteracil for the treatment of advanced gastric cancer. 2011-03-14 EMA
Click to view adipic acid Solute carrier family 22 member 6 (Organism: Mus musculus, class: Transporter, accessions: Q8VC69, gene: Slc22a6, swissprot: S22A6_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17553798) Solute carrier family 22 member 20 (Organism: Mus musculus, class: Transporter, accessions: Q80UJ1, gene: Slc22a20, swissprot: S22AK_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17553798) Adipic acid is an alpha,omega-dicarboxylic acid that is the 1,4-dicarboxy derivative of butane. It has a role as a food acidity regulator and a human xenobiotic metabolite. It is used to make plastics and foams and for other uses. Adipic acid in the urine and in the blood is typically exogenous in origin and is a good biomarker of jello consumption. In fact, a condition known as adipic aciduria is actually an artifact of jello consumption. However, certain disorders (such as diabetes and glutaric aciduria type I) can lead to elevated levels of adipic acid snd other dicarboxcylic acids (such as suberic acid) in urine. Moreover, adipic acid is also found to be associated with 3-hydroxy-3-methylglutaryl-CoA lyase deficiency, carnitine-acylcarnitine translocase deficiency, malonyl-Coa decarboxylase deficiency, and medium Chain acyl-CoA dehydrogenase deficiency, which are inborn errors of metabolism. food acidity regulator (Code: CHEBI:64049) 0L1
Click to view isosorbide Isosorbide is an effective hyperosmotic agent which can be administered orally without gastrointestinal irritation. Isosorbide (Ismotic, Hydronol) is a dihydric alcohol formed by the removal of two molecules of water from sorbitol. Its actions are similar to those of glycerol. Hyperosmotic agents lower intraocular pressure by creating an osmotic gradient between the blood and the ocular fluids. Isosorbide is used for the short-term reduction of intraocular pressure. May be used prior to and after intraocular surgery. May be used to interrupt an acute attack of glaucoma. Diuretics (Code: D004232) Diuretics, Osmotic (Code: D004234) Natriuretic Agents (Code: D045283) 1974-01-30 FDA
Click to view coumarin Carbonic anhydrase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P00915, gene: CA1, swissprot: CAH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19206230) Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19206230) Carbonic anhydrase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P22748, gene: CA4, swissprot: CAH4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19206230) Carbonic anhydrase 5B, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: Q9Y2D0, gene: CA5B, swissprot: CAH5B_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19206230) Amine oxidase [flavin-containing] A (Organism: Rattus norvegicus, class: Enzyme, accessions: P21396, gene: Maoa, swissprot: AOFA_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11123983) Amine oxidase [flavin-containing] B (Organism: Rattus norvegicus, class: Enzyme, accessions: P19643, gene: Maob, swissprot: AOFB_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11123983) Cytochrome P450 2A6 (Organism: Homo sapiens, class: Enzyme, accessions: P11509, gene: CYP2A6, swissprot: CP2A6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15658857) Coumarin and its derivatives are alpha-benzopyrones. Coumarin is metabolized in humans to 7-hydroxycoumarin. Coumarin is isolated from the tonka bean Coumarouna odorata. Coumarin is a secondary phytochemical with hepatotoxic and carcinogenic properties. Coumarin has been reported to exhibit antioxidant, analgesic, anti-inflammatory, and antimutagenic properties. Coumarin is used in the pharmaceutical industry as a precursor reagent in the synthesis of a number of synthetic anticoagulant pharmaceuticals. Also it was used as a homeopatic drug for temporary relief of allergies caused products. fluorescent dye (Code: CHEBI:51121) 1995 CDSCO (INDIA) COU
Click to view glutamine Glutamine is a non-essential amino acid present abundantly throughout the body and is involved in many metabolic processes. It is synthesized from glutamic acid and ammonia. It is the principal carrier of nitrogen in the body and is an important energy source for many cells. L-glutamine is an optically active form of glutamine having L-configuration. L-glutamine appears to play a major role in protecting the integrity of the gastrointestinal tract and, in particular, the large intestine. L-glutamine is the preferred respiratory fuel for enterocytes, colonocytes and lymphocytes. The exact mechanism of the possible immunomodulatory action of supplemental L-glutamine remains unclear. It is conceivable that the major effect of L-glutamine occurs at the level of the intestine. Perhaps enteral L-glutamine acts directly on intestine-associated lymphoid tissue and stimulates overall immune function by that mechanism, without passing beyond the splanchnic bed. Glutamine is used for nutritional supplementation, also for treating dietary shortage or imbalance. Amino Acid (Code: N0000175780) Amino Acids (Code: N0000006806) 2004-06-10 FDA DGN
GLN
Click to view acetylpheneturide Acetylpheneturide suppresses epileptic attacks by acting on the central nerves. Acetylpheneturide is used as an anticonvulsant in the treatment of epilepsy.
Click to view lysine G-protein coupled receptor family C group 6 member A (Organism: Homo sapiens, class: GPCR, accessions: Q5T6X5, gene: GPRC6A, swissprot: GPC6A_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/15576628) Mitochondrial ornithine transporter 1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y619, gene: SLC25A15, swissprot: ORNT1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12807890) Mitochondrial ornithine transporter 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9BXI2, gene: SLC25A2, swissprot: ORNT2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12807890) Sodium-coupled neutral amino acid transporter 4 (Organism: Homo sapiens, class: Transporter, accessions: Q969I6, gene: SLC38A4, swissprot: S38A4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11342143) Lysine is one of nine essential amino acids in humans required for growth and tissue repair, Lysine is supplied by many foods, especially red meats, fish, and dairy products. L-Lysine is a nutritional supplement containing the biologically active L-isomer of the essential amino acid lysine, with potential anti-mucositis activity. Upon oral intake, L-lysine promotes healthy tissue function, growth and healing and improves the immune system. L-Lysine promotes calcium uptake, is essential for carnitine production and collagen formation. As collagen is essential for connective tissue maintenance, this agent may also help heal mucosal wounds. This may help decrease and prevent mucositis induced by radiation or chemotherapy. nutraceutical (Code: CHEBI:50733) anticonvulsant (Code: CHEBI:35623) 1971-09-24 FDA LYS
DLY
Click to view oxapropanium Oxapropanium is a synthetic cholinomimetics.
Click to view acetylcholine Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9224827) Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9224827) Muscarinic acetylcholine receptor M4 (Organism: Homo sapiens, class: GPCR, accessions: P08173, gene: CHRM4, swissprot: ACM4_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9224827) Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9224827) Muscarinic acetylcholine receptor M5 (Organism: Homo sapiens, class: GPCR, accessions: P08912, gene: CHRM5, swissprot: ACM5_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/22677319) Vesicular acetylcholine transporter (Organism: Rattus norvegicus, class: Transporter, accessions: Q62666, gene: Slc18a3, swissprot: VACHT_RAT) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15485505) Neuronal acetylcholine receptor; alpha4/beta2 (Organism: Homo sapiens, class: Ion channel, accessions: P43681|P17787, gene: CHRNA4|CHRNB2, swissprot: ACHA4_HUMAN|ACHB2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/26225816) Neuronal acetylcholine receptor; alpha3/beta4 (Organism: Rattus norvegicus, class: Ion channel, accessions: P04757|P12392, gene: Chrna3|Chrnb4, swissprot: ACHA3_RAT|ACHB4_RAT) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/19027295) Solute carrier family 22 member 1 (Organism: Rattus norvegicus, class: Transporter, accessions: Q63089, gene: Slc22a1, swissprot: S22A1_RAT) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/8898084) Acetylcholine (ACh) is a neurotransmitter. Acetylcholine in vertebrates is the major transmitter at neuromuscular junctions, autonomic ganglia, parasympathetic effector junctions, a subset of sympathetic effector junctions, and at many sites in the central nervous system. Various nicotinic and muscarinic ACh receptors are present in both afferent nerve endings and glomus cells. Therefore, ACh can depolarize or hyperpolarize the cell membrane depending on the available receptor type in the vicinity. Binding of ACh to its receptor can create a wide variety of cellular responses including opening cation channels (nicotinic ACh receptor activation), releasing Ca2+ from intracellular storage sites (via muscarinic ACh receptors), and modulating activities of K+ and Ca2+ channels. Acetylcholine is used to obtain miosis of the iris in seconds after delivery of the lens in cataract surgery, in penetrating keratoplasty, iridectomy and other anterior segment surgery where rapid miosis may be required. vasodilator agent (Code: CHEBI:35620) muscarinic agonist (Code: CHEBI:38325) Cardiovascular Agents (Code: D002317) Cholinergic Agents (Code: D018678) Cholinergic Agonists (Code: D018679) Neurotransmitter Agents (Code: D018377) Vasodilator Agents (Code: D014665) Cholinergic Receptor Agonist (Code: N0000175884) 1973-10-09 FDA ACH
Click to view trientine copper (Organism: None, class: Inorganic material, accessions: None, gene: None, swissprot: None) chelating agent (Source: http://www.ncbi.nlm.nih.gov/pubmed/6121964) Carbonic anhydrase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P22748, gene: CA4, swissprot: CAH4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20590092) Carbonic anhydrase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P00915, gene: CA1, swissprot: CAH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20590092) Carbonic anhydrase 5A, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P35218, gene: CA5A, swissprot: CAH5A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20590092) Carbonic anhydrase 5B, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: Q9Y2D0, gene: CA5B, swissprot: CAH5B_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20590092) Carbonic anhydrase 3 (Organism: Homo sapiens, class: Enzyme, accessions: P07451, gene: CA3, swissprot: CAH3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20590092) Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20590092) Carbonic anhydrase 14 (Organism: Homo sapiens, class: Enzyme, accessions: Q9ULX7, gene: CA14, swissprot: CAH14_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20590092) Carbonic anhydrase 7 (Organism: Homo sapiens, class: Enzyme, accessions: P43166, gene: CA7, swissprot: CAH7_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20590092) Carbonic anhydrase 13 (Organism: Mus musculus, class: Enzyme, accessions: Q9D6N1, gene: Ca13, swissprot: CAH13_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20590092) Carbonic anhydrase 12 (Organism: Homo sapiens, class: Enzyme, accessions: O43570, gene: CA12, swissprot: CAH12_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20590092) Carbonic anhydrase 9 (Organism: Homo sapiens, class: Enzyme, accessions: Q16790, gene: CA9, swissprot: CAH9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20590092) Carbonic anhydrase 15 (Organism: Mus musculus, class: Enzyme, accessions: Q99N23, gene: Ca15, swissprot: CAH15_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20590092) Carbonic anhydrase 6 (Organism: Homo sapiens, class: Enzyme, accessions: P23280, gene: CA6, swissprot: CAH6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20590092) Trientine ( triethylenetatramine, TETA) is a chelating compound for removal of excess copper from the body. Its salt form, trientine (triethylenetetramine dihydrochloride or 2,2,2-tetramine) was introduced as an alternative to D-penicillamine. It consists of a polyamine-like structure different from D-penicillamine, as it lack sulfhydryl groups. Although penicillamine treatment is believed to be more extensive, TETA therapy has been shown to be an effective initial therapy, even with patients with decompensated liver disease at the outset, and prolonged TETA treatment is not associated with adverse effects as expected in penicillamine treatment. Trietine is indicated in the treatment of patients with Wilson's disease who are intolerant of penicillamine. Metal Chelating Activity (Code: N0000175472) Metal Chelator (Code: N0000175473) Chelating Agents (Code: D002614) Sequestering Agents (Code: D064449) 1985-11-08 FDA 104
Click to view ambazone Ambazone is an antiseptic agent with potential antibacterial and antileukemic activity. Although the exact mechanism of action remains to be fully elucidated, ambazone appears to interfere with the membrane-bound nucleotide system by increasing the intracellular concentration of cAMP in leukemia cells and macrophages, which potentially contributes to this agent's antineoplastic activity. Furthermore, this agent's affinity for various cellular targets, i.e. membranes, nucleic acids and proteins, may contribute to the overall antibacterial effect. Ambazone is used as an adjunct in the treatment of acute infectious oral and pharyngeal infections (eg, gingivitis, stomatitis, tonsillitis) and after removal of tonsils or teeth. 2008-03-01 NAMMDR (National Agency for Medicines and Medical Devices of Romania)
Click to view glutamic acid Metabotropic glutamate receptor 2 (Organism: Homo sapiens, class: GPCR, accessions: Q14416, gene: GRM2, swissprot: GRM2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10530814) Metabotropic glutamate receptor 3 (Organism: Homo sapiens, class: GPCR, accessions: Q14832, gene: GRM3, swissprot: GRM3_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10530814) Metabotropic glutamate receptor 1 (Organism: Homo sapiens, class: GPCR, accessions: Q13255, gene: GRM1, swissprot: GRM1_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10443583) Metabotropic glutamate receptor 4 (Organism: Homo sapiens, class: GPCR, accessions: Q14833, gene: GRM4, swissprot: GRM4_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10443583) Metabotropic glutamate receptor 5 (Organism: Homo sapiens, class: GPCR, accessions: P41594, gene: GRM5, swissprot: GRM5_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10443583) Metabotropic glutamate receptor 6 (Organism: Homo sapiens, class: GPCR, accessions: O15303, gene: GRM6, swissprot: GRM6_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10443583) Metabotropic glutamate receptor 8 (Organism: Homo sapiens, class: GPCR, accessions: O00222, gene: GRM8, swissprot: GRM8_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10443583) Sodium-coupled neutral amino acid transporter 3 (Organism: Homo sapiens, class: Transporter, accessions: Q99624, gene: SLC38A3, swissprot: S38A3_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10823827) Monocarboxylate transporter 1 (Organism: Rattus norvegicus, class: Transporter, accessions: P53987, gene: Slc16a1, swissprot: MOT1_RAT) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10579682) Glutamic acid is a non-essential aminoacid used in biosynthesis of proteins. Besides being a building block of proteins, glutamic acid plays a principal role in neural activation. Glutamic acid is also responsible for the umami (savory) flavor of certain foods. In medicine, glutamate is used as a metabolic supplemnet in patients undergoing coronary surgery. Glutamic acid activates both ionotropic and metabotropic glutamate receptors. The ionotropic ones being non-NMDA (AMPA and kainate) and NMDA receptors. Free glutamic acid cannot cross the blood-brain barrier in appreciable quantities; instead it is converted into L-glutamine, which the brain uses for fuel and protein synthesis. It is conjectured that glutamate is involved in cognitive functions like learning and memory in the brain, though excessive amounts may cause neuronal damage associated in diseases like amyotrophic lateral sclerosis, lathyrism, and Alzheimer's disease. Also, the drug phencyclidine (more commonly known as PCP) antagonizes glutamate at the NMDA receptor, causing behavior reminiscent of schizophrenia. Glutamic acid in action is extremely difficult to study due to its transient nature. 1985 FDA GLU
Click to view meldonium Gamma-butyrobetaine dioxygenase (Organism: Homo sapiens, class: Enzyme, accessions: O75936, gene: BBOX1, swissprot: BODG_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/24571165) Meldonium is an ammonium betaine that is beta-alaninate in which one of the amino hydrogens is replaced by a trimethylamino group. Meldonium is a cardioprotective drug that is used for treatment of heart failure, myocardial infarction, arrhythmia, atherosclerosis and diabetes. Meldonium was added to the World Anti-Doping Agency’s (WADA) list of banned substances. cardioprotective agent (Code: CHEBI:77307) neuroprotective agent (Code: CHEBI:63726) 1998-05-20
Click to view carbachol Muscarinic acetylcholine receptor M5 (Organism: Homo sapiens, class: GPCR, accessions: P08912, gene: CHRM5, swissprot: ACM5_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10323594) Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10323594) Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12505062) Muscarinic acetylcholine receptor M4 (Organism: Homo sapiens, class: GPCR, accessions: P08173, gene: CHRM4, swissprot: ACM4_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10323594) Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10323594) Carbachol is a synthetic choline ester and a positively charged quaternary ammonium compound. Carbachol is a parasympathomimetic that mimics the effect of acetylcholine on both the muscarinic and nicotinic receptors. Carbachol is used for the treatment of glaucoma, but is also used during ophthalmic surgery. nicotinic acetylcholine receptor agonist (Code: CHEBI:47958) muscarinic agonist (Code: CHEBI:38325) cardiotonic drug (Code: CHEBI:38147) miotic (Code: CHEBI:51068) non-narcotic analgesic (Code: CHEBI:35481) Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Autonomic Agents (Code: D001337) Cardiotonic Agents (Code: D002316) Cardiovascular Agents (Code: D002317) Central Nervous System Agents (Code: D002491) Cholinergic Agents (Code: D018678) Cholinergic Agonists (Code: D018679) Miotics (Code: D008916) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Protective Agents (Code: D020011) Sensory System Agents (Code: D018689) 1972-09-28 FDA CCE
Click to view ketoxal Kethoxal (3-Ethoxy-alpha-ketobutyraldehyde) modifies guanine containing oligoribonucleotides (by reacting selectively with guanine in polynucleotides). Ketoxal was used as an antiviral drug. Now ketoxal is used for the modification bases in RNA. Anti-Infective Agents (Code: D000890) Antiviral Agents (Code: D000998)
Click to view viloxazine Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9871604) Viloxazine is a selective norepinephrine reuptake inhibitor. It structurally differs from conventional tri- or tetra-cyclic antidepressants and it does not produce sedative anticholinergic or adrenergic effects in man. It was used in some European countries as an antidepressant drug. Adrenergic Agents (Code: D018663) Adrenergic Uptake Inhibitors (Code: D018759) Antidepressive Agents (Code: D000928) Antidepressive Agents, Second-Generation (Code: D018687) Central Nervous System Agents (Code: D002491) Membrane Transport Modulators (Code: D049990) Neurotransmitter Agents (Code: D018377) Neurotransmitter Uptake Inhibitors (Code: D014179) Psychotropic Drugs (Code: D011619) 1988-04-28 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view trolamine Trolamine is the salt formed between triethanolamine and salicylic acid. It is widely used as a topical analgesic such as are creams for temporarily relief of minor aches and pains of muscles and joints associated with arthritis, simple backache, lumbago, neuralgia, strains, bruises, and sprains. Trolamine was used as triethanolamine polypeptide in otic solution drops for removal of impacted cerumen prior to ear examination, otologic therapy and/or audiometry. Now trolamine is used for the treatment and prevention of radiotherapy-induced skin erythema. It is also used for the treatment burns and any other uninfected skin wounds. 1958 FDA 211
Click to view methionine S-adenosylmethionine synthase isoform type-2 (Organism: Rattus norvegicus, class: Enzyme, accessions: P18298, gene: Mat2a, swissprot: METK2_RAT) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/3755757) S-adenosylmethionine synthase isoform type-1 (Organism: Rattus norvegicus, class: Enzyme, accessions: P13444, gene: Mat1a, swissprot: METK1_RAT) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/3755757) Methionine is an non-polar, aliphatic, essential alpha-amino acid that is used in the biosynthesis of proteins. Methionine is sulphur containing amino acid and improves the tone and pliability of skin, hair, and strengthens nails. Involved in many detoxifying processes, sulphur provided by methionine protects cells from pollutants, slows cell aging, and is essential for absorption and bio-availability of selenium and zinc. Methionine chelates heavy metals, such as lead and mercury, aiding their excretion. It also acts as a lipotropic agent and prevents excess fat buildup in the liver. nutraceutical (Code: CHEBI:50733) 1975 FDA MED
MET
Click to view penicillamine Copper (Organism: None, class: Inorganic material, accessions: None, gene: None, swissprot: None) chelating agent (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2004/19853s012,014lbl.pdf) Penicillamine is a beta dimethyl analog of the amino acid cysteine. As a degradation product of penicillin antibiotics, penicillamine chelates with heavy metals and increases their urinary excretion. From in vitro studies which indicate that one atom of copper combines with two molecules of penicillamine, it would appear that one gram of penicillamine should be followed by the excretion of about 200 milligrams of copper. Penicillamine is used for treatment of Wilson's disease, cystinuria and active rheumatoid arthritis. antirheumatic drug (Code: CHEBI:35842) Antidotes (Code: D000931) Antirheumatic Agents (Code: D018501) Chelating Agents (Code: D002614) Protective Agents (Code: D020011) Sequestering Agents (Code: D064449) Antirheumatic Agent (Code: N0000175713) 1970-12-04 FDA LEI
Click to view phenpromethamine Phenpromethamine is a stimulant; it is chemically and structurally related to amphetamine. Phenpromethamine is prohibited from sport under the 'S6: Stimulants' of the WADA List of Prohibited Substances and Methods as a result of its purported stimulant properties due to its structural relationship to amphetamine, its derivatives (e.g. methamphetamine) and analogues (WADA 2019).
Click to view tioxolone Carbonic anhydrase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P00915, gene: CA1, swissprot: CAH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18572406) Carbonic anhydrase 12 (Organism: Homo sapiens, class: Enzyme, accessions: O43570, gene: CA12, swissprot: CAH12_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18572406) Carbonic anhydrase 13 (Organism: Mus musculus, class: Enzyme, accessions: Q9D6N1, gene: Ca13, swissprot: CAH13_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18572406) Carbonic anhydrase 14 (Organism: Homo sapiens, class: Enzyme, accessions: Q9ULX7, gene: CA14, swissprot: CAH14_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18572406) Carbonic anhydrase 15 (Organism: Mus musculus, class: Enzyme, accessions: Q99N23, gene: Ca15, swissprot: CAH15_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18572406) Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18572406) Carbonic anhydrase 3 (Organism: Homo sapiens, class: Enzyme, accessions: P07451, gene: CA3, swissprot: CAH3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18572406) Carbonic anhydrase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P22748, gene: CA4, swissprot: CAH4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18572406) Carbonic anhydrase 5A, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P35218, gene: CA5A, swissprot: CAH5A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18572406) Carbonic anhydrase 5B, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: Q9Y2D0, gene: CA5B, swissprot: CAH5B_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18572406) Carbonic anhydrase 6 (Organism: Homo sapiens, class: Enzyme, accessions: P23280, gene: CA6, swissprot: CAH6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18572406) Carbonic anhydrase 7 (Organism: Homo sapiens, class: Enzyme, accessions: P43166, gene: CA7, swissprot: CAH7_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18572406) Carbonic anhydrase 9 (Organism: Homo sapiens, class: Enzyme, accessions: Q16790, gene: CA9, swissprot: CAH9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18572406) Amine oxidase [flavin-containing] A (Organism: Homo sapiens, class: Enzyme, accessions: P21397, gene: MAOA, swissprot: AOFA_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/26821818) Amine oxidase [flavin-containing] B (Organism: Homo sapiens, class: Enzyme, accessions: P27338, gene: MAOB, swissprot: AOFB_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/26821818) Tioxolone is a metalloenzyme carbonic anhydrase I inhibitor. Tioxolone has cytostatic, antipsoriatic, antibacterial and anti-mycotic properties. It has been used topically for many years, in the treatment of various skin and scalp disorders. It is used in anti-acne and rinse-off products respectively. The substance has also been used for seborrheic dermatitis. antiseborrheic (Code: CHEBI:59010)
Click to view phentermine Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/022580s016lbl.pdf) Trace amine-associated receptor 1 (Organism: Homo sapiens, class: GPCR, accessions: Q96RJ0, gene: TAAR1, swissprot: TAAR1_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/18602830) Sodium-dependent dopamine transporter (Organism: Rattus norvegicus, class: Transporter, accessions: P23977, gene: Slc6a3, swissprot: SC6A3_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11071707) Sodium-dependent serotonin transporter (Organism: Mus musculus, class: Transporter, accessions: Q60857, gene: Slc6a4, swissprot: SC6A4_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11071707) Amine oxidase [flavin-containing] A (Organism: Homo sapiens, class: Enzyme, accessions: P21397, gene: MAOA, swissprot: AOFA_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11911838) Amine oxidase [flavin-containing] B (Organism: Homo sapiens, class: Enzyme, accessions: P27338, gene: MAOB, swissprot: AOFB_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11911838) Phentermine is a sympathomimetic amine anorectic agent. It is chemically related to amphetamine and it is commonly referred to as an atypical amphetamine. Phentermine is an indirect-acting sympathomimetic agent that acts by releasing noradrenaline from the presynaptic vesicles in the lateral hypothalamus. Phentermine is indicated, alone or in combination with topiramate, as a short-term adjunct, not pass a few weeks, in a regimen of weight reduction based on exercise, behavioral modifications and caloric restriction in the management of exogenous obesity. dopaminergic agent (Code: CHEBI:48560) adrenergic agent (Code: CHEBI:37962) sympathomimetic agent (Code: CHEBI:35524) appetite depressant (Code: CHEBI:50507) central nervous system drug (Code: CHEBI:35470) central nervous system stimulant (Code: CHEBI:35337) Appetite Suppression (Code: N0000175372) Increased Sympathetic Activity (Code: N0000175651) Sympathomimetic Amine Anorectic (Code: N0000175423) Adrenergic Agents (Code: D018663) Anti-Obesity Agents (Code: D019440) Appetite Depressants (Code: D001067) Autonomic Agents (Code: D001337) Central Nervous System Agents (Code: D002491) Central Nervous System Stimulants (Code: D000697) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Sympathomimetics (Code: D013566) 1959-05-04 FDA
Click to view isocarboxazid Amine oxidase [flavin-containing] A (Organism: Homo sapiens, class: Enzyme, accessions: P21397, gene: MAOA, swissprot: AOFA_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/011961s045lbl.pdf) Amine oxidase [flavin-containing] B (Organism: Homo sapiens, class: Enzyme, accessions: P27338, gene: MAOB, swissprot: AOFB_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/011961s045lbl.pdf) Isocarboxazid is a monoamine oxidase inhibitor. In vivo and in vitro studies demonstrated inhibition of MAO in the brain, heart, and liver. The mechanism by which MAO inhibitors act as antidepressants is not fully understood, but it is thought to involve the elevation of brain levels of biogenic amines. Isocarboxazid is indicated for the treatment of depression. Monoamine Oxidase Inhibitor (Code: N0000175744) Antidepressive Agents (Code: D000928) Central Nervous System Agents (Code: D002491) Enzyme Inhibitors (Code: D004791) Monoamine Oxidase Inhibitors (Code: D008996) Psychotropic Drugs (Code: D011619) 1959-07-01 FDA
Click to view methamphetamine Trace amine-associated receptor 1 (Organism: Homo sapiens, class: GPCR, accessions: Q96RJ0, gene: TAAR1, swissprot: TAAR1_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/22037049) Synaptic vesicular amine transporter (Organism: Rattus norvegicus, class: Transporter, accessions: Q01827, gene: Slc18a2, swissprot: VMAT2_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23993667) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/9311621) Solute carrier family 22 member 3 (Organism: Rattus norvegicus, class: Transporter, accessions: O88446, gene: Slc22a3, swissprot: S22A3_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9830022) Solute carrier family 22 member 5 (Organism: Homo sapiens, class: Transporter, accessions: O76082, gene: SLC22A5, swissprot: S22A5_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9618255) Methamphetamine is a central nervous system stimulant and sympathomimetic. Methamphetamine is a mixture of two isomers. One isomer called Dextro, or D Methamphetamine, is active as a central nervous system stimulant. Desoxyn, a prescription drug also contains D Methamphetamine, is used for the treatment of attention deficit disorder with hyperactivity. The other isomer, levomethamphetamine, the L-enantiomer of methamphetamine is a sympathomimetic vasoconstrictor used in some over-the-counter (OTC) nasal decongestant inhalers in the United States.D-methamphetamine is the more physiologically active isomer. psychotropic drug (Code: CHEBI:35471) central nervous system stimulant (Code: CHEBI:35337) Amphetamine Anorectic (Code: N0000175425) Amphetamines (Code: N0000007883) Appetite Suppression (Code: N0000175372) Central Nervous System Stimulation (Code: N0000175729) Increased Sympathetic Activity (Code: N0000175651) Adrenergic Agents (Code: D018663) Adrenergic Uptake Inhibitors (Code: D018759) Autonomic Agents (Code: D001337) Central Nervous System Agents (Code: D002491) Central Nervous System Stimulants (Code: D000697) Dopamine Agents (Code: D015259) Dopamine Uptake Inhibitors (Code: D018765) Membrane Transport Modulators (Code: D049990) Neurotransmitter Agents (Code: D018377) Neurotransmitter Uptake Inhibitors (Code: D014179) Peripheral Nervous System Agents (Code: D018373) Sympathomimetics (Code: D013566) 1943-12-31 FDA B40
Click to view ditiocarb Cytochrome P450 2E1 (Organism: Homo sapiens, class: Enzyme, accessions: P05181, gene: CYP2E1, swissprot: CP2E1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11501186) Ditiocarb is a sulfhydryl-containing carbamate that is the primary in vivo metabolite of disulfiram. Diethyldithiocarbamate chelates zinc, thereby inhibiting metalloproteinases, thereby preventing the degradation of the extracellular matrix and inhibiting an initial step in cancer metastasis and angiogenesis. A known inhibitor of superoxide dismutase, this agent can either potentiate or protect against cell oxidative damage caused by ionizing radiation, depending on the time of administration. Adjuvants, Immunologic (Code: D000276) Anti-Infective Agents (Code: D000890) Antiviral Agents (Code: D000998) Chelating Agents (Code: D002614) Immunologic Factors (Code: D007155) Sequestering Agents (Code: D064449) 1969-12-31 New Zealand Medicines and Medical Devices Safety Authority DCD
Click to view tartaric acid Tartaric acid is found in many plants such as grapes, tamarinds, pineapples, mulberries and so on. L-(+)-tartaric acid is widely used in food and beverage as acidity regulator with E number E334. Tartaric acid is used to generate carbon dioxide through interaction with sodium bicarbonate following oral administration. Carbon dioxide extends the stomach and provides a negative contrast medium during double contrast radiography. In high doses, this agent acts as a muscle toxin by inhibiting the production of malic acid, which could cause paralysis and maybe death. 1985-08-07 FDA TAR
TLA
Click to view moroxydine Moroxydine is a heterocyclic biguanidine with activity against influenza and other viral infections. Although its mechanism of action is not fully known the effects seem to be due to an influence on the virus host-cell system. bMoroxydine may be effective against a number of DNA and RNA viruses. Moroxydine is given as HCl orally or topically for treating herpes simplex and varicella-zoster infections. It is also used in the treatment of cold and influenza symptoms. Anti-Infective Agents (Code: D000890) Antiviral Agents (Code: D000998)
Click to view xylose Xylose is a sugar originally isolated from wood. Xylose is classified as a monosaccharide of the aldopentose type, which means that it contains five carbon atoms and includes a formyl functional group. Xylose is used to sweeten products intended for use by obese and diabetic customers because it is a non-caloric sweetener. D-xylose absorbtion test has been used for diagnosis of intestinal malabsorption. 1987-03-26 FDA XYP
XYS
Click to view levofacetoperane Levofacetoperane is a sympathomimetic central nervous system stimulant and is commonly used to treat depression. Levophacetoperane is also a known analeptic.
Click to view cresatin Cresatin (m-Cresyl Acetate) is the acetic acid ester of metacresol, an agent with antiseptic and analgesic properties. Cresatin is used in an otic solution to treat bacterial and fungal infections of the outer ear, and in endodontic procedures.
Click to view paroxypropione Paroxypropione is a synthetic, non-steroidal estrogen. Paroxypropione has antigonadotropin action. Paroxypropione is a product from the oxidative splitting of stilbestrol, with a low degree of estrogenicity. As the drug possesses relatively low affinity for the estrogen receptor and must be given at high dosages to achieve significant estrogenic and antigonadotropic action.
Click to view pheniprazine Amine oxidase [flavin-containing] A (Organism: Homo sapiens, class: Enzyme, accessions: P21397, gene: MAOA, swissprot: AOFA_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/17404836) Amine oxidase [flavin-containing] B (Organism: Homo sapiens, class: Enzyme, accessions: P27338, gene: MAOB, swissprot: AOFB_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/17404836) Pheniprazine is an irreversible and nonselective monoamine oxidase inhibitor (MAOI) of the hydrazine chemical class that was used as an antidepressant in the 1960s. It was also used in the treatment of angina pectoris and schizophrenia. Pheniprazine has been largely discontinued due to toxicity concerns such as jaundice, amblyopia, and optic neuritis.
Click to view ethylmethylthiambutene Ethylmethylthiambutene is a member of thiambutenes a class of opioid analgesics, around 1.3x the potency of morphine. Ethylmethylthiambutene is illegal throughout the world.
Click to view paracetamol Prostaglandin G/H synthase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P23219, gene: PTGS1, swissprot: PGH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17884974) Prostaglandin G/H synthase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P35354, gene: PTGS2, swissprot: PGH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17884974) Fatty-acid amide hydrolase 1 (Organism: Homo sapiens, class: Enzyme, accessions: O00519, gene: FAAH, swissprot: FAAH1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/22750843) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11095574) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/11811955) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11811955) Cytochrome P450 2E1 (Organism: Homo sapiens, class: Enzyme, accessions: P05181, gene: CYP2E1, swissprot: CP2E1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2010/022450lbl.pdf) Arylamine N-acetyltransferase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P11245, gene: NAT2, swissprot: ARY2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9918139) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23897240) Carbonic anhydrase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P00915, gene: CA1, swissprot: CAH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18501600) Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18501600) Carbonic anhydrase 15 (Organism: Mus musculus, class: Enzyme, accessions: Q99N23, gene: Ca15, swissprot: CAH15_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18501600) Carbonic anhydrase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P22748, gene: CA4, swissprot: CAH4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18579385) Carbonic anhydrase 3 (Organism: Homo sapiens, class: Enzyme, accessions: P07451, gene: CA3, swissprot: CAH3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18579385) Carbonic anhydrase 14 (Organism: Homo sapiens, class: Enzyme, accessions: Q9ULX7, gene: CA14, swissprot: CAH14_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18579385) Carbonic anhydrase 7 (Organism: Homo sapiens, class: Enzyme, accessions: P43166, gene: CA7, swissprot: CAH7_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18579385) Carbonic anhydrase 13 (Organism: Mus musculus, class: Enzyme, accessions: Q9D6N1, gene: Ca13, swissprot: CAH13_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18579385) Carbonic anhydrase 9 (Organism: Homo sapiens, class: Enzyme, accessions: Q16790, gene: CA9, swissprot: CAH9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18579385) Carbonic anhydrase 12 (Organism: Homo sapiens, class: Enzyme, accessions: O43570, gene: CA12, swissprot: CAH12_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18579385) Carbonic anhydrase 5A, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P35218, gene: CA5A, swissprot: CAH5A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18579385) Carbonic anhydrase 5B, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: Q9Y2D0, gene: CA5B, swissprot: CAH5B_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18579385) Carbonic anhydrase 6 (Organism: Homo sapiens, class: Enzyme, accessions: P23280, gene: CA6, swissprot: CAH6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18579385) Myoglobin (Organism: Homo sapiens, class: Unclassified, accessions: P02144, gene: MB, swissprot: MYG_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/24482730) Paracetamol (acetaminophen) is the most commonly taken analgesic worldwide and is recommended as first-line therapy in pain conditions by the World Health Organization. At normal therapeutic doses, its reactive metabolite N-acetyl-p-benzoquinone imine (NAPQI) undergoes fast conjugation with glutathione and is subsequently metabolized to produce both cysteine and mercapturic acid conjugates. High doses of acetaminophen (overdoses) can lead to hepatic necrosis due to the depletion of glutathione and of binding of high levels of reactive metabolite (NAPQI) to important parts of liver cells. Paracetamol is used for the treatment of mild to moderate pain and reduction of fever. non-narcotic analgesic (Code: CHEBI:35481) antipyretic (Code: CHEBI:35493) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Antipyretics (Code: D058633) Central Nervous System Agents (Code: D002491) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1968-11-07 FDA TYL
Click to view aminomethylbenzoic acid Solute carrier family 15 member 1 (Organism: Rattus norvegicus, class: Transporter, accessions: P51574, gene: Slc15a1, swissprot: S15A1_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9882198) Aminomethylbenzoic acid is an unnatural amino acid derivative and is an antifibrinolytic agent. It is used for the treatment of bleeding caused by hyperfibrinolysis. Antifibrinolytic Agents (Code: D000933) Coagulants (Code: D003029) Enzyme Inhibitors (Code: D004791) Fibrin Modulating Agents (Code: D050299) Hematologic Agents (Code: D006401) Hemostatics (Code: D006490) Protease Inhibitors (Code: D011480) 1983-08-04 Ministry of Health of the Russian Federation
Click to view phenicarbazide Phenicarbazide, also known as phenylsemicarbazide, is an antipyretic compound. It has analgetic and antipyretic activity. It has been withdrawn from the market on grounds of its adverse effect profile (phenicarbazide can cause hemolytic anemia in human).
Click to view phenylpropanolamine Alpha-1A adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P43140, gene: Adra1a, swissprot: ADA1A_RAT) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12238918) Alpha-1D adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P23944, gene: Adra1d, swissprot: ADA1D_RAT) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12238918) Alpha-1B adrenergic receptor (Organism: Mesocricetus auratus, class: GPCR, accessions: P18841, gene: ADRA1B, swissprot: ADA1B_MESAU) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12238918) Amine oxidase [flavin-containing] A (Organism: Homo sapiens, class: Enzyme, accessions: P21397, gene: MAOA, swissprot: AOFA_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/3961266) Amine oxidase [flavin-containing] B (Organism: Rattus norvegicus, class: Enzyme, accessions: P19643, gene: Maob, swissprot: AOFB_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/3961266) Phenylpropanolamine (norephedrine) is a sympathomimetic agent that acts as a nonselective adrenergic receptor agonist. It has been used as a decongestant and appetite suppressant. Currently, it is withdrawn from the market in Canada and the United States due to the risk for hemorrahgic strokes. The compound exists as 4 stereoisomers, which include d- and l-norephedrine and d- and l-norpseudoephedrine. Cathine (d-Phenylpropanolamine or pseudonorephedrine) is found naturally in Catha edulis. Cathine is a Schedule III drug under the Convention on Psychotropic Substances. Adrenergic Agents (Code: D018663) Adrenergic Agonists (Code: D000322) Adrenergic alpha-Agonists (Code: D000316) Anti-Obesity Agents (Code: D019440) Appetite Depressants (Code: D001067) Autonomic Agents (Code: D001337) Cardiovascular Agents (Code: D002317) Central Nervous System Agents (Code: D002491) Nasal Decongestants (Code: D014663) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Respiratory System Agents (Code: D019141) Sympathomimetics (Code: D013566) Vasoconstrictor Agents (Code: D014662) 2000-09-29 FDA NPU
Click to view hydroxyamfetamine Trace amine-associated receptor 1 (Organism: Homo sapiens, class: GPCR, accessions: Q96RJ0, gene: TAAR1, swissprot: TAAR1_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/22037049) Hydroxyamfetamine is an amphetamine metabolite with sympathomimetic effects. It is sometimes called alpha-methyltyramine, which may also refer to the meta isomer, gepefrine. Hydroxyamphetamine, when applied topically to the eye, stimulates the release of norepinephrine from postganglionic adrenergic nerves resulting in the stimulation of both alpha and beta adrenergic receptors. Local alpha stimulatory effects include dilation of the pupil, increased flow of aqueous humor, and vasoconstriction; whereas beta stimulatory effects include relaxation of the ciliary muscle and a decreased production in aqueous humor. The main use of hydroxyamphetamines as eye drops is the diagnosis of Horner's syndrome which is characterized by nerve lesions. Adrenergic Agonists (Code: N0000000122) Adrenergic Receptor Agonist (Code: N0000175883) 1969-07-16 FDA AEG
Click to view gepefrine isomer of PARA-HYDROXYAMPHETAMINE which is also called alpha-methyl-tyramine
Click to view amantadine Glutamate [NMDA] receptor (Organism: Homo sapiens, class: Ion channel, accessions: Q05586|Q12879|Q13224|Q14957|O15399|Q8TCU5|O60391, gene: GRIN1|GRIN2A|GRIN2B|GRIN2C|GRIN2D|GRIN3A|GRIN3B, swissprot: NMDZ1_HUMAN|NMDE1_HUMAN|NMDE2_HUMAN|NMDE3_HUMAN|NMDE4_HUMAN|NMD3A_HUMAN|NMD3B_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208944lbl.pdf) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208944lbl.pdf) Multidrug and toxin extrusion protein 1 (Organism: Homo sapiens, class: Transporter, accessions: Q96FL8, gene: SLC47A1, swissprot: S47A1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208944lbl.pdf) Matrix protein 2 (Organism: Influenza A virus (strain A/Udorn/307/1972 H3N2), class: Ion channel, accessions: P63231, gene: M, swissprot: M2_I72A2) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/016023s041,018101s016lbl.pdf) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12089365) Amantadine is an antiviral that is used in the prophylactic or symptomatic treatment of influenza A. The mechanisms of its effects in movement disorders are not well understood but probably reflect an increase in synthesis and release of dopamine, with perhaps some inhibition of dopamine uptake. It is also used as an antiparkinsonian agent, to treat extrapyramidal reactions, and for postherpetic neuralgia. antiviral drug (Code: CHEBI:36044) antiparkinson drug (Code: CHEBI:48407) dopaminergic agent (Code: CHEBI:48560) analgesic (Code: CHEBI:35480) non-narcotic analgesic (Code: CHEBI:35481) Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Dyskinesia Agents (Code: D018726) Anti-Infective Agents (Code: D000890) Antiparkinson Agents (Code: D000978) Antiviral Agents (Code: D000998) Central Nervous System Agents (Code: D002491) Dopamine Agents (Code: D015259) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) Influenza A M2 Protein Inhibitor (Code: N0000175543) M2 Protein Inhibitors (Code: N0000175542) 1968-02-14 FDA 308
Click to view methylparaben Carbonic anhydrase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P00915, gene: CA1, swissprot: CAH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22668600) Carbonic anhydrase 12 (Organism: Homo sapiens, class: Enzyme, accessions: O43570, gene: CA12, swissprot: CAH12_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22668600) Carbonic anhydrase 14 (Organism: Homo sapiens, class: Enzyme, accessions: Q9ULX7, gene: CA14, swissprot: CAH14_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22668600) Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22668600) Carbonic anhydrase 7 (Organism: Homo sapiens, class: Enzyme, accessions: P43166, gene: CA7, swissprot: CAH7_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22668600) Carbonic anhydrase 9 (Organism: Homo sapiens, class: Enzyme, accessions: Q16790, gene: CA9, swissprot: CAH9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22668600) Transient receptor potential cation channel subfamily A member 1 (Organism: Mus musculus, class: Unclassified, accessions: Q8BLA8, gene: Trpa1, swissprot: TRPA1_MOUSE) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/17351650) Methylparaben (E number E218) is preservative in the food, cosmetic, and pharmaceutical industries. It is completely absorbed through the skin or after ingestion and and it is hydrolyzed to para-hydroxybenzoic acid, and metabolites are rapidly excreted in the urine. Methylparaben is used in allergenic testing. Also methylparaben in combination with other drugs used for short term treatment of chronic wounds including stage III & IV pressure sores, leg ulcers. antimicrobial food preservative (Code: CHEBI:65256) neuroprotective agent (Code: CHEBI:63726) Pharmaceutic Aids (Code: D010592) Preservatives, Pharmaceutical (Code: D011310) Standardized Chemical Allergen (Code: N0000185508) Increased Histamine Release (Code: N0000175629) Cell-mediated Immunity (Code: N0000184306) Allergens (Code: N0000171131) 2010-07-06 CDSCO (INDIA) MPB
Click to view mandelic acid Mandelic Acid is an aromatic alpha hydroxy acid. In an acid urine, mandelic acid exerts its antibacterial action and also contributes to the acidification of the urine. Mandelic acid is excreted by both glomerular filtration and tubular excretion. Mandelic acid is used for the treatment of urinary tract infections. 1951-12-31 Health Canada SMN
RMN
Click to view hydroxymethylnicotinamide Hydroxymethylnicotinamide the amide derivative of nicotinic acid and formaldehyde. Has a choleretic effect, and also promotes the secretion of bile. In addition, it has a bacteriostatic and bactericidal action, which is due to the fact that during the metabolism, the formaldehyde part of the drug molecule is cleaved. The other part of the molecule (nicotinamide) has the properties of vitamin PP, increases the secretory function of the liver parenchyma, enhancing the secretion of bile and facilitating its entry into the intestine. Hydroxymethylnicotinamide is used in complex treatment violations of the liver, with cholecystitis, as well as infections of the urinary tract and gastroenteritis. It is effective in the treatment of infections caused by E. coli. 1964-04-30 Ministry of Health of the Russian Federation
Click to view tisopurine Thiopurinol inhibited aggregation of platelets induced by ADP and arachidonic acid but did not inhibit superoxide generation. Tisopurine has been shown to reduce effectively both the plasma and urinary uric acid levels of hyperexcretors, but plasma levels only of normal excretors. Tisopurine reduces uric acid concentrations by interfering with the early stages of its synthesis, thus avoiding increased blood concentrations of hypoxanthine and xanthine. Thiopurinol was used for the treatment of gout. Antirheumatic Agents (Code: D018501) Gout Suppressants (Code: D006074)
Click to view debrisoquine Amine oxidase [flavin-containing] A (Organism: Homo sapiens, class: Enzyme, accessions: P21397, gene: MAOA, swissprot: AOFA_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/2601584) Amine oxidase [flavin-containing] B (Organism: Homo sapiens, class: Enzyme, accessions: P27338, gene: MAOB, swissprot: AOFB_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/2601584) Cytochrome P450 1A1 (Organism: Homo sapiens, class: Enzyme, accessions: P04798, gene: CYP1A1, swissprot: CP1A1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12023534) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12023534) Debrisoquin is an antihypertensive drug having guanethidine-like properties. Debrisoquin acts at the sympathetic neuroeffector junction by inhibiting or interfering with the release and/or distribution of norepinephrine, rather than acting at the effector cell by inhibiting the association of norepinephrine with its receptors. Debrisoquine was used for the treatment of hypertension. Debrisoquine hydroxylation has been used test in humans to evaluate CYP2D6 activity. antihypertensive agent (Code: CHEBI:35674) adrenergic agent (Code: CHEBI:37962) sympatholytic agent (Code: CHEBI:66991) Adrenergic Agents (Code: D018663) Antihypertensive Agents (Code: D000959) Autonomic Agents (Code: D001337) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Sympatholytics (Code: D013565) 1965-01-01 YEAR INTRODUCED
Click to view mercaptopurine Solute carrier family 22 member 8 (Organism: Homo sapiens, class: Transporter, accessions: Q8TCC7, gene: SLC22A8, swissprot: S22A8_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12358729) Mercaptopurine activation occurs via hypoxanthine-guanine phosphoribosyl transferase (HGPRTase) and several enzymes to form 6-thioguanine nucleotides (6-TGNs). Incorporation of 6-TGN into nucleic acids (instead of purine bases) results in cell-cycle arrest and cell death. Mercaptopurine competes with hypoxanthine and guanine for HGPRTase and is itself converted to thioinosinic acid (TIMP). This intracellular nucleotide inhibits several reactions involving inosinic acid (IMP), including the conversion of IMP to xanthylic acid (XMP) and the conversion of IMP to adenylic acid (AMP) via adenylosuccinate (SAMP). In addition, 6-methylthioinosinate (MTIMP) is formed by the methylation of TIMP. Both TIMP and MTIMP have been reported to inhibit glutamine-5-phosphoribosylpyrophosphate amidotransferase, the first enzyme unique to the de novo pathway for purine ribonucleotide synthesis. Experiments indicate that radiolabeled mercaptopurine may be recovered from the DNA in the form of deoxythioguanosine. Some mercaptopurine is converted to nucleotide derivatives of 6-thioguanine (6-TG) by the sequential actions of inosinate (IMP) dehydrogenase and xanthylate (XMP) aminase, converting TIMP to thioguanylic acid (TGMP). antineoplastic agent (Code: CHEBI:35610) Antimetabolites (Code: D000963) Antimetabolites, Antineoplastic (Code: D000964) Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Immunologic Factors (Code: D007155) Immunosuppressive Agents (Code: D007166) Noxae (Code: D009676) Nucleic Acid Synthesis Inhibitors (Code: D019384) 1953-09-11 FDA
Click to view homocamfin Homocamfin is a stimulant. It has cardiopulmonary effect (increase output). It is no longer available.
Click to view camphor Transient receptor potential cation channel subfamily V member 1 (Organism: Rattus norvegicus, class: Unclassified, accessions: O35433, gene: Trpv1, swissprot: TRPV1_RAT) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/16192383) Transient receptor potential cation channel subfamily A member 1 (Organism: Mus musculus, class: Unclassified, accessions: Q8BLA8, gene: Trpa1, swissprot: TRPA1_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16192383) A bicyclic monoterpene ketone found widely in plants, especially cinnamomum camphora. It is used topically as a skin antipruritic and as an anti-infective agent. Anti-Infective Agents (Code: D000890) Anti-Infective Agents, Local (Code: D000891) 1970-11-12 Ministry of Health of the Russian Federation
Click to view aminosalicylic acid Dihydrofolate reductase (Organism: Mycobacterium tuberculosis, class: Enzyme, accessions: P9WNX1, gene: folA, swissprot: DYR_MYCTU) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23779105) Aminosalicylic acid is bacteriostatic against Mycobacterium tuberculosis. It inhibits the onset of bacterial resistance to streptomycin and isoniazid. The mechanism of action has been postulated to be inhibition of folic acid synthesis (but without potentiation with antifolic compounds) and/or inhibition of synthesis of the cell wall component, mycobactin, thus reducing iron uptake by M. tuberculosis. Aminosalicylic acid is indicated for the treatment of tuberculosis in combination with other active agents. It is most commonly used in patients with Multi-drug Resistant TB or in situations when therapy with isoniazid and rifampin is not possible due to a combination of resistance and/or intolerance. antitubercular agent (Code: CHEBI:33231) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Antitubercular Agents (Code: D000995) 1982-01-01 FDA BHA
Click to view mesalazine Peroxisome proliferator-activated receptor gamma (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P37231, gene: PPARG, swissprot: PPARG_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/15824083) Prostaglandin G/H synthase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P35354, gene: PTGS2, swissprot: PGH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12950415) Prostaglandin G/H synthase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P23219, gene: PTGS1, swissprot: PGH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12950415) Mitogen-activated protein kinase 1 (Organism: Homo sapiens, class: Kinase, accessions: P28482, gene: MAPK1, swissprot: MK01_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12950415) Mitogen-activated protein kinase 3 (Organism: Homo sapiens, class: Kinase, accessions: P27361, gene: MAPK3, swissprot: MK03_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12950415) Mitogen-activated protein kinase 8 (Organism: Homo sapiens, class: Kinase, accessions: P45983, gene: MAPK8, swissprot: MK08_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12950415) Arachidonate 5-lipoxygenase (Organism: Homo sapiens, class: Enzyme, accessions: P09917, gene: ALOX5, swissprot: LOX5_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/6131674) Nitric oxide synthase, inducible (Organism: Homo sapiens, class: Enzyme, accessions: P35228, gene: NOS2, swissprot: NOS2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10493988) Intermediate conductance calcium-activated potassium channel protein 4 (Organism: Homo sapiens, class: Ion channel, accessions: O15554, gene: KCNN4, swissprot: KCNN4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23516517) Mesalamine is an agent derived from sulfasalazine, an antiinflammatory agent. Mesalamine may reduce inflammation through inhibition of cyclooxygenase and prostaglandin production. Mesalamine is used for the treatment of ulcerative colitis to both induce and maintain remissions in disease. non-steroidal anti-inflammatory drug (Code: CHEBI:35475) Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) Aminosalicylate (Code: N0000175781) Aminosalicylic Acids (Code: N0000005760) 1987-12-24 FDA
Click to view octopamine Trace amine-associated receptor 1 (Organism: Homo sapiens, class: GPCR, accessions: Q96RJ0, gene: TAAR1, swissprot: TAAR1_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/18524885) Octopamine is an organic chemical closely related to norepinephrine. Octopamine exerts adrenergic effects. Octopamine is an endogenous selective beta(3)-AR agonist. In humans Octopamine is a trace amine found endogenously in the human brain where it interacts with signalling of catecholamines; it is structurally similar to synephrine and tyramine, being a metabolite of the latter (via dopamine beta-hydroxylase) and substrate for the synthesis of the former (via phenethanolamine N-methyltransferase) while being perhaps the closest in structure to noradrenaline. Octopamine is used as dietary supplements.Octopamine was used as a nootropic. All optical isomers (enantiomers) of octopamine are on the World Anti-Doping Agency (WADA) 2014 list of substances prohibited in competition. It was used for the treatment of hypotension. Adrenergic Agents (Code: D018663) Adrenergic Agonists (Code: D000322) Adrenergic alpha-Agonists (Code: D000316) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377) Vasoconstrictor Agents (Code: D014662) OTS
OTR
Click to view enbucrilate A tissue adhesive that is applied as a monomer to moist tissue and polymerizes to form a bond. It is slowly biodegradable and used in all kinds of surgery, including dental.
Click to view norfenefrine Norfenefrine (meta-octopamine) is an adrenergic agent. Along with its structural isomer p-octopamine and the tyramines, norfenefrine is a naturally occurring, endogenous trace amine and plays a role as a minor neurotransmitter in the brain. Norfenefrine is used for the treatment of acute hypotension. Adrenergic Agents (Code: D018663) Adrenergic Agonists (Code: D000322) Adrenergic alpha-Agonists (Code: D000316) Neurotransmitter Agents (Code: D018377)
Click to view dopamine D(4) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21917, gene: DRD4, swissprot: DRD4_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/17301410) D(1B) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21918, gene: DRD5, swissprot: DRD5_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/17301410) D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/17301410) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/17301410) D(1A) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21728, gene: DRD1, swissprot: DRD1_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/17301410) Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11071707) Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11071707) One of the catecholamine NEUROTRANSMITTERS in the brain. It is derived from TYROSINE and is the precursor to NOREPINEPHRINE and EPINEPHRINE. Dopamine is a major transmitter in the extrapyramidal system of the brain, and important in regulating movement. A family of receptors (RECEPTORS, DOPAMINE) mediate its action. cardiotonic drug (Code: CHEBI:38147) beta-adrenergic agonist (Code: CHEBI:35522) dopaminergic agent (Code: CHEBI:48560) sympathomimetic agent (Code: CHEBI:35524) Catecholamine (Code: N0000175570) Catecholamines (Code: N0000007715) Autonomic Agents (Code: D001337) Cardiotonic Agents (Code: D002316) Cardiovascular Agents (Code: D002317) Dopamine Agents (Code: D015259) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Protective Agents (Code: D020011) Sympathomimetics (Code: D013566) 1974-02-25 FDA LDP
Click to view gentisic acid Carbonic anhydrase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P00915, gene: CA1, swissprot: CAH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22668600) Carbonic anhydrase 12 (Organism: Homo sapiens, class: Enzyme, accessions: O43570, gene: CA12, swissprot: CAH12_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22668600) Carbonic anhydrase 14 (Organism: Homo sapiens, class: Enzyme, accessions: Q9ULX7, gene: CA14, swissprot: CAH14_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22668600) Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22668600) Carbonic anhydrase 7 (Organism: Homo sapiens, class: Enzyme, accessions: P43166, gene: CA7, swissprot: CAH7_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22668600) Carbonic anhydrase 9 (Organism: Homo sapiens, class: Enzyme, accessions: Q16790, gene: CA9, swissprot: CAH9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22668600) Gentisic acid is a dihydroxybenzoic acid. Gentisic acid is an active metabolite of salicylic acid degradation. Gentisic acid is also a byproduct of tyrosine and benzoate metabolism. The antioxidant activity and radioprotective properties of gentisic acid are exerted by its phenoxyl group. It is also used in cosmetics as a skin-whitening agent for the treatment of skin pigmentary disorders by influencing the synthesis of melanin through inhibition of melanosomal tyrosinase activity. In the laboratory, it is used as a sample matrix in matrix-assisted laser desorption/ionization (MALDI) mass spectrometry, and has been shown to conveniently detect peptides incorporating the boronic acid moiety by MALDI. MALDI matrix material (Code: CHEBI:64345) GTQ
Click to view acipimox Hydroxycarboxylic acid receptor 2 (Organism: Homo sapiens, class: GPCR, accessions: Q8TDS4, gene: HCAR2, swissprot: HCAR2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12522134) Acipimox is a niacin derivative used as a hypolipidemic agent. It is used in low doses and may have less marked adverse effects, although it is unclear whether the recommended dose is as effective as are standard doses of nicotinic acid. Acipimox inhibits the production of triglycerides by the liver and the secretion of VLDL, which leads indirectly to a modest reduction in LDL and increase in HDL. Long-term administration is associated with reduced mortality, but unwanted effects limit its clinical use. Acipimox is indicated as alternative or adjunct treatment to reduce triglyceride levels in patients who have not responded adequately to other treatments such as statin or fibrate treatment for hypertriglyceridaemia (Fredrickson type IV hyperlipoproteinaemia) or hypercholesterolaemia and hypertriglyceridaemia (Fredrickson type IIB hyperlipoproteinaemia). Antimetabolites (Code: D000963) Hypolipidemic Agents (Code: D000960) Lipid Regulating Agents (Code: D057847) 1991-01-16 Austrian Medicines and Medical Devices Agency
Click to view guancidine Guancidine is an antihypertensive agent.
Click to view allomethadione Allomethadione (aloxidone) is an anticonvulsivant N-allyl derivatives of hydantoin. It was used for the treatment of epilepsy.
Click to view chlorphenesin carbamate A centrally acting muscle relaxant. Its mode of action is unknown. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1203) muscle relaxant (Code: CHEBI:51371) Central Nervous System Agents (Code: D002491) Muscle Relaxants, Central (Code: D009125) Neuromuscular Agents (Code: D009465) Peripheral Nervous System Agents (Code: D018373) 1965-06-14 FDA
Click to view histidine Histidine decarboxylase (Organism: Homo sapiens, class: Enzyme, accessions: P19113, gene: HDC, swissprot: DCHS_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/17965265) Carbonic anhydrase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P00915, gene: CA1, swissprot: CAH1_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/17499996) Carbonic anhydrase 6 (Organism: Homo sapiens, class: Enzyme, accessions: P23280, gene: CA6, swissprot: CAH6_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/17499996) Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/17499996) Carbonic anhydrase 3 (Organism: Homo sapiens, class: Enzyme, accessions: P07451, gene: CA3, swissprot: CAH3_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/18627905) Carbonic anhydrase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P22748, gene: CA4, swissprot: CAH4_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/18627905) Carbonic anhydrase 14 (Organism: Homo sapiens, class: Enzyme, accessions: Q9ULX7, gene: CA14, swissprot: CAH14_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/17540561) Carbonic anhydrase 7 (Organism: Homo sapiens, class: Enzyme, accessions: P43166, gene: CA7, swissprot: CAH7_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/17540561) Carbonic anhydrase 12 (Organism: Homo sapiens, class: Enzyme, accessions: O43570, gene: CA12, swissprot: CAH12_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/18294854) Carbonic anhydrase 9 (Organism: Homo sapiens, class: Enzyme, accessions: Q16790, gene: CA9, swissprot: CAH9_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/18294854) Solute carrier family 15 member 4 (Organism: Homo sapiens, class: Transporter, accessions: Q8N697, gene: SLC15A4, swissprot: S15A4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/16289537) Solute carrier family 15 member 3 (Organism: Rattus norvegicus, class: Transporter, accessions: Q924V4, gene: Slc15a3, swissprot: S15A3_RAT) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11336635) Carbonic anhydrase 13 (Organism: Mus musculus, class: Enzyme, accessions: Q9D6N1, gene: Ca13, swissprot: CAH13_MOUSE) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/16730978) Carbonic anhydrase 15 (Organism: Mus musculus, class: Enzyme, accessions: Q99N23, gene: Ca15, swissprot: CAH15_MOUSE) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/19464888) Carbonic anhydrase (Organism: Candida albicans (strain SC5314 / ATCC MYA-2876), class: Enzyme, accessions: Q5AJ71, gene: NCE103, swissprot: CAN_CANAL) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/20061162) Histidine is an essential amino acid. L-histidine is converted to histamine by histidine decarboxylase, a pyridoxal 5'-phosphate-dependent enzyme. The efficacy of L-histidine in protecting inflamed tissue is attributed to the capacity of the imidazole ring to scavenge reactive oxygen species generated by cells during acute inflammatory response. Histidine, when administered in therapeutic quantities is able to inhibit cytokines and growth factors involved in cell and tissue damage. 1975 FDA DHI
HIS
Click to view bemegride Bemegride is a CNS stimulant that is used to induce convulsions in experimental animals. It has also been used as a respiratory stimulant and in the treatment of barbiturate overdose. Central Nervous System Agents (Code: D002491) Central Nervous System Stimulants (Code: D000697) Convulsants (Code: D003292) Respiratory System Agents (Code: D019141) 1970-03-30 Ministry of Health of the Russian Federation
Click to view valdetamide Sedative
Click to view propylhexedrine Propylhexedrine is considered to be an agonist of alpha-adrenergic receptors. Exact mechanism of action unknown but thought to be similar to amphetamine. It is used for temporary symptomatic relief of nasal decongestion due to colds, allergies and allergic rhinitis.
Click to view pempidine A nicotinic antagonist most commonly used as an experimental tool. It has been used as a ganglionic blocker in the treatment of hypertension but has largely been supplanted for that purpose by more specific drugs. Antihypertensive Agents (Code: D000959) Autonomic Agents (Code: D001337) Cardiovascular Agents (Code: D002317) Cholinergic Agents (Code: D018678) Cholinergic Antagonists (Code: D018680) Ganglionic Blockers (Code: D005730) Neurotransmitter Agents (Code: D018377) Nicotinic Antagonists (Code: D018733) Peripheral Nervous System Agents (Code: D018373)
Click to view bucolome Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10497145) Bucolome (Paramidine) is a barbiturate derivative. It is a non-steroidal anti-inflammatory drug. It has been used as a uricosuric and/or anti-inflammatory agent. Bucolome is used to treatment inflammation, pain, fever in rheumatoid arthritis, osteoarthritis, cystitis, erythema multiforme, acute sinusitis, otitis media, appendicitis and for the treatment of gout hyperuricemia. 1989-01-01 PMDA
Click to view mechlorethamine Mechlorethamine, also known as nitrogen mustard, is an alkylating agent which inhibits rapidly proliferating cells. Nitrogen mustard (a member of a family of chemotherapy agents including cyclophosphamide and chlorambucil) is an irritant and carcinogenic agent metabolized to a highly reactive ethylene immonium derivative; the ethylene immonium derivative alkylates DNA and inhibits DNA replication. This agent also exhibits lympholytic properties. Mechlorethamine has been in clinical use for more than 60 years, given systemically in combination with other antineoplastic agents to treat Hodgkin disease, chronic leukemias, lung cancer and polycythemia vera. Currently, however, it is used largely as a topical gel for therapy of cutaneous T-cell lymphomas and mycosis fungoides. Alkylating Activity (Code: N0000000236) Alkylating Drug (Code: N0000175558) Alkylating Agents (Code: D000477) Antineoplastic Agents (Code: D000970) Antineoplastic Agents, Alkylating (Code: D018906) Chemical Warfare Agents (Code: D002619) Irritants (Code: D007509) Noxae (Code: D009676) Poisons (Code: D011042) 1949-03-15 FDA
Click to view orotic acid Uridine 5'-monophosphate synthase (Organism: Homo sapiens, class: Enzyme, accessions: P11172, gene: UMPS, swissprot: UMPS_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/26059769) Orotic acid appears as minor dietary constituent. Indeed, until it was realized that it could be synthesized by humans, orotic acid was known as vitamin B-13. but it is now known that it is not a vitamin and is synthesized in the body, where it arises as an intermediate in the pathway for the synthesis of pyrimidine nucleotides. The richest dietary sources of orotic acid are cow's milk and other dairy products as well as root vegetables such as carrots and beets. Orotic acid levels are elevated in the urea cycle defects ornithine transcarbamylase (OTC) deficiency, citrullinemia and argininosuccinic acidemia, as well as the mitochondrial transport disorder hyperornithinemia-hyperammonemia-homocitrullinuria (HHH) syndrome. 1968-04-30 Ministry of Health of the Russian Federation ORO
Click to view nifuroxime Nifuroxime is anti-infective agent used in protozoal and fungal infections. It works by adsorbing (binding) large numbers of bacteria and toxins and reducing the loss of water. Nifuroxime has been withdrawm from the market in many countries.
Click to view diethadione Diethadione is an analeptics with a strong stimulating action on the CNS and especially on the respiratory center.
Click to view ectylurea Ectylurea (2-ethyl-cis crotonylurea) is a sedative and psychotherapeutic drug that produces mild depression of the central nervous system, an action shared with other substituted urea compounds. It was used for the treatment of anxiety and tension. 1956 YEAR INTRODUCED
Click to view iprazochrome used in prophylaxis of migraine Neurotransmitter Agents (Code: D018377) Serotonin Agents (Code: D018490) Serotonin Antagonists (Code: D012702)
Click to view chloroxylenol Chloroxylenol (para-chloro-meta-xylenol) is an antiseptic and disinfectant agent. It is bactericidal against most Gram-positive bacteria but less effective against Staphylococci and Gram-negative bacteria, and often inactive against Pseudomonas species. It is ineffective against bacterial spores. The hydroxyl -OH groups of the chloroxylenol molecule binds to certain proteins on the cell membrane of bacteria, and disrupts the membrane. This allows chloroxylenol to enter the bacterial cell to bind further with more proteins and enzymes. At particularly high concentrations of chloroxylenol, the protein and nucleic acid content of targeted bacterial cells become coagulated and cease to function, leading to rapid cell death. Chloroxylenol is used for cleaning and disinfecting wounds, abrasions and abscesses, for minor cuts and scratches, insect bites, burns, inflammation of the skin. It is also found in hair conditioners, toilet cleaners, deodorants, soaps and paste. molluscicide (Code: CHEBI:33904) antiseptic drug (Code: CHEBI:48218) Anthelmintics (Code: D000871) Anti-Infective Agents (Code: D000890) Anti-Infective Agents, Local (Code: D000891) Antiparasitic Agents (Code: D000977) Antiplatyhelmintic Agents (Code: D000980) Disinfectants (Code: D004202) Schistosomicides (Code: D012556) 1951-12-31 Health Canada
Click to view oteracil Uridine 5'-monophosphate synthase (Organism: Homo sapiens, class: Enzyme, accessions: P11172, gene: UMPS, swissprot: UMPS_HUMAN) inhibitor (Source: https://www.ema.europa.eu/documents/product-information/teysuno-epar-product-information_en.pdf) Oteracil is an orotate phosphoribosyltransferase (OPRT) inhibitor that decreases the activity of 5-fluorouracil in normal gastrointestinal mucosa. It is used in combination with Gimeracil and Tegafur as an adjunct to antineoplastic therapy, used to reduce the toxic side effects associated with chemotherapy. 2011-03-14 EMA
Click to view furamicid Furamicid (2-methoxymethyl-5-nitrofuran) is an derivative of 5-nitrofuran and an antifungal agent.
Click to view paramethadione Paramethadione is an anticonvulsant in the oxazolidinedione class. Paramethadione acts to reduce T-type calcium currents in thalamic neurons. Paramethadione is used for the control of absence (petit mal) seizures that are refractory to treatment with other medications. 1949-06-15 FDA
Click to view nitrefazole Nitrefazole is a nitroimidazole derivative with the ability to inhibit aldehyde dehydrogenase. Nitrefazole was used in the treatment of alcoholism and withdrawn following reports of hepatotoxicity.
Click to view ethadione Ethadione is an oxazolidine derivative and an anticonvulsant. Ethadione was used as an anti-seizure preparation.
Click to view tranexamic acid Plasminogen (Organism: Homo sapiens, class: Enzyme, accessions: P00747, gene: PLG, swissprot: PLMN_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/019281s041lbl.pdf) Tranexamic Acid is a synthetic derivative of the amino acid lysine with antifibrinolytic activity. With strong affinity for the five lysine-binding sites of plasminogen, tranexamic acid competitively inhibits the activation of plasminogen to plasmin, resulting in inhibition of fibrinolysis; at higher concentrations, this agent noncompetitively inhibits plasmin. This agent has a longer half-life, is approximately ten times more potent, and is less toxic than aminocaproic acid, which possesses similar mechanisms of action. Tranexamic Acid is indicated in patients with hemophilia for short-term use (two to eight days) to reduce or prevent hemorrhage and reduce the need for replacement therapy during and following tooth extraction. hematologic agent (Code: CHEBI:50248) antifibrinolytic drug (Code: CHEBI:48675) Antifibrinolytic Agent (Code: N0000175634) Decreased Fibrinolysis (Code: N0000175632) Antifibrinolytic Agents (Code: D000933) Coagulants (Code: D003029) Fibrin Modulating Agents (Code: D050299) Hematologic Agents (Code: D006401) Hemostatics (Code: D006490) 1986-12-30 FDA AMH
Click to view oxanamide Oxanamide is a central nervous system depressant resembling short-acting barbiturates. The exact mechanism of action of oxanamide is unknown.
Click to view buformin Solute carrier family 22 member 1 (Organism: Rattus norvegicus, class: Transporter, accessions: Q63089, gene: Slc22a1, swissprot: S22A1_RAT) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12130709) Buformin is an agent belonging to the biguanide class of antidiabetics with antihyperglycemic activity. Buformin exerts its activity via activation of AMPK and inhibition of the mTOR signaling pathways. Buformin is used for the treatment of type 2 diabetes mellitus. Buformin was withdrawn from the market in many countries due to an elevated risk of causing lactic acidosis. Hypoglycemic Agents (Code: D007004) 2007-09-14 PMDA
Click to view isovaleryl diethylamide -
Click to view methylphenidate Sodium-dependent dopamine transporter (Organism: Homo sapiens, class: Transporter, accessions: Q01959, gene: SLC6A3, swissprot: SC6A3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17228864) Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17228864) Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) (Source: https://www.ncbi.nlm.nih.gov/pubmed/17228864) Liver carboxylesterase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P23141, gene: CES1, swissprot: EST1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15082749) Methylphenidate is a central nervous system (CNS) stimulant. Methylphenidate is thought to block the reuptake of norepinephrine and dopamine into the presynaptic neuron and increase the release of these monoamines into the extraneuronal space.Methylphenidate is a racemic mixture comprised of the d-and l-threo enantiomers. The d-threo enantiomer is more pharmacologically active than the l-threo enantiomer. Methylphenidate is indicated for the treatment of attention deficit hyperactivity disorder and narcolepsy. adrenergic agent (Code: CHEBI:37962) adrenergic uptake inhibitor (Code: CHEBI:35640) dopamine uptake inhibitor (Code: CHEBI:51039) central nervous system stimulant (Code: CHEBI:35337) sympathomimetic agent (Code: CHEBI:35524) psychotropic drug (Code: CHEBI:35471) Central Nervous System Agents (Code: D002491) Central Nervous System Stimulants (Code: D000697) Dopamine Agents (Code: D015259) Dopamine Uptake Inhibitors (Code: D018765) Membrane Transport Modulators (Code: D049990) Neurotransmitter Agents (Code: D018377) Neurotransmitter Uptake Inhibitors (Code: D014179) Central Nervous System Stimulation (Code: N0000175729) methylphenidate: 1955-12-05 FDA dexmethylphenidate: 2001-11-13 FDA
Click to view oxiracetam Oxiracetam is an ampakine of the nootropic racetam chemical class. Oxiracetam is a positive AMPA modulator similar in mechanism and potency (but not the binding site) to both piracetam and aniracetam but may have an additional benefit of increasing glutamate, acetylcholine, and D-aspartic acid release from activated but not resting neurons. Oxiracetam has been proved as an efficient memory enhancer if taken consistently. Thus, the drug enhances an overall quality of life of patients suffering from ADHD, dementia, and other neurological problems. Central Nervous System Agents (Code: D002491) Nootropic Agents (Code: D018697) Psychotropic Drugs (Code: D011619) 1988 Italian Medicines Agency (AIFA)
Click to view tiliquinol Catechol O-methyltransferase (Organism: Rattus norvegicus, class: Enzyme, accessions: P22734, gene: Comt, swissprot: COMT_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/817025) Tiliquinol is an antiprotozoal agent that is used in combination with tibroquinol. The combination agent was withdrawn in some countries because of hepatoxicity. 1997-06-30 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view citiolone Citiolone is a derivative of the amino acid cysteine.Citiolone is a mucolytic agent. Citiolone is used for the treatment of hepatic disorders. 1976 Italian Medicines Agency (AIFA)
Click to view pregabalin Voltage-dependent calcium channel subunit alpha-2/delta-1 (Organism: Homo sapiens, class: Ion channel, accessions: P54289, gene: CACNA2D1, swissprot: CA2D1_HUMAN) modulator (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021446s036,022488s014lbl.pdf) Voltage-dependent calcium channel subunit alpha-2/delta-2 (Organism: Homo sapiens, class: Ion channel, accessions: Q9NY47, gene: CACNA2D2, swissprot: CA2D2_HUMAN) modulator (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021446s036,022488s014lbl.pdf) Large neutral amino acids transporter small subunit 1 (Organism: Homo sapiens, class: Transporter, accessions: Q01650, gene: SLC7A5, swissprot: LAT1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021446s036,022488s014lbl.pdf) Pregabalin is a 3-isobutyl derivative of gamma-amino butyric acid (GABA) with anti-convulsant, anti-epileptic, anxiolytic, and analgesic activities. Pregabalin binds with high affinity to the alpha2-delta site of voltage-gated calcium channels in central nervous system tissues. Pregabalin is indicated for the treatment neuropathic pain associated with diabetic peripheral neuropathy, postherpetic neuralgia, fibromyalgia, neuropathic pain associated with spinal cord injury and for adjunctive therapy for patients with partial onset seizures. anticonvulsant (Code: CHEBI:35623) Analgesics (Code: D000700) Anti-Anxiety Agents (Code: D014151) Anticonvulsants (Code: D000927) Calcium Channel Blockers (Code: D002121) Cardiovascular Agents (Code: D002317) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Membrane Transport Modulators (Code: D049990) Peripheral Nervous System Agents (Code: D018373) Psychotropic Drugs (Code: D011619) Sensory System Agents (Code: D018689) Tranquilizing Agents (Code: D014149) 2004-07-06 EMA
Click to view pargyline Pargyline is a monoamine oxidase (MAO) inhibitor with antidepressant activity. Pargyline selectively inhibits MAO type B, an enzyme catalyzing the oxidative deamination and inactivation of certain catecholamines, such as norepinephrine and dopamine, within the presynaptic nerve terminals. By inhibiting the metabolism of these biogenic amines in the brain, pargyline increases their concentration and binding to postsynaptic receptors. Increased receptor stimulation may cause downregulation of central receptors which may attribute to pargyline's antidepressant effect. It was approved for the treatment hypertension, but then this drug was discontinued. Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Enzyme Inhibitors (Code: D004791) Monoamine Oxidase Inhibitors (Code: D008996) 1982-01-01 FDA
Click to view methylchromone Methylchromone (3-methylchromone) is the first synthetic chromone to be used clinically. It has both antispasmodic and coronary vasodilator actions. It was recommended for the treatment of angina pectoris but it doesn’t produce any remarkable improvements and its clinical use has been discontinued.
Click to view hydralazine Myeloperoxidase (Organism: Homo sapiens, class: Enzyme, accessions: P05164, gene: MPO, swissprot: PERM_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/28197313) Hydralazine is a selective dilator of arterial smooth muscle. Animal data suggests that hydralazine may also mitigate tolerance to nitrates. It inhibits membrane-bound enzymes that form reactive oxygen species, such as superoxides. Excessive superoxide counteracts NO-induced vasodilation. Hydralazine is used for the treatment of essential hypertension, alone or as an adjunct. Also for the management of severe hypertension when the drug cannot be given orally or when blood pressure must be lowered immediately, congestive heart failure (in combination with cardiac glycosides and diuretics and/or with isosorbide dinitrate), and hypertension secondary to pre-eclampsia/eclampsia. antihypertensive agent (Code: CHEBI:35674) vasodilator agent (Code: CHEBI:35620) Arteriolar Vasodilation (Code: N0000175379) Arteriolar Vasodilator (Code: N0000175564) Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Vasodilator Agents (Code: D014665) 1953-01-15 FDA HLZ
Click to view tolazoline Alpha-2C adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18825, gene: ADRA2C, swissprot: ADA2C_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9605427) Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9605427) Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9605427) Tolazoline is a vasodilator that apparently has direct actions on blood vessels and also increases cardiac output. Tolazoline can interact to some degree with histamine, adrenergic, and cholinergic receptors, but the mechanisms of its therapeutic effects are not clear. It is used in treatment of persistent pulmonary hypertension of the newborn. alpha-adrenergic antagonist (Code: CHEBI:37890) antihypertensive agent (Code: CHEBI:35674) vasodilator agent (Code: CHEBI:35620) Adrenergic Agents (Code: D018663) Adrenergic alpha-Antagonists (Code: D000317) Adrenergic Antagonists (Code: D018674) Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377) Vasodilator Agents (Code: D014665) 1948-03-17 FDA
Click to view methacholine Muscarinic acetylcholine receptor M1 (Organism: Rattus norvegicus, class: GPCR, accessions: P08482, gene: Chrm1, swissprot: ACM1_RAT) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9622546) Muscarinic acetylcholine receptor M3 (Organism: Rattus norvegicus, class: GPCR, accessions: P08483, gene: Chrm3, swissprot: ACM3_RAT) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9622546) Methacholine is a parasympathomimetic (cholinergic) bronchoconstrictor agent. Methacholine agonizes the muscarinic receptors which eventually induce bronchoconstriction. It is hydrolyzed by acetylcholinesterase at a considerably slower rate than acetylcholine and is more resistant to hydrolysis by nonspecific cholinesterases so that its actions are more prolonged. Methacholine is indicated for the diagnosis of bronchial airway hyperreactivity (methacholine challenge test). muscarinic agonist (Code: CHEBI:38325) bronchoconstrictor agent (Code: CHEBI:50141) cholinergic agonist (Code: CHEBI:38324) vasodilator agent (Code: CHEBI:35620) Cholinergic Receptor Agonist (Code: N0000175884) Autonomic Agents (Code: D001337) Bronchoconstrictor Agents (Code: D016085) Cholinergic Agents (Code: D018678) Cholinergic Agonists (Code: D018679) Miotics (Code: D008916) Muscarinic Agonists (Code: D018721) Neurotransmitter Agents (Code: D018377) Parasympathomimetics (Code: D010277) Peripheral Nervous System Agents (Code: D018373) Respiratory System Agents (Code: D019141) 1986-10-31 FDA
Click to view carpronium a hair growth reagent with a vasodilatory action. Carpronium chloride has local vasodilating effect and hair growth stimulatory effect to improve alopecia and vitiligo. It is usually used for the prevention of hair loss, for hair growth stimulation, and in the treatment of seborrhea sicca and vitiligo vulgaris. 1987 PMDA
Click to view clomethiazole Cytochrome P450 2A6 (Organism: Homo sapiens, class: Enzyme, accessions: P11509, gene: CYP2A6, swissprot: CP2A6_HUMAN) inhibitor (Source: https://mhraproductsprod.blob.core.windows.net/docs/d6d032495d6cf95a02c5f40d74aa45e2559809fd) Cytochrome P450 2E1 (Organism: Homo sapiens, class: Enzyme, accessions: P05181, gene: CYP2E1, swissprot: CP2E1_HUMAN) inhibitor (Source: https://mhraproductsprod.blob.core.windows.net/docs/d6d032495d6cf95a02c5f40d74aa45e2559809fd) Clomethiazole is a short acting hypnotic and sedative with anticonvulsant effect. Clomethiazole interacts with the picrotoxin/barbiturate site of the GABAA-receptor-chloride channel complex. It is used for the management of restlessness and agitation in the elderly, short term treatment of severe insomnia in the elderly and treatment of alcohol withdrawal symptoms where close hospital supervision is also provided. Anticonvulsants (Code: D000927) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) GABA Agents (Code: D018682) GABA Modulators (Code: D018757) Hypnotics and Sedatives (Code: D006993) Neuroprotective Agents (Code: D018696) Neurotransmitter Agents (Code: D018377) Protective Agents (Code: D020011) 1968-05-01 Spanish Agency of Medicines and Medical Products (AEMPS)
Click to view meglutol Meglutol (3-Hydroxy-3-methylglutaric acid, HMGA) is an antilipemic agent which lowers cholesterol, triglycerides, serum beta-lipoproteins and phospholipids, and inhibits the activity of hydroxymethylglutaryl CoA reductases, which is the rate limiting enzyme in the biosynthesis of cholesterol. It acts by interfering with the enzymatic steps involved in the conversion of acetate to hydroxymethylglutaryl coenzyme A. Meglutol is used as a hypolipidaemic agent. anticholesteremic drug (Code: CHEBI:35821) Anticholesteremic Agents (Code: D000924) Antimetabolites (Code: D000963) Enzyme Inhibitors (Code: D004791) Hydroxymethylglutaryl-CoA Reductase Inhibitors (Code: D019161) Hypolipidemic Agents (Code: D000960) Lipid Regulating Agents (Code: D057847) 1983 Italian Medicines Agency (AIFA) MAH
Click to view fenadiazole Fenadiazole is a hypnotic drug with a unique oxadiazole-based structure.
Click to view aminorex An amphetamine-like anorectic agent. It may cause pulmonary hypertension.
Click to view levocarnitine Carnitine O-palmitoyltransferase 1, liver isoform (Organism: Homo sapiens, class: Enzyme, accessions: P50416, gene: CPT1A, swissprot: CPT1A_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/16362726) Levocarnitine is an amino acid derivative. Levocarnitine facilitates long-chain fatty acid entry into mitochondria, delivering substrate for oxidation and subsequent energy production. antilipemic drug (Code: CHEBI:35679) nutraceutical (Code: CHEBI:50733) nootropic agent (Code: CHEBI:66980) Carnitine (Code: N0000006688) Carnitine Analog (Code: N0000175903) 1985-12-27 FDA DCK
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Click to view oxydibutanol Oxydibutanol is an choleretic and spasmolytic agent. It is used for the treatment of constipation.
Click to view nicotine Neuronal acetylcholine receptor; alpha2/beta4 (Organism: Homo sapiens, class: Ion channel, accessions: Q15822|P30926, gene: CHRNA2|CHRNB4, swissprot: ACHA2_HUMAN|ACHB4_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/20081230) Neuronal acetylcholine receptor; alpha3/beta2 (Organism: Homo sapiens, class: Ion channel, accessions: P32297|P17787, gene: CHRNA3|CHRNB2, swissprot: ACHA3_HUMAN|ACHB2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/20081230) Neuronal acetylcholine receptor; alpha3/beta4 (Organism: Homo sapiens, class: Ion channel, accessions: P32297|P30926, gene: CHRNA3|CHRNB4, swissprot: ACHA3_HUMAN|ACHB4_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/20081230) Neuronal acetylcholine receptor; alpha4/beta2 (Organism: Homo sapiens, class: Ion channel, accessions: P43681|P17787, gene: CHRNA4|CHRNB2, swissprot: ACHA4_HUMAN|ACHB2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/20081230) Neuronal acetylcholine receptor; alpha4/beta4 (Organism: Homo sapiens, class: Ion channel, accessions: P43681|P30926, gene: CHRNA4|CHRNB4, swissprot: ACHA4_HUMAN|ACHB4_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/20081230) Neuronal acetylcholine receptor subunit alpha-7 (Organism: Homo sapiens, class: Ion channel, accessions: P36544, gene: CHRNA7, swissprot: ACHA7_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/20081230) Transient receptor potential cation channel subfamily A member 1 (Organism: Homo sapiens, class: Ion channel, accessions: O75762, gene: TRPA1, swissprot: TRPA1_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/19749751) Cytochrome P450 2A6 (Organism: Homo sapiens, class: Enzyme, accessions: P11509, gene: CYP2A6, swissprot: CP2A6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/22864238/) Cytochrome P450 2A13 (Organism: Homo sapiens, class: Enzyme, accessions: Q16696, gene: CYP2A13, swissprot: CP2AD_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/22864238/) Nicotine is a plant alkaloid, found in the tobacco plant, and addictive central nervous system (CNS) stimulant that causes either ganglionic stimulation in low doses or ganglionic blockage in high doses. Nicotine acts as an agonist at the nicotinic cholinergic receptors in the autonomic ganglia, at neuromuscular junctions, and in the adrenal medulla and the brain. Nicotine's CNS-stimulating activities may be mediated through the release of several neurotransmitters, including acetylcholine, beta-endorphin, dopamine, norepinephrine, serotonin, and ACTH. As a result, peripheral vasoconstriction, tachycardia, and elevated blood pressure may be observed with nicotine intake. This agent may also stimulate the chemoreceptor trigger zone, thereby inducing nausea and vomiting. biomarker (Code: CHEBI:59163) immunomodulator (Code: CHEBI:50846) peripheral nervous system drug (Code: CHEBI:49110) psychotropic drug (Code: CHEBI:35471) anxiolytic drug (Code: CHEBI:35474) nicotinic acetylcholine receptor agonist (Code: CHEBI:47958) phytogenic insecticide (Code: CHEBI:22917) Cholinergic Nicotinic Agonist (Code: N0000175706) Nicotine (Code: N0000006496) Autonomic Agents (Code: D001337) Cholinergic Agents (Code: D018678) Cholinergic Agonists (Code: D018679) Ganglionic Stimulants (Code: D005731) Neurotransmitter Agents (Code: D018377) Nicotinic Agonists (Code: D018722) Peripheral Nervous System Agents (Code: D018373) 1991-11-07 FDA NCT
Click to view carsalam Carsalam is a cyclised carbamyl derivative of salicylamide. Carsalam was used as a nonsteroidal anti-inflammatory drug.
Click to view tiopronin Tiopronin is N-(2-Mercaptopropionyl) glycine which is is a reducing and cystine-binding thiol drug. Tiopronin is an active reducing agent which undergoes thiol-disulfide exchange with cystine to form a mixed disulfide of tiopronin-cysteine. From this reaction, a water-soluble mixed disulfide is formed and the amount of sparingly soluble cystine is reduced. Tiopronin is indicated, in combination with high fluid intake, alkali, and diet modification, for the prevention of cystine stone formation in patients with severe homozygous cystinuria, who are not responsive to these measures alone. Cystine Disulfide Reduction (Code: N0000175549) N-substituted Glycines (Code: N0000011378) Reducing and Complexing Thiol (Code: N0000175898) 1988-08-11 FDA WJZ
Click to view acetylcysteine Acetylcysteine is the N-acetyl derivative of the naturally occurring amino acid, L-cysteine. Acetylcysteine has been shown to reduce the extent of liver injury following acetaminophen overdose. Acetylcysteine is essentially a prodrug that is converted to cysteine (in the intestine by the enzyme aminoacylase 1) and absorbed in the intestine into the blood stream. Acetylcysteine also used as a mucolytic. (See: cysteine) antidote to paracetamol poisoning (Code: CHEBI:74529) antiinfective agent (Code: CHEBI:35441) antiviral drug (Code: CHEBI:36044) mucolytic (Code: CHEBI:77034) vulnerary (Code: CHEBI:73336) Antidote (Code: N0000175429) Antidote for Acetaminophen Overdose (Code: N0000175961) Decreased Respiratory Secretion Viscosity (Code: N0000008867) Increased Glutathione Concentration (Code: N0000175960) Reduction Activity (Code: N0000175547) Anti-Infective Agents (Code: D000890) Antioxidants (Code: D000975) Antiviral Agents (Code: D000998) Expectorants (Code: D005100) Free Radical Scavengers (Code: D016166) Respiratory System Agents (Code: D019141) 1963-09-14 FDA SC2
1ZT
Click to view cloforex carbamic ethyl ester of chlorphentermine; structure in Negwer, 5th ed, #2275
Click to view pentorex Pentorex is a phenyl-isopropylamone derivative and has an anorexigenous activity. It was used to assist with weight loss.
Click to view mephentermine Mephentermine is an amphetamine-derived phenethylamine. It is an alpha 1 adrenergic receptor agonist and a hypertensive drug. Mephentermine is mainly used as a vasopressor agent with a sympathomimetic action, primarily causing release of noradrenaline and increasing cardiac output due to positive inotropic effect on the myocardium. Adrenergic Agents (Code: D018663) Adrenergic Agonists (Code: D000322) Adrenergic alpha-1 Receptor Agonists (Code: D058646) Adrenergic alpha-Agonists (Code: D000316) Autonomic Agents (Code: D001337) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Sympathomimetics (Code: D013566) Vasoconstrictor Agents (Code: D014662) 1951-12-29 FDA
Click to view etilamfetamine Etilamfetamine is an amphetamine analog and was used as an appetite suppressant in the 1950s. Etilamfetamine is prohibited by WADAas a stimulant.
Click to view phenylbutanoic acid phenylbutanoic acid: Histone deacetylase 8 (Organism: Homo sapiens, class: Enzyme, accessions: Q9BY41, gene: HDAC8, swissprot: HDAC8_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21874153) Histone deacetylase 1 (Organism: Homo sapiens, class: Enzyme, accessions: Q13547, gene: HDAC1, swissprot: HDAC1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21874153) Histone deacetylase 2 (Organism: Homo sapiens, class: Enzyme, accessions: Q92769, gene: HDAC2, swissprot: HDAC2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21874153) Histone deacetylase 3 (Organism: Homo sapiens, class: Enzyme, accessions: O15379, gene: HDAC3, swissprot: HDAC3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21874153) Histone deacetylase 6 (Organism: Homo sapiens, class: Enzyme, accessions: Q9UBN7, gene: HDAC6, swissprot: HDAC6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21874153) Dihydroneopterin aldolase (Organism: Paracoccus denitrificans, class: Enzyme, accessions: P95468, gene: tyrB, swissprot: TYRB_PARDE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9930977) phenylacetate: glutamine (Organism: None, class: Amino acid, accessions: None, gene: None, swissprot: None) Binding Agent (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020572s016,020573s015lbl.pdf) Phenylbutanoic acid is a pro-drug and is rapidly metabolized to phenylacetate. Phenylacetate is a metabolically-active compound that conjugates with glutamine via acetylation to form phenylacetylglutamine which is excreted by the kidneys. On a molar basis, phenylacetylglutamine, like urea, contains 2 moles of nitrogen and provides an alternate vehicle for waste nitrogen excretion. Phenylbutanoic acid is indicated as adjunctive therapy in the chronic management of patients with urea cycle disorders involving deficiencies of carbamylphosphate synthetase (CPS), ornithine transcarbamylase (OTC), or argininosuccinic acid synthetase (AS). antineoplastic agent (Code: CHEBI:35610) prodrug (Code: CHEBI:50266) Antineoplastic Agents (Code: D000970) 1996-04-30 FDA CLT
Click to view fenipentol stimulates plasma secretion & exocrine pancreatic secretion Cholagogues and Choleretics (Code: D002756) Gastrointestinal Agents (Code: D005765) Ministry of Health of the Russian Federation
Click to view methiosulfonium chloride Methiosulfonium chloride (methylmethionine sulfonium chloride, vitamin U) is a derivative of methionine metabolism in some plants. Methylmethionine has therapeutic effects on gastrointestinal ulceration potentially via its ability to promote dermal fibroblast migration and growth. It is used in the treatment of peptic ulcers, colitis, and gastritis and has an effect on secretory, acid-forming, and enzymatic functions of the intestinal tract. 1960-06-01 PMDA
Click to view methoxyflurane Glycine receptor subunit alpha-1 (Organism: Homo sapiens, class: Ion channel, accessions: P23415, gene: GLRA1, swissprot: GLRA1_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10683198) GABA-A receptor alpha-2/beta-1 (Organism: Homo sapiens, class: Ion channel, accessions: P47869|P18505, gene: GABRA2|GABRB1, swissprot: GBRA1_HUMAN|GBRB1_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10683198) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/8214760) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/8214760) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/8214760) Cytochrome P450 2E1 (Organism: Homo sapiens, class: Enzyme, accessions: P05181, gene: CYP2E1, swissprot: CP2E1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/8214760) Cytochrome P450 2A6 (Organism: Homo sapiens, class: Enzyme, accessions: P11509, gene: CYP2A6, swissprot: CP2A6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/7879937) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/7879937) Methoxyflurane is a general inhalation anesthetic used for induction and maintenance of general anesthesia. It induces muscle relaxation and reduces pains sensitivity by altering tissue excitability. It does so by decreasing the extent of gap junction mediated cell-cell coupling and altering the activity of the channels that underlie the action potential. It was withdrawn from US market due to safety concerns. inhalation anaesthetic (Code: CHEBI:38870) non-narcotic analgesic (Code: CHEBI:35481) Anesthetics (Code: D000777) Anesthetics, General (Code: D018681) Anesthetics, Inhalation (Code: D018685) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) 1962 FDA
Click to view atrolactamide Atrolactamide (themisone) is an anticonvulsant. It was used for the treatment of epileptic seizures, but is no longer available due to its side effects.
Click to view phenylalanine Monocarboxylate transporter 10 (Organism: Homo sapiens, class: Transporter, accessions: Q8TF71, gene: SLC16A10, swissprot: MOT10_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11278508) Monocarboxylate transporter 10 (Organism: Homo sapiens, class: Transporter, accessions: Q8TF71, gene: SLC16A10, swissprot: MOT10_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11827462) Carbonic anhydrase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P00915, gene: CA1, swissprot: CAH1_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/16214338) Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/16214338) Carbonic anhydrase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P22748, gene: CA4, swissprot: CAH4_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/16214338) Carbonic anhydrase 5A, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P35218, gene: CA5A, swissprot: CAH5A_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/17174092) Carbonic anhydrase 5B, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: Q9Y2D0, gene: CA5B, swissprot: CAH5B_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/17174092) Carbonic anhydrase 12 (Organism: Homo sapiens, class: Enzyme, accessions: O43570, gene: CA12, swissprot: CAH12_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/17540561) Carbonic anhydrase 14 (Organism: Homo sapiens, class: Enzyme, accessions: Q9ULX7, gene: CA14, swissprot: CAH14_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/17540561) Carbonic anhydrase 9 (Organism: Homo sapiens, class: Enzyme, accessions: Q16790, gene: CA9, swissprot: CAH9_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/18294854) Carbonic anhydrase 6 (Organism: Homo sapiens, class: Enzyme, accessions: P23280, gene: CA6, swissprot: CAH6_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/20176489) Probable G-protein coupled receptor 139 (Organism: Homo sapiens, class: Unclassified, accessions: Q6DWJ6, gene: GPR139, swissprot: GP139_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/24826842) Phenylalanine is an essential aromatic amino acid in humans (provided by food), Phenylalanine is a precursor of melanin; dopamine; noradrenalin (norepinephrine), and thyroxine and plays a key role in the biosynthesis of other amino acids. Phenylalanine is converted to tyrosine, used in the biosynthesis of dopamine and norepinephrine neurotransmitters. The L-form of Phenylalanine is incorporated into proteins, while the D-form acts as a painkiller. The supposed antidepressant effects of L-phenylalanine may be due to its role as a precursor in the synthesis of the neurotransmitters norepinephrine and dopamine. Elevated brain norepinephrine and dopamine levels are thought to be associated with antidepressant effects. The mechanism of L-phenylalanine's possible antivitiligo activity is not well understood. It is thought that L-phenylalanine may stimulate the production of melanin in the affected skin. 1975 FDA DPN
PHE
Click to view ethenzamide Ethenzamide is a non-steroidal anti-inflammatory drug. It is used in combination with other ingredients for the relief of fever, headaches, and other minor aches and pains. Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1988-04-01 PMDA
Click to view sulfaperin Sulfaperin is a long-acting sulfanilamide antibiotic. antibacterial drug (Code: CHEBI:36047)
Click to view benzocaine Sodium channel protein type 10 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q9Y5Y9, gene: SCN10A, swissprot: SCNAA_HUMAN) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/19661462) Benzocaine is a local anesthetic. Benzocaine is an ester, a compound made from the organic acid PABA (para-aminobenzoic acid) and ethanol. It acts by blocking voltage-gated sodium ion channels in nerve endings. Benzocaine is available over-the counter for local anesthesia of oral and pharyngeal mucous membranes (sore throat, cold sores, mouth ulcers, toothache, sore gums, denture irritation), otic pain, and as a local anesthetic for surgical or diagnostic procedures. Topical application of benzocaine to gums or mouth may cause rare, but serious and potentially fatal adverse effect methemoglobinemia. antipruritic drug (Code: CHEBI:59683) topical anaesthetic (Code: CHEBI:48425) Standardized Chemical Allergen (Code: N0000185508) Increased Histamine Release (Code: N0000175629) Cell-mediated Immunity (Code: N0000184306) Allergens (Code: N0000171131) Anesthetics (Code: D000777) Anesthetics, Local (Code: D000779) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1964-04-30 Ministry of Health of the Russian Federation
Click to view pholedrine Pholedrineis (4-Hydroxymethamphetamine) is a metabolite of methamphetamine. It was used as a topical eye drop for the purpose of dilating the pupil for diagnostic of Horner's syndrome. Also pholedrine was a frequently used drug for the treatment of severe hypotension. Autonomic Agents (Code: D001337) Central Nervous System Agents (Code: D002491) Central Nervous System Stimulants (Code: D000697) Peripheral Nervous System Agents (Code: D018373) Sympathomimetics (Code: D013566) 1WF
Click to view ephedrine Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208609s000lbl.pdf) Alpha-1B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35368, gene: ADRA1B, swissprot: ADA1B_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208609s000lbl.pdf) Alpha-1D adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P25100, gene: ADRA1D, swissprot: ADA1D_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208609s000lbl.pdf) Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208609s000lbl.pdf) Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208609s000lbl.pdf) Alpha-2C adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18825, gene: ADRA2C, swissprot: ADA2C_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208609s000lbl.pdf) Beta-1 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08588, gene: ADRB1, swissprot: ADRB1_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208609s000lbl.pdf) Beta-2 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P07550, gene: ADRB2, swissprot: ADRB2_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208609s000lbl.pdf) Beta-3 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P13945, gene: ADRB3, swissprot: ADRB3_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208609s000lbl.pdf) Ephedrine is an alpha- and beta-adrenergic agonist that may also enhance release of norepinephrine. Ephedrine is similar in molecular structure to the well-known drugs phenylpropanolamine and methamphetamine, as well as to the important neurotransmitter epinephrine (adrenalin). Chemically, it is an alkaloid with a phenethylamine skeleton found in various plants in the genus Ephedra (family Ephedraceae). It works mainly by increasing the activity of norepinephrine (noradrenalin) on adrenergic receptors. It is most usually marketed as the hydrochloride or sulfate salt. It has been used in the treatment of several disorders including asthma, heart failure, rhinitis, and urinary incontinence, and for its central nervous system stimulatory effects in the treatment of narcolepsy and depression. It has become less extensively used with the advent of more selective agonists. Pseudoephedrine is a phenethylamine that is an isomer of ephedrine which has less central nervous system effects and usage is mainly for respiratory tract decongestion. sympathomimetic agent (Code: CHEBI:35524) vasoconstrictor agent (Code: CHEBI:50514) nasal decongestant (Code: CHEBI:77715) alpha-Adrenergic Agonist (Code: N0000175552) Adrenergic alpha-Agonists (Code: N0000000209) beta-Adrenergic Agonist (Code: N0000175555) Adrenergic beta-Agonists (Code: N0000000245) Norepinephrine Releasing Agent (Code: N0000192563) Increased Norepinephrine Activity (Code: N0000009456) Adrenergic Agents (Code: D018663) Autonomic Agents (Code: D001337) Cardiovascular Agents (Code: D002317) Central Nervous System Agents (Code: D002491) Central Nervous System Stimulants (Code: D000697) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Sympathomimetics (Code: D013566) Vasoconstrictor Agents (Code: D014662) 1963-10-18 FDA
Click to view cycloguanil Bifunctional dihydrofolate reductase-thymidylate synthase (Organism: Plasmodium falciparum, class: Enzyme, accessions: P13922, gene: None, swissprot: DRTS_PLAFK) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9037017) Cycloguanil is a dihydrofolate reductase inhibitor and is a metabolite of the antimalarial drug proguanil. Cycloguanil acts on both the erythrocytic and on the pre-erythrocytic (hepatic) forms of the malaria parasites. Anti-Infective Agents (Code: D000890) Antimalarials (Code: D000962) Antiparasitic Agents (Code: D000977) Antiprotozoal Agents (Code: D000981) Enzyme Inhibitors (Code: D004791) Folic Acid Antagonists (Code: D005493) 1CY
Click to view fenoxypropazine Fenoxypropazine is a non-selective and irreversible monoamine oxidase enzyme inhibitor (MAOI), belonging to the hydrazine chemical class. It was marketed as an antidepressant in 1961 but was later withdrawn in 1966 because of its hepatotoxic potential.
Click to view edrophonium Acetylcholinesterase (Organism: Homo sapiens, class: Enzyme, accessions: P22303, gene: ACHE, swissprot: ACES_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/019677s006lbl.pdf) Edrophonium is a rapid-onset, short-acting cholinesterase inhibitor used in cardiac arrhythmias and in the diagnosis of myasthenia gravis. It has also been used as an antidote to curare principles. Also it is used in combination with atropine as a reversal agent or antagonist of nondepolarizing neuromuscular blocking agents. diagnostic agent (Code: CHEBI:33295) antidote (Code: CHEBI:50247) Cholinesterase Inhibitor (Code: N0000175723) Antidotes (Code: D000931) Cholinergic Agents (Code: D018678) Cholinesterase Inhibitors (Code: D002800) Enzyme Inhibitors (Code: D004791) Neurotransmitter Agents (Code: D018377) Protective Agents (Code: D020011) 1951-05-03 FDA EDR
Click to view ethionamide Polyphenol oxidase 2 (Organism: Agaricus bisporus, class: Enzyme, accessions: O42713, gene: PPO2, swissprot: PPO2_AGABI) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/26544630) Ethionamide is a thiocarboxamide that is pyridine-4-carbothioamide substituted by an ethyl group at position 2. Ethionamide is a prodrug that undergoes metabolic activation by conversion to the ethionamide sulphoxide. Ethionamide may be bacteriostatic or bactericidal in action, depending on the concentration of the drug attained at the site of infection and the susceptibility of the infecting organism. The exact mechanism of action of ethionamide has not been fully elucidated, but the drug appears to inhibit peptide synthesis in susceptible organisms. Its sulphoxide metabolite has been demonstrated to have antimicrobial activity against Mycobacterium tuberculosis. Ethionamide is primarily indicated for the treatment of active tuberculosis in patients with M. tuberculosis resistant to isoniazid or rifampin, or when there is intolerance on the part of the patient to other drugs. Its use alone in the treatment of tuberculosis results in the rapid development of resistance. antitubercular agent (Code: CHEBI:33231) antilipemic drug (Code: CHEBI:35679) leprostatic drug (Code: CHEBI:35816) prodrug (Code: CHEBI:50266) Antimycobacterial (Code: N0000175483) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Antimetabolites (Code: D000963) Antitubercular Agents (Code: D000995) Fatty Acid Synthesis Inhibitors (Code: D054872) Hypolipidemic Agents (Code: D000960) 1965-04-30 FDA
Click to view orthocaine Orthocaine (methyl m-amino-p-hydroxybenzoate) was used as an anaesthetic for painful wounds.
Click to view aminosalicylic acid hydrazide Aminosalicylic acid hydrazide (apacizin) has activity against Mycobacterium tuberculosis.
Click to view thioguanine DNA (Organism: None, class: DNA, accessions: None, gene: None, swissprot: None) intercalation (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/012429s028lbl.pdf) Hypoxanthine-guanine phosphoribosyltransferase (Organism: Homo sapiens, class: Enzyme, accessions: P00492, gene: HPRT1, swissprot: HPRT_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/012429s028lbl.pdf) Multidrug resistance-associated protein 4 (Organism: Homo sapiens, class: Transporter, accessions: O15439, gene: ABCC4, swissprot: MRP4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/14643890) Thioguanine is an analogue of the nucleic acid constituent guanine, and is closely related structurally and functionally to mercaptopurine. Thioguanine is incorporated into the DNA and the RNA of human bone marrow cells. Intracellular activation results in incorporation into DNA as a false purine base. An additional cytotoxic effect is related to its incorporation into RNA. Thioguanine is cross-resistant with mercaptopurine. Cytotoxicity is cell cycle phase-specific (S-phase). Thioguanine competes with hypoxanthine and guanine for the enzyme hypoxanthine-guanine phosphoribosyltransferase (HGPRTase) and is itself converted to 6-thioguanilyic acid (TGMP), which reaches high intracellular concentrations at therapeutic doses. TGMP interferes with the synthesis of guanine nucleotides by its inhibition of purine biosynthesis by pseudofeedback inhibition of glutamine-5-phosphoribosylpyrophosphate amidotransferase, the first enzyme unique to the de novo pathway of purine ribonucleotide synthesis. TGMP also inhibits the conversion of inosinic acid (IMP) to xanthylic acid (XMP) by competition for the enzyme IMP dehydrogenase. Thioguanine is used in the treatment of several forms of leukemia including acute nonlymphocytic leukemia. antineoplastic agent (Code: CHEBI:35610) Antimetabolites (Code: D000963) Antimetabolites, Antineoplastic (Code: D000964) Antineoplastic Agents (Code: D000970) Noxae (Code: D009676) 1966-01-18 FDA DX4
Click to view oxedrine Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/20217639) Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/20217639) Alpha-2C adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18825, gene: ADRA2C, swissprot: ADA2C_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/20217639) Neuromedin-U receptor 2 (Organism: Homo sapiens, class: GPCR, accessions: Q9GZQ4, gene: NMUR2, swissprot: NMUR2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/25262941) Oxedrine (synephrine) is naturally occurring alkaloid. It is known for its longer acting adrenergic effects compared to norepinephrine. It is used as a vasoconstrictor in circulatory failure, asthma, nasal congestion, and glaucoma. Also it is used for the treatment and prevention of arterial collapse. alpha-adrenergic agonist (Code: CHEBI:35569) Adrenergic Agents (Code: D018663) Adrenergic Agonists (Code: D000322) Adrenergic alpha-Agonists (Code: D000316) Autonomic Agents (Code: D001337) Cardiovascular Agents (Code: D002317) Nasal Decongestants (Code: D014663) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Respiratory System Agents (Code: D019141) Sympathomimetics (Code: D013566) Vasoconstrictor Agents (Code: D014662) 1947-01-01 Hungary National Institute of Pharmacy and Nutrition
Click to view pyrithyldione Pyrithyldione is a sedative and hypnotic drug. It was indicated in mild cases of insomnia. Pyrithyldione was withdrawn from the marked due to several cases of agranulocytosis.
Click to view phenylephrine Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/204300lbl.pdf) Alpha-1B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35368, gene: ADRA1B, swissprot: ADA1B_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/204300lbl.pdf) Alpha-1D adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P25100, gene: ADRA1D, swissprot: ADA1D_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/204300lbl.pdf) Amine oxidase [flavin-containing] A (Organism: Homo sapiens, class: Enzyme, accessions: P21397, gene: MAOA, swissprot: AOFA_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10025828) Phenylephrine is a sympathomimetic amine and a postsynaptic ?1-receptor agonist with little effect on ?-receptors of the heart. Phenylephrine is mainly used to treat nasal congestion, but may also be useful in treating hypotension and shock, hypotension during spinal anaesthesia, prolongation of spinal anaesthesia, paroxysmal supraventricular tachycardia, symptomatic relief of external or internal hemorrhoids, and to increase blood pressure as an aid in the diagnosis of heart murmurs. cardiotonic drug (Code: CHEBI:38147) mydriatic agent (Code: CHEBI:50513) protective agent (Code: CHEBI:50267) vasoconstrictor agent (Code: CHEBI:50514) sympathomimetic agent (Code: CHEBI:35524) nasal decongestant (Code: CHEBI:77715) alpha-adrenergic agonist (Code: CHEBI:35569) alpha-1 Adrenergic Agonist (Code: N0000186105) Adrenergic alpha1-Agonists (Code: N0000009917) Adrenergic Agents (Code: D018663) Adrenergic Agonists (Code: D000322) Adrenergic alpha-1 Receptor Agonists (Code: D058646) Adrenergic alpha-Agonists (Code: D000316) Autonomic Agents (Code: D001337) Cardiotonic Agents (Code: D002316) Cardiovascular Agents (Code: D002317) Mydriatics (Code: D009184) Nasal Decongestants (Code: D014663) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Protective Agents (Code: D020011) Respiratory System Agents (Code: D019141) Sympathomimetics (Code: D013566) Vasoconstrictor Agents (Code: D014662) 1952-01-21 FDA
Click to view metaraminol Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) agonist A sympathomimetic agent that acts predominantly at alpha-1 adrenergic receptors. It has been used primarily as a vasoconstrictor in the treatment of HYPOTENSION. alpha-adrenergic agonist (Code: CHEBI:35569) vasoconstrictor agent (Code: CHEBI:50514) sympathomimetic agent (Code: CHEBI:35524) Adrenergic Agents (Code: D018663) Adrenergic Agonists (Code: D000322) Adrenergic alpha-1 Receptor Agonists (Code: D058646) Adrenergic alpha-Agonists (Code: D000316) Autonomic Agents (Code: D001337) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Sympathomimetics (Code: D013566) Vasoconstrictor Agents (Code: D014662) 1954-09-29 FDA
Click to view ethinamate short duration hypnotic with fast onset & relatively low toxicity; may cause dependence; minor descriptor (76-85); on-line & Index Medicus search CARBAMATES (76-85) sedative (Code: CHEBI:35717) 1955-03-13 FDA
Click to view mecamylamine Neuronal acetylcholine receptor; alpha3/beta2 (Organism: Homo sapiens, class: Ion channel, accessions: P32297|P17787, gene: CHRNA3|CHRNB2, swissprot: ACHA3_HUMAN|ACHB2_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/11303054) Neuronal acetylcholine receptor; alpha4/beta2 (Organism: Homo sapiens, class: Ion channel, accessions: P43681|P17787, gene: CHRNA4|CHRNB2, swissprot: ACHA4_HUMAN|ACHB2_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/11303054) Neuronal acetylcholine receptor; alpha3/beta4 (Organism: Homo sapiens, class: Ion channel, accessions: P32297|P30926, gene: CHRNA3|CHRNB4, swissprot: ACHA3_HUMAN|ACHB4_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/11303054) Neuronal acetylcholine receptor subunit alpha-7 (Organism: Homo sapiens, class: Ion channel, accessions: P36544, gene: CHRNA7, swissprot: ACHA7_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/11303054) Mecamylamine is a nicotinic antagonist that is well absorbed from the gastrointestinal tract and crosses the blood-brain barrier. Mecamylamine has been used as a ganglionic blocker in treating hypertension, but, like most ganglionic blockers, is more often used now as a research tool. S-(+)-mecamylamine might be preferable to R-(-)-mecamylamine, because it has the decreased side effects associated with muscle-type receptors. Autonomic Ganglionic Blocker (Code: N0000175641) Decreased Autonomic Ganglionic Activity (Code: N0000175644) Antihypertensive Agents (Code: D000959) Autonomic Agents (Code: D001337) Cardiovascular Agents (Code: D002317) Cholinergic Agents (Code: D018678) Cholinergic Antagonists (Code: D018680) Ganglionic Blockers (Code: D005730) Neurotransmitter Agents (Code: D018377) Nicotinic Antagonists (Code: D018733) Peripheral Nervous System Agents (Code: D018373) 1956-03-01 FDA
Click to view desflurane Desflurane is a highly fluorinated methyl ethyl ether used for maintenance of general anaesthesia. It induces muscle relaxation and reduces pains sensitivity by altering tissue excitability. It does so by decreasing the extent of gap junction mediated cell-cell coupling and altering the activity of the channels that underlie the action potential. Desflurane is used as an inhalation agent for induction and/or maintenance of anesthesia for inpatient and outpatient surgery in adults. inhalation anaesthetic (Code: CHEBI:38870) General Anesthesia (Code: N0000175975) General Anesthetic (Code: N0000175681) Anesthetics (Code: D000777) Anesthetics, General (Code: D018681) Anesthetics, Inhalation (Code: D018685) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) 1992-09-18 FDA DSF
Click to view sulfametrole Sulfametrole is a sulfonamide antibiotic. Sulfametrole inhibits folic acid formation. Sulfametrole is used in combintion with trimethoprim for the treatment of urinary tract infections, gastrointestinal infections (typhoid, paratyphoid A and B, shigellosis), diarhhea, respiratory tract infections (acute exacerbation of chronic bronchitis, otitis media, Pneumocystis jiroveci pneumonia), and ginecological infections. 1979-10-30 Austrian Medicines and Medical Devices Agency
Click to view cicrotoic acid Cicrotoic acid is an unsaturated fatty acid. Cicrotoic acid acts on bile flow and liquid composition of human bile.
Click to view zoxazolamine Intermediate conductance calcium-activated potassium channel protein 4 (Organism: Homo sapiens, class: Ion channel, accessions: O15554, gene: KCNN4, swissprot: KCNN4_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/10712246) Small conductance calcium-activated potassium channel protein 2 (Organism: Rattus norvegicus, class: Unclassified, accessions: P70604, gene: Kcnn2, swissprot: KCNN2_RAT) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/10712246) Zoxazolamine is a centrally acting muscle relaxant. Zoxazolamine was shown to decrease striatal dopamine turnover without directly affecting dopamine synthesis, catabolism, reuptake, or release. It was used for the relief of muscle spasm in conditions such as musculoskeletal disorders and neurological diseases. Later, it was submitted for the drug's use as a uricosuric agent to treat gout. It was withdrawn from the market due to hepatotoxicity. Antirheumatic Agents (Code: D018501) Central Nervous System Agents (Code: D002491) Gout Suppressants (Code: D006074) Muscle Relaxants, Central (Code: D009125) Neuromuscular Agents (Code: D009465) Peripheral Nervous System Agents (Code: D018373) Renal Agents (Code: D012076) Uricosuric Agents (Code: D014528) 1956-01-13 FDA 36R
Click to view pyridoxine Pyridoxine is the 4-methanol form of vitamin B6, an important water-soluble vitamin that is naturally present in many foods. As its classification as a vitamin implies, pyridoxine are essential nutrients required for normal functioning of many biological systems within the body. While many plants and microorganisms are able to synthesize pyridoxine through endogenous biological processes, animals must obtain it through their diet. More specifically, pyridoxine is converted to pyridoxal 5-phosphate in the body. Pyridoxine is indicated for the treatment of vitamin B6 deficiency and for the prophylaxis of Isoniazid-induced peripheral neuropathy. It is also approved for the treatment of nausea and vomiting. Growth Substances (Code: D006133) Micronutrients (Code: D018977) Vitamin B Complex (Code: D014803) Vitamins (Code: D014815) Vitamin B6 Analog (Code: N0000192800) Vitamin B 6 (Code: N0000005657) Analogs/Derivatives (Code: N0000175452) 1947-07-28 FDA UEG
Click to view norepinephrine Alpha-1B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35368, gene: ADRA1B, swissprot: ADA1B_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/007513Orig1s024lbl.pdf) Alpha-2C adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18825, gene: ADRA2C, swissprot: ADA2C_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/007513Orig1s024lbl.pdf) Beta-2 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P07550, gene: ADRB2, swissprot: ADRB2_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/007513Orig1s024lbl.pdf) Alpha-1D adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P25100, gene: ADRA1D, swissprot: ADA1D_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/007513Orig1s024lbl.pdf) Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/007513Orig1s024lbl.pdf) Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/007513Orig1s024lbl.pdf) Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/007513Orig1s024lbl.pdf) Beta-3 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P13945, gene: ADRB3, swissprot: ADRB3_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/007513Orig1s024lbl.pdf) Beta-1 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08588, gene: ADRB1, swissprot: ADRB1_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/007513Orig1s024lbl.pdf) Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/16722247) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/9812985) Solute carrier family 22 member 1 (Organism: Homo sapiens, class: Transporter, accessions: O15245, gene: SLC22A1, swissprot: S22A1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/9776363) Solute carrier family 22 member 3 (Organism: Homo sapiens, class: Transporter, accessions: O75751, gene: SLC22A3, swissprot: S22A3_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/9830022) Solute carrier family 22 member 5 (Organism: Homo sapiens, class: Transporter, accessions: O76082, gene: SLC22A5, swissprot: S22A5_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10454528) Adrenergic receptor alpha-2 (Organism: Rattus norvegicus, class: GPCR, accessions: P22909|P19328|P22086, gene: Adra2a|Adra2b|Adra2c, swissprot: ADA2A_RAT|ADA2B_RAT|ADA2C_RAT) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/8230093) Adrenergic receptor beta (Organism: Rattus norvegicus, class: GPCR, accessions: P18090|P10608|P26255, gene: Adrb1|Adrb2|Adrb3, swissprot: ADRB1_RAT|ADRB2_RAT|ADRB3_RAT) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/8230093) Adrenergic receptor alpha-1 (Organism: Rattus norvegicus, class: GPCR, accessions: P43140|P15823|P23944, gene: Adra1a|Adra1b|Adra1d, swissprot: ADA1A_RAT|ADA1B_RAT|ADA1D_RAT) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/8230093) Norepinephrine is a naturally occurring catecholamine hormone that functions as a neurotransmitter in the sympathetic nervous system. Norepinephrine directly stimulates adrenergic receptors. Stimulation of alpha-adrenergic receptors causes vasoconstriction of the radial smooth muscle of the iris, arteries, arterioles, veins, urinary bladder, and the sphincter of the gastrointestinal tract. Stimulation of beta-1 adrenergic receptors causes an increase in myocardial contractility, heart rate, automaticity, and atrioventricular (AV) conduction while stimulation of beta-2 adrenergic receptors causes bronchiolar and vascular smooth muscle dilatation. Norepinephrine may be used for blood pressure control in certain acute hypotensive states (e.g., pheochromocytomectomy, sympathectomy, poliomyelitis, spinal anesthesia, myocardial infarction, septicemia, blood transfusion, and drug reactions) and as an adjunct in the treatment of cardiac arrest and profound hypotension. Catecholamine (Code: N0000175570) Catecholamines (Code: N0000007715) Adrenergic Agents (Code: D018663) Adrenergic Agonists (Code: D000322) Adrenergic alpha-Agonists (Code: D000316) Autonomic Agents (Code: D001337) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Sympathomimetics (Code: D013566) Vasoconstrictor Agents (Code: D014662) 1950-07-13 FDA LNR
E5E
Click to view dichlorobenzyl alcohol Dichlorobenzyl alcohol is a mild antiseptic with a broad spectrum for bacterial and virus associated with mouth and throat infections. Dichlorobenzyl alcohol is considered as an active ingredient found in several marketed OTC products. On the other hand, dichlorobenzyl alcohol is categorized by the FDA in the inactive ingredient for approved drug products. The local anesthetic action of dichlorobenzyl alcohol is thought to be due to a reduced sodium channel blockade. The antiseptic mechanism of action of dichlorobenzyl alcohol is not fully understood but it is thought to be related to a denaturation of external proteins and rearrangement of the tertiary structure proteins. Dichlorobenzyl alcohol in combination with Amylmetacresol is available in over-the-counter products used for symptomatic relief of acute sore throat and postoperative sore throat. antiseptic drug (Code: CHEBI:48218) 1996-12-31 Health Canada
Click to view piperidione Piperidione has a sedative and hypnotic properties. Piperidione was used as an antitussive, but piperidione inhibited respiration.
Click to view chlorzoxazone Intermediate conductance calcium-activated potassium channel protein 4 (Organism: Homo sapiens, class: Ion channel, accessions: O15554, gene: KCNN4, swissprot: KCNN4_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/10712246) Small conductance calcium-activated potassium channel protein 2 (Organism: Rattus norvegicus, class: Unclassified, accessions: P70604, gene: Kcnn2, swissprot: KCNN2_RAT) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/10712246) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/7550365) Cytochrome P450 2E1 (Organism: Homo sapiens, class: Enzyme, accessions: P05181, gene: CYP2E1, swissprot: CP2E1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/7550365) Cytochrome P450 1A1 (Organism: Homo sapiens, class: Enzyme, accessions: P04798, gene: CYP1A1, swissprot: CP1A1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10534312) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10534312) Chlorzoxazone is a benzoxazolone derivative with mild sedative and centrally-acting muscle relaxant activities. Although its exact mechanism of action is unknown, chlorzoxazone appears to act at the spinal cord and subcortical levels of the brain to inhibit multisynaptic reflex arcs involved in producing and maintaining muscle spasms. The clinical result is a reduction of the skeletal muscle spasm with relief of pain and increased mobility of the involved muscles. Chlorzoxazone is indicated as an adjunct to rest, physical therapy, and other measures for the relief of discomfort associated with acute, painful musculoskeletal conditions. Chlorzoxazone does not directly relax tense skeletal muscles in man. muscle relaxant (Code: CHEBI:51371) sedative (Code: CHEBI:35717) Centrally-mediated Muscle Relaxation (Code: N0000175730) Central Nervous System Agents (Code: D002491) Muscle Relaxants, Central (Code: D009125) Neuromuscular Agents (Code: D009465) Peripheral Nervous System Agents (Code: D018373) 1958-08-15 FDA CLW
Click to view levetiracetam Synaptic vesicle glycoprotein 2A (Organism: Homo sapiens, class: Transporter, accessions: Q7L0J3, gene: SV2A, swissprot: SV2A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17461889) Voltage-dependent N-type calcium channel subunit alpha-1B (Organism: Homo sapiens, class: Ion channel, accessions: Q00975, gene: CACNA1B, swissprot: CACNA1B_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/207958s008lbl.pdf) Levetiracetam is a pyrrolidine with antiepileptic activity. Levetiracetam inhibits burst firing without affecting normal neuronal excitability, which suggests that it may selectively prevent hyper-synchronization of epileptiform burst firing and propagation of seizure activity. The antiepileptic activity of levetiracetam was assessed in a number of animal models of epileptic seizures. Levetiracetam did not inhibit single seizures induced by maximal stimulation with electrical current or different chemoconvulsants and showed only minimal activity in submaximal stimulation and in threshold tests. Protection was observed, however, against secondarily generalized activity from focal seizures induced by pilocarpine and kainic acid, two chemoconvulsants that induce seizures that mimic some features of human complex partial seizures with secondary generalization. Levetiracetam also displayed inhibitory properties in the kindling model in rats, another model of human complex partial seizures, both during kindling development and in the fully kindled state. anticonvulsant (Code: CHEBI:35623) Decreased Central Nervous System Disorganized Electrical Activity (Code: N0000008486) 1999-11-30 FDA
Click to view propylthiouracil Thyroid peroxidase (Organism: Homo sapiens, class: Enzyme, accessions: P07202, gene: TPO, swissprot: PERT_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/26509551) Myeloperoxidase (Organism: Homo sapiens, class: Enzyme, accessions: P05164, gene: MPO, swissprot: PERM_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/26509551) Dopamine beta-hydroxylase (Organism: Bos taurus, class: Unclassified, accessions: P15101, gene: DBH, swissprot: DOPO_BOVIN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/880264) Propylthiouracil (PTU) is a thiourea derivative with antithyroid property. Propylthiouracil interferes with the oxidation of iodine possibly by interaction with peroxidase or a peroxidase-mediated complex reaction, thereby inhibiting synthesis of thyroid hormones tri-iodothyronine (T3) and thyroxine (T4). In addition, this agent inhibits the Type I 5'-deiodinase (D1), an enzyme involved in the peripheral conversion of thyroxine to tri-iodothyronine. Propylthiouracil is used to manage hyperthyroidism which is due to Grave's disease. antithyroid drug (Code: CHEBI:50671) hormone antagonist (Code: CHEBI:49020) antidote to paracetamol poisoning (Code: CHEBI:74529) Antimetabolites (Code: D000963) Antithyroid Agents (Code: D013956) Hormone Antagonists (Code: D006727) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Noxae (Code: D009676) Thyroid Hormone Synthesis Inhibitor (Code: N0000175918) Thyroid Hormone Synthesis Inhibitors (Code: N0000175917) 1947-07-28 FDA 3CJ
Click to view sobrerol Sobrerol is a cyclic terpene derivative. Sobrerol may increase mucus production and volume but reduce overall viscosity. (-)-trans-sobrerol enantiomer has a central antitussive activity, which has never been described for racemic sobrerol, as well as a lower toxicity than the latter. Sobrerol is used as mucolitic for the treatment of chronic obstructive pulmonary diseases. Expectorants (Code: D005100) Respiratory System Agents (Code: D019141) 1970 Italian Medicines Agency (AIFA)
Click to view metronidazole Cytochrome P450 2A6 (Organism: Homo sapiens, class: Enzyme, accessions: P11509, gene: CYP2A6, swissprot: CP2A6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/23813797) Metronidazole, a nitroimidazole, exerts antibacterial effects in an anaerobic environment against most obligate anaerobes. Once metronidazole enters the organism by passive diffusion and activated in the cytoplasm of susceptible anaerobic bacteria, it is reduced; this process includes intracellular electron transport proteins such as ferredoxin, transfer of an electron to the nitro group of the metronidazole, and formation of a short-lived nitroso free radical. Because of this alteration of the metronidazole molecule, a concentration gradient is created and maintained which promotes the drug’s intracellular transport. The reduced form of metronidazole and free radicals can interact with DNA leading to inhibition of DNA synthesis and DNA degradation leading to death of the bacteria. The precise mechanism of action of metronidazole is unclear. Metronidazole has been shown to be active against: Clostridium species, Eubacterium species, Peptococcus species, Peptostreptococcus species, Bacteroides fragilis group (B. fragilis, B. distasonis, B. ovatus, B. thetaiotaomicron, B.vulgatus), Fusobacterium species, Entamoeba histolytica and Trichomonas vaginalis. Metronidazole is indicated for the treatment of trichomoniasis, amebiasis, intra-abdominal infections, skin and skin structure infections, gynecologycal infections, septicimia, bone and joint infections, CNS infections, lower respiratory tract infections, endocarditis. antitrichomonal drug (Code: CHEBI:50685) prodrug (Code: CHEBI:50266) antibacterial drug (Code: CHEBI:36047) antiparasitic agent (Code: CHEBI:35442) radiosensitizing agent (Code: CHEBI:132992) Nitroimidazole Antimicrobial (Code: N0000175435) Nitroimidazoles (Code: N0000007663) Anti-Infective Agents (Code: D000890) Antiparasitic Agents (Code: D000977) Antiprotozoal Agents (Code: D000981) Radiation-Sensitizing Agents (Code: D011838) 1963-07-18 FDA 2MN
Click to view gabapentin Voltage-dependent calcium channel subunit alpha-2/delta-1 (Organism: Homo sapiens, class: Ion channel, accessions: P54289, gene: CACNA2D1, swissprot: CA2D1_HUMAN) modulator (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020235s064_020882s047_021129s046lbl.pdf) Cytochrome P450 2A6 (Organism: Homo sapiens, class: Enzyme, accessions: P11509, gene: CYP2A6, swissprot: CP2A6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020235s064_020882s047_021129s046lbl.pdf) Potassium voltage-gated channel subfamily KQT member 3 (Organism: Homo sapiens, class: Ion channel, accessions: O43525, gene: KCNQ3, swissprot: KCNQ3_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/30021858) Potassium voltage-gated channel subfamily KQT member 5 (Organism: Homo sapiens, class: Ion channel, accessions: Q9NR82, gene: KCNQ5, swissprot: KCNQ5_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/30021858) Branched-chain-amino-acid aminotransferase, cytosolic (Organism: Homo sapiens, class: Enzyme, accessions: P54687, gene: BCAT1, swissprot: BCAT1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16141215) L-type amino acid transporter 1 (Organism: Homo sapiens, class: Transporter, accessions: Q01650, gene: SLC7A5, swissprot: LAT1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/23567998) Gabapentin is gamma-amino-2-cyclohexyl-butyric acid. Gabapentin is structurally related to the neurotransmitter GABA (gamma-aminobutyric acid), but it does not modify GABAA or GABAB radioligand binding, it is not converted metabolically into GABA or a GABA agonist, and it is not an inhibitor of GABA uptake or degradation. The mechanism of action by which gabapentin exerts its analgesic action is unknown but in animal models of analgesia, gabapentin prevents allodynia and hyperalgesia. The relevance of these models to human pain is not known. Gabapentin is indicated for the management of postherpetic neuralgia and for adjunctive therapy in the treatment of partial onset seizures, with/without secondary generalization. anticonvulsant (Code: CHEBI:35623) Anti-epileptic Agent (Code: N0000175753) Decreased Central Nervous System Disorganized Electrical Activity (Code: N0000008486) Analgesics (Code: D000700) Anti-Anxiety Agents (Code: D014151) Anti-Dyskinesia Agents (Code: D018726) Anticonvulsants (Code: D000927) Antimanic Agents (Code: D018692) Antiparkinson Agents (Code: D000978) Calcium Channel Blockers (Code: D002121) Cardiovascular Agents (Code: D002317) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Excitatory Amino Acid Agents (Code: D018683) Excitatory Amino Acid Antagonists (Code: D018691) Membrane Transport Modulators (Code: D049990) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Psychotropic Drugs (Code: D011619) Sensory System Agents (Code: D018689) Tranquilizing Agents (Code: D014149) 1993-12-30 FDA GBN
Click to view rasagiline Amine oxidase [flavin-containing] B (Organism: Homo sapiens, class: Enzyme, accessions: P27338, gene: MAOB, swissprot: AOFB_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021641s020lbl.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021641s020lbl.pdf) Apoptosis regulator Bcl-2 (Organism: Homo sapiens, class: Cytosolic other, accessions: P10415, gene: BCL2, swissprot: BCL2_HUMAN) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/12057839) Amine oxidase [flavin-containing] A (Organism: Homo sapiens, class: Enzyme, accessions: P21397, gene: MAOA, swissprot: AOFA_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15027867) Rasagiline is an inhibitor of monamine oxidase used as adjunctive therapy in combination with levodopa and carbidopa in the management of Parkinson’s disease. neuroprotective agent (Code: CHEBI:63726) Monoamine Oxidase Inhibitor (Code: N0000175744) Central Nervous System Agents (Code: D002491) Enzyme Inhibitors (Code: D004791) Monoamine Oxidase Inhibitors (Code: D008996) Neuroprotective Agents (Code: D018696) Protective Agents (Code: D020011) 2005-02-21 EMA RAU
Click to view iproheptine Iproheptine is a vasoconstrictor, antihistamine, and nasal decongestant.
Click to view menadione M-phase inducer phosphatase 3 (Organism: Homo sapiens, class: Enzyme, accessions: P30307, gene: CDC25C, swissprot: MPIP3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15501045) M-phase inducer phosphatase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P30305, gene: CDC25B, swissprot: MPIP2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19028102) NAD(P)H dehydrogenase [quinone] 1 (Organism: Homo sapiens, class: Enzyme, accessions: P15559, gene: NQO1, swissprot: NQO1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/17850125) Aldehyde oxidase (Organism: Homo sapiens, class: Enzyme, accessions: Q06278, gene: AOX1, swissprot: AOXA_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22996261) Trypanothione reductase (Organism: Trypanosoma cruzi, class: Enzyme, accessions: P28593, gene: TPR, swissprot: TYTR_TRYCR) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11170645) Amine oxidase [flavin-containing] A (Organism: Homo sapiens, class: Enzyme, accessions: P21397, gene: MAOA, swissprot: AOFA_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22071524) Amine oxidase [flavin-containing] B (Organism: Homo sapiens, class: Enzyme, accessions: P27338, gene: MAOB, swissprot: AOFB_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22071524) Menadione is a synthetic form of vitamin K. Menadione is prescribed for the treatment of hemorrhage, vitamin K deficiency, moderate to severe forms of hypoprothrombinaemia in adults and children. Large doses of menadione have been reported to cause adverse outcomes including hemolytic anemia due to glucose-6-phosphate dehydrogenase deficiency, neonatal brain or liver damage, or neonatal death in some rare cases. nutraceutical (Code: CHEBI:50733) 1940 FDA VK3
Click to view sulfanilamide Dihydropteroate synthase (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P0AC13, gene: folP, swissprot: DHPS_ECOLI) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9127492) Carbonic anhydrase 9 (Organism: Homo sapiens, class: Enzyme, accessions: Q16790, gene: CA9, swissprot: CAH9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15149691) Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/14971907) Carbonic anhydrase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P22748, gene: CA4, swissprot: CAH4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/14971907) Carbonic anhydrase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P00915, gene: CA1, swissprot: CAH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/14971907) Carbonic anhydrase 7 (Organism: Homo sapiens, class: Enzyme, accessions: P43166, gene: CA7, swissprot: CAH7_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15686895) Carbonic anhydrase 13 (Organism: Mus musculus, class: Enzyme, accessions: Q9D6N1, gene: Ca13, swissprot: CAH13_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15686895) Carbonic anhydrase (Organism: Methanosarcina thermophila, class: Enzyme, accessions: P40881, gene: None, swissprot: CAH_METTE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15546717) Carbonic anhydrase (Organism: Helicobacter pylori (strain ATCC 700392 / 26695), class: Enzyme, accessions: O24855, gene: cynT, swissprot: CYNT_HELPY) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16459077) Beta-carbonic anhydrase 1 (Organism: Mycobacterium tuberculosis (strain ATCC 25618 / H37Rv), class: Enzyme, accessions: P9WPJ7, gene: mtcA1, swissprot: MTCA1_MYCTU) inhibitor (Source:https://www.ncbi.nlm.nih.gov/pubmed/19338333) Carbonic anhydrase 2 (Organism: Mycobacterium tuberculosis (strain ATCC 25618 / H37Rv), class: Enzyme, accessions: P9WPJ9, gene: mtcA2, swissprot: MTCA2_MYCTU) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19338333) Delta carbonic anhydrase (Organism: Thalassiosira weissflogii, class: Unclassified, accessions: Q5U9J1, gene: ca1, swissprot: Q5U9J1_THAWE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/24314394) Sulfanilamide is an organic sulfur compound structurally similar to p-aminobenzoic acid (PABA) with antibacterial property. Sulfanilamide competes with PABA for the bacterial enzyme dihydropteroate synthase, thereby preventing the incorporation of PABA into dihydrofolic acid, the immediate precursor of folic acid. This leads to an inhibition of bacterial folic acid synthesis and de novo synthesis of purines and pyrimidines, ultimately resulting in cell growth arrest and cell death. Sulfanilamide is used for the treatment of vulvovaginitis caused by Candida albicans. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) 1965-06-05 FDA SAN
Click to view sodium hexacyclonate used in treatment of hyperlipoproteinemia
Click to view terpin Terpin is derived from oil of turpentine, oregano, thyme and eucalyptus. It was banned by FDA in the 1990s due to lack of proof of efficacy but is a medicine available in a number of countries worldwide commonly used in combination with codein. Terpin is an expectorant which used to loosen mucus in patients presenting with acute or chronic bronchitis, and related conditions. Expectorants (Code: D005100) Respiratory System Agents (Code: D019141) 2004-06-01 Ministry of Health of the Russian Federation
Click to view loprodiol Loprodiol (2,2-bis(chloromethyl)-1,3-propanediol) was used as a sedative agent.
Click to view oxaceprol Oxaceprol is a structural analog of hydroxyproline. It was shown that oxaceprol does not inhibit the synthesis of prostaglandins in vitro, but acts predominantly by inhibiting leukocyte adhesion and migration, thus inhibiting inflammation at an early stage and helps in pain relief. Oxaceprol is used for the treatment of osteoarthritis and rheumatoid arthritis. Antirheumatic Agents (Code: D018501) Dermatologic Agents (Code: D003879) 2011-03-15 CDSCO (INDIA)
Click to view acexamic acid Acexamic acid is a wound-healing agent component of plasmutan.
Click to view acetylleucine Acetylleucine is a modified amino acid used for treating vestibular-related imbalance and vertigo. L-Acetylleucine is enantiomer of acetylleucine and the active part of the racemate component since it induces a significant acceleration of the vestibular compensation process similar and even better than that observed under treatment with the racemate component only. Acetylleucine may act as a precursor of a peptidic neuromediator responsible for activation of vestibular afferents. 1992-09-30 ANSM (French National Agency for Medicines and Health Products Safety) LAY
Click to view menadiol sodium sulfate Menadiol sodium sulfate (Menadiol disulfate, Vitamin k4 sodium sulfate) is a synthetic vitamin K analogue and a prothrombogenic agent.
Click to view ascorbic acid Solute carrier family 23 member 1 (Organism: Homo sapiens, class: Unclassified, accessions: Q9UHI7, gene: SLC23A1, swissprot: S23A1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/18094143) Solute carrier family 23 member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UGH3, gene: SLC23A2, swissprot: S23A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/19216494) Ascorbic acid is a six carbon compound related to glucose. It is found naturally in citrus fruits and many vegetables. Ascorbic acid is an essential nutrient in human diets, and necessary to maintain connective tissue and bone. Its biologically active form, vitamin C or L-ascorbic acid, functions as a reducing agent and coenzyme in several metabolic pathways. Vitamin C is considered an antioxidant. Ascorbic acid is used to treat vitamin C deficiency, scurvy, delayed wound and bone healing, urine acidification, and in general as an antioxidant. It has also been suggested to be an effective antiviral agent. vitamin C (Code: CHEBI:21241) flour treatment agent (Code: CHEBI:64577) food antioxidant (Code: CHEBI:77962) Ascorbic Acid (Code: N0000006439) Antioxidants (Code: D000975) Growth Substances (Code: D006133) Micronutrients (Code: D018977) Protective Agents (Code: D020011) Vitamins (Code: D014815) 1947-07-28 FDA ASC
ISD
Click to view arginine Nitric oxide synthase, inducible (Organism: Homo sapiens, class: Enzyme, accessions: P35228, gene: NOS2, swissprot: NOS2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11527735) Glycine amidinotransferase, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P50440, gene: GATM, swissprot: GATM_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/27233232) Arginase-2 (Organism: Homo sapiens, class: Enzyme, accessions: P78540, gene: ARG2, swissprot: ARGI2_HUMAN) substrate (Source: https://www.uniprot.org/uniprot/P78540) Arginine is an essential amino acid that is physiologically active in the L-form. In mammals, arginine is formally classified as a semi-essential or conditionally essential amino acid, depending on the developmental stage and health status of the individual. Arginine helps dispose of ammonia, is used to make compounds such as nitric oxide, creatine, L-glutamate, and L-proline, and it can be converted into glucose and glycogen if needed. In large doses, L-arginine also stimulates the release of the hormones growth hormone and prolactin. Catabolic disease states such as sepsis, injury, and cancer cause an increase in arginine utilization, which can exceed normal body production, leading to arginine depletion. Arginine is found in plant and animal proteins, such as dairy products, meat, poultry, fish, and nuts. 1973-02-28 FDA ARG
DAR
Click to view carfimate Carfimate (?-Ethynylbenzenemethanol carbamate) is a carboxylic ester. It derives from a benzyl alcohol. Carfimate has sedative and hypnotic activities.
Click to view citrulline Argininosuccinate synthase (Organism: Homo sapiens, class: Enzyme, accessions: P00966, gene: ASS1, swissprot: ASSY_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/27287393) Citrulline is an amino acid. It is made from ornithine and carbamoyl phosphate in one of the central reactions in the urea cycle. It is a non-essential amino acid and a precursor of arginine. L-citrulline is converted into L-arginine by the enzymes argininosuccinate synthetase and argininosuccinate lyase in the presence of L-aspartate and ATP. Subsequently, L-arginine is converted to nitric oxide by nitric oxide synthase and L-citrulline is regenerated as a by-product. Citrulline supplements have been claimed to promote energy levels, stimulate the immune system and help detoxify ammonia (a cell toxin). 2000-03-15 Spanish Agency of Medicines and Medical Products (AEMPS) CIR
Click to view benzalamide Benzalamide is a hypocholesterolemic and hypolipemic agent reducing the biosynthesis of cholesterol and fatty acids.
Click to view tidiacic Tidiacic is a hepatoprotective drug that acts as an antioxidant and a sulfur donor. Tidiacic is a component of tidiacic arginine that used for the treatment of toxic liver damage. 1988-02-22 ANSM (French National Agency for Medicines and Health Products Safety) 5XB
Click to view glucurolactone Glucurolactone (Glucuronolactone) is a naturally occurring metabolite of glucose. It is used as an additive in energy drinks, because it increases alertness and decreases sleepiness. Glucurolactone is also used as a conventional hepatoprotective drug that is used in epidemical hepatitis, cirrhosis of the liver and poisoning due to food and drugs. It acts as a hepatic antidote and immune regulator. 2014 China Food and Drug Administration (CFDA)
Click to view hymecromone Testosterone 17-beta-dehydrogenase 3 (Organism: Homo sapiens, class: Enzyme, accessions: P37058, gene: HSD17B3, swissprot: DHB3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19954971) Aldose reductase (Organism: Homo sapiens, class: Enzyme, accessions: P15121, gene: AKR1B1, swissprot: ALDR_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20805028) Hymecromone is a choleretic with spasmolytic activity on the gallbladder (sphincter of Oddi) and without spasmolytic effect on other organs. It is used as choleretic and antispasmodic drug. antineoplastic agent (Code: CHEBI:35610) Indicators and Reagents (Code: D007202) 1970-06-30 Italian Medicines Agency (AIFA) 4MU
Click to view pemoline Pemoline is an oxazolidine compound with central nervous system (CNS) stimulant property. Although pemoline has pharmacological activity similar to other CNS stimulants, the exact mechanism and site of action are unknown. This agent has minimal sympathomimetic properties, but animal studies indicate it may work through dopaminergic mechanisms. Pemoline has been withdrawn from the market because of the agent's association with life threatening hepatic failure. Pemoline was used for the treatment of Attention Deficit Hyperactivity Disorder (ADHD). central nervous system stimulant (Code: CHEBI:35337) Central Nervous System Agents (Code: D002491) Central Nervous System Stimulants (Code: D000697) 1975-01-27 FDA
Click to view cotinine Cotinine is the major metabolite of nicotine. Cotinine has antipsychotic, anxiolytic, and antidepressant properties and modulates the serotonergic, cholinergic and dopaminergic systems. Cotinine behaves as a positive allosteric modulator of the nicotinic acetylcholine receptors and has anti-inflammatory effects. Measuring cotinine in people’s blood is the most reliable way to determine exposure to nicotine for both smokers and nonsmokers exposed to environmental tobacco smoke. biomarker (Code: CHEBI:59163) antidepressant (Code: CHEBI:35469) Indicators and Reagents (Code: D007202)
Click to view meptazinol Acetylcholinesterase (Organism: Mus musculus, class: Enzyme, accessions: P21836, gene: Ache, swissprot: ACES_MOUSE) Cholinesterase (Organism: Mus musculus, class: Enzyme, accessions: Q03311, gene: Bche, swissprot: CHLE_MOUSE) Mu-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P35372, gene: OPRM1, swissprot: OPRM_HUMAN) partial agonist (Source: ) A narcotic antagonist with analgesic properties. It is used for the control of moderate to severe pain. Analgesics (Code: D000700) Analgesics, Opioid (Code: D000701) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Narcotic Antagonists (Code: D009292) Narcotics (Code: D009294) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1983-01-01 YEAR INTRODUCED
Click to view metamfepramone Metamfepramone (dimethylcathinone, dimethylpropion, and dimepropion) is a sympathomimetic agent that was used for the treatment of the common cold and hyptonic conditions. Metamfepramone is considered to be an analogue of dimethylamphetamine and is a controlled substance.
Click to view phenmetrazine Sodium-dependent dopamine transporter (Organism: Rattus norvegicus, class: Transporter, accessions: P23977, gene: Slc6a3, swissprot: SC6A3_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12106802) Phenmetrazine is an anti-obesity drug. It is suggested that the drug exerts its effect by inhibiting the monoamine transport. Later on the drug was withdrawn from the market due to the reported cases of abuse. Anti-Obesity Agents (Code: D019440) Appetite Depressants (Code: D001067) Autonomic Agents (Code: D001337) Central Nervous System Agents (Code: D002491) Central Nervous System Stimulants (Code: D000697) Peripheral Nervous System Agents (Code: D018373) Sympathomimetics (Code: D013566) 1982-01-01 FDA
Click to view betanidine Betanidine is a guanidinium antihypertensive agent that acts by blocking adrenergic transmission. Betanidine is a peripherally acting antiadrenergic agent which primarily acts as an alpha2a adrenergic agonist. Betanidine effectively decreases blood pressure by suppressing renin secretion or interfering with function of the sympathetic nervous system. antihypertensive agent (Code: CHEBI:35674) adrenergic antagonist (Code: CHEBI:37887) Adrenergic Agents (Code: D018663) Antihypertensive Agents (Code: D000959) Autonomic Agents (Code: D001337) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Sympatholytics (Code: D013565) 1981-05-29 FDA
Click to view rimantadine Multidrug and toxin extrusion protein 1 (Organism: Homo sapiens, class: Transporter, accessions: Q96FL8, gene: SLC47A1, swissprot: S47A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23241029) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23241029) Rimantadine is a cyclic amine and alpha-methyl derivative of amantadine with antiviral activity. Rimantadine appears to exert its inhibitory effect early in the viral replicative cycle, possibly inhibiting the uncoating of the virus. Genetic studies suggest that a virus protein specified by the virion M2 gene plays an important role in the susceptibility of influenza A virus to inhibition by rimantadine. Rimantadine inhibits the replication in cell culture of influenza A virus isolates from each of the three antigenic subtypes, i.e., H1N1, H2N2 and H3N2, that have been isolated from man. Rimantadine has little or no activity against influenza B virus. Influenza A M2 Protein Inhibitor (Code: N0000175543) M2 Protein Inhibitors (Code: N0000175542) Anti-Infective Agents (Code: D000890) Antiviral Agents (Code: D000998) Enzyme Inhibitors (Code: D004791) Nucleic Acid Synthesis Inhibitors (Code: D019384) 1993-09-17 FDA RIM
EU7
Click to view lidocaine Sodium channel protein type 5 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q14524, gene: SCN5A, swissprot: SCN5A_HUMAN) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/8786356) Sodium channel protein type 2 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q99250, gene: SCN2A, swissprot: SCN2A_HUMAN) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/8799190) Sodium channel protein type 5 subunit alpha (Organism: Rattus norvegicus, class: Unclassified, accessions: P15389, gene: Scn5a, swissprot: SCN5A_RAT) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/2546048) Sodium channel protein type 9 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q15858, gene: SCN9A, swissprot: SCN9A_HUMAN) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/17430993) Sodium channel protein type 4 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: P35499, gene: SCN4A, swissprot: SCN4A_HUMAN) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/24440379) Sodium channel protein type 3 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q9NY46, gene: SCN3A, swissprot: SCN3A_HUMAN) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/24440379) Epidermal growth factor receptor (Organism: Homo sapiens, class: Kinase, accessions: P00533, gene: EGFR, swissprot: EGFR_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16551906) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10215663) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/27906699) A local anesthetic and cardiac depressant used as an antiarrhythmia agent. Lidocaine stabilizes the neuronal membrane by binding to and inhibiting voltage-gated sodium channels, thereby inhibiting the ionic fluxes required for the initiation and conduction of impulses and effecting local anesthesia. Amide Local Anesthetic (Code: N0000175682) Amides (Code: N0000007681) Antiarrhythmic (Code: N0000175426) Local Anesthesia (Code: N0000175976) Anesthetics (Code: D000777) Anesthetics, Local (Code: D000779) Anti-Arrhythmia Agents (Code: D000889) drug allergen (Code: CHEBI:88188) local anaesthetic (Code: CHEBI:36333) anti-arrhythmia drug (Code: CHEBI:38070) Cardiovascular Agents (Code: D002317) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Membrane Transport Modulators (Code: D049990) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) Sodium Channel Blockers (Code: D026941) Voltage-Gated Sodium Channel Blockers (Code: D061567) 1948-11-19 FDA LQZ
Click to view chlorobutanol Chlorobutanol, or chlorbutol, is an alcohol-based preservative with no surfactant activity. Similar in nature to chloral hydrate, it is formed by the simple nucleophilic addition of chloroform and acetone. It also elicits sedative-hypnotic and weak local anesthetic actions in addition to antibacterial and antifungal properties. Due to the long terminal half-life of 37 days, the use of chlorobutanol as a sedative is limited because of the considerable accumulation which will occur following multiple dosing. Chlorobutanol is a common detergent preservative in eye drops and other ophthalmic therapeutic formulations. Chlorobutanol is used as a local anesthetic in combination with hexetidine, chlorhexidine or levomenthol for the treatment of bacterial infections. Pharmaceutic Aids (Code: D010592) Preservatives, Pharmaceutical (Code: D011310) 1971-12-31 Health Canada
Click to view phenacemide Sodium channel protein type 1 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: P35498, gene: SCN1A, swissprot: SCN1A_HUMAN) blocker anti-epileptic drug; structure 1951-06-28 FDA
Click to view nikethamide Nikethamide is a central nervous system stimulant. It was used as a medical countermeasure against tranquilizer overdoses, before the advent of endotracheal intubation and positive-pressure lung expansion. In some sports, nikethamide is listed by the World Anti-Doping Agency as a banned substance. Central Nervous System Agents (Code: D002491) Central Nervous System Stimulants (Code: D000697) Convulsants (Code: D003292) 1967-07-11 Ministry of Health of the Russian Federation
Click to view propofol GABA-A receptor; anion channel (Organism: Homo sapiens, class: Ion channel, accessions: P14867|P47869|P34903|P48169|P31644|Q16445|P18505|P47870|P28472|O14764|P78334|Q8N1C3|P18507|Q99928|O00591|Q9UN88, gene: GABRA1|GABRA2|GABRA3|GABRA4|GABRA5|GABRA6|GABRB1|GABRB2|GABRB3|GABRD|GABRE|GABRG1|GABRG2|GABRG3|GABRP|GABRQ, swissprot: GBRA1_HUMAN|GBRA2_HUMAN|GBRA3_HUMAN|GBRA4_HUMAN|GBRA5_HUMAN|GBRA6_HUMAN|GBRB1_HUMAN|GBRB2_HUMAN|GBRB3_HUMAN|GBRD_HUMAN|GBRE_HUMAN|GBRG1_HUMAN|GBRG2_HUMAN|GBRG3_HUMAN|GBRP_HUMAN|GBRT_HUMAN) positive allosteric modulator (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/019627s066lbl.pdf) Fatty-acid amide hydrolase 1 (Organism: Rattus norvegicus, class: Enzyme, accessions: P97612, gene: Faah, swissprot: FAAH1_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18983142) Carbonic anhydrase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P00915, gene: CA1, swissprot: CAH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19231207) Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19231207) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9764927) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9764927) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9764927) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9764927) Cytochrome P450 1A1 (Organism: Homo sapiens, class: Enzyme, accessions: P04798, gene: CYP1A1, swissprot: CP1A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/7772432) Cytochrome P450 1B1 (Organism: Homo sapiens, class: Enzyme, accessions: Q16678, gene: CYP1B1, swissprot: CP1B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/7772432) Cytochrome P450 2E1 (Organism: Homo sapiens, class: Enzyme, accessions: P05181, gene: CYP2E1, swissprot: CP2E1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/7772432) UDP-glucuronosyltransferase 1-1 (Organism: Homo sapiens, class: Enzyme, accessions: P22309, gene: UGT1A1, swissprot: UD11_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17697043) UDP-glucuronosyltransferase 1-9 (Organism: Homo sapiens, class: Enzyme, accessions: O60656, gene: UGT1A9, swissprot: UD19_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/17697043) Propofol is an intravenous general anesthetic and sedation drug for use in the induction and maintenance of anesthesia or sedation. The mechanism of action is poorly understood. However, propofol is thought to produce its sedative/anesthetic effects by the positive modulation of the inhibitory function of the neurotransmitter GABA through the ligand-gated GABAA receptors. Propofol is used for induction and maintenance of anaesthesia and for management of refractory status epilepticus. intravenous anaesthetic (Code: CHEBI:38877) sedative (Code: CHEBI:35717) antiemetic (Code: CHEBI:50919) anticonvulsant (Code: CHEBI:35623) General Anesthesia (Code: N0000175975) General Anesthetic (Code: N0000175681) Anesthetics (Code: D000777) Anesthetics, General (Code: D018681) Anesthetics, Intravenous (Code: D018686) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Hypnotics and Sedatives (Code: D006993) 1989-10-02 FDA PFL
Click to view fluostigmine Acetylcholinesterase (Organism: Homo sapiens, class: Enzyme, accessions: P22303, gene: ACHE, swissprot: ACES_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20189400) Fluostigmine (isoflurophate) is a long acting cholinesterase inhibitor and potent miotic. It works as an indirect acting parasympathomimetic agent to reduce intraocular pressure. Isoflurophate has been replaced by the more stable anticholinesterase agents. Now fluostigmine is used as a research tool in neuroscience for its ability to inhibit cholinesterase (by phosphorylation) on an acute/sub-acute basis and to produce a delayed neuropathy. Cholinergic Agents (Code: D018678) Cholinesterase Inhibitors (Code: D002800) Enzyme Inhibitors (Code: D004791) Neurotransmitter Agents (Code: D018377) Protease Inhibitors (Code: D011480) 1957-04-02 FDA
Click to view glucosamine Solute carrier family 22 member 1 (Organism: Homo sapiens, class: Transporter, accessions: O15245, gene: SLC22A1, swissprot: S22A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18788725) Glucosamine is an amino sugar and a prominent precursor in the biochemical synthesis of glycosylated proteins and lipids. Glucosamine is one of the most abundant monosaccharides. Oral glucosamine is a dietary supplement. D-Glucosamine is made naturally in the form of glucosamine-6-phosphate, and is the biochemical precursor of all nitrogen-containing sugars. Glucosamine is commonly used as a treatment for osteoarthritis, although its acceptance as a medical therapy varies. 1989-11-02 Italian Medicines Agency (AIFA) GCS
Click to view salacetamide Salacetamide is a derivative of salicylic acid. It is analgesic, anti-inflammatory and antipyretic agent.
Click to view phenprobamate Muscle relaxant & tranquiliser 1964 CDSCO (INDIA)
Click to view phenacetin Prostaglandin G/H synthase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P23219, gene: PTGS1, swissprot: PGH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/14592552) Arylacetamide deacetylase (Organism: Homo sapiens, class: Enzyme accessions: P22760, gene: AADAC, swissprot: AAAD_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/22207054) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/22331994) Cytochrome P450 1A1 (Organism: Homo sapiens, class: Enzyme, accessions: P04798, gene: CYP1A1, swissprot: CP1A1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/8474022) Cytochrome P450 2A13 (Organism: Homo sapiens, class: Enzyme, accessions: Q16696, gene: CYP1A13, swissprot: CP2AD_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/17178771) Cytochrome P450 2E1 (Organism: Homo sapiens, class: Enzyme, accessions: P05181, gene: CYP2E1, swissprot: CP2E1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10421611) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10548449) Solute carrier family 22 member 6 (Organism: Homo sapiens, class: Transporter, accessions: Q4U2R8, gene: SLC22A6, swissprot: S22A6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10991954) Phenacetin was the first NSAID and fever reducer to go on the market. It acts as an analgesic at the spinal cord as well as a negative inotrope at the heart. Human ingestion of phenacetin can result in a bluish discoloration of the skin due to a lack of oxygen in the blood (cyanosis), dizziness and respiratory depression. It is reasonably anticipated to be a human carcinogen. It is used in research as the preferred marker for detecting CYP1A2-based inhibition potential in vitro. In medicine phenacetin is used for the relief of mild to moderate pain, fever. non-narcotic analgesic (Code: CHEBI:35481) peripheral nervous system drug (Code: CHEBI:49110) Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Central Nervous System Agents (Code: D002491) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1951-05-15 Hungary National Institute of Pharmacy and Nutrition N4E
Click to view homarylamine Homarylamine is a sympathomimetic agent proposed as an antitussive.
Click to view glucose Hexokinase HKDC1 (Organism: Homo sapiens, class: Enzyme, accessions: Q2TB90, gene: HKDC1, swissprot: HKDC1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/30517626) Solute carrier family 2, facilitated glucose transporter member 2 (Organism: Homo sapiens, class: Transporter, accessions: P11168, gene: SLC2A2, swissprot: GTR2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/23506862) Solute carrier family 2, facilitated glucose transporter member 3 (Organism: Homo sapiens, class: Transporter, accessions: P11169, gene: SLC2A3, swissprot: GTR3_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/23506862) Solute carrier family 2, facilitated glucose transporter member 4 (Organism: Homo sapiens, class: Transporter, accessions: P14672, gene: SLC2A4, swissprot: GTR4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/23506862) Solute carrier family 2, facilitated glucose transporter member 5 (Organism: Homo sapiens, class: Transporter, accessions: P22732, gene: SLC2A5, swissprot: GTR5_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/23506862) Solute carrier family 2, facilitated glucose transporter member 6 (Organism: Homo sapiens, class: Transporter, accessions: Q9UGQ3, gene: SLC2A6, swissprot: GTR6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/23506862) Solute carrier family 2, facilitated glucose transporter member 7 (Organism: Homo sapiens, class: Transporter, accessions: Q6PXP3, gene: SLC2A7, swissprot: GTR7_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/23506862) Solute carrier family 2, facilitated glucose transporter member 8 (Organism: Homo sapiens, class: Transporter, accessions: Q9NY64, gene: SLC2A8, swissprot: GTR8_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/23506862) Solute carrier family 2, facilitated glucose transporter member 9 (Organism: Homo sapiens, class: Transporter, accessions: Q9NRM0, gene: SLC2A9, swissprot: GTR9_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/23506862) Solute carrier family 2, facilitated glucose transporter member 10 (Organism: Homo sapiens, class: Transporter, accessions: O95528, gene: SLC2A10, swissprot: GTR10_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/23506862) Solute carrier family 2, facilitated glucose transporter member 11 (Organism: Homo sapiens, class: Transporter, accessions: Q9BYW1, gene: SLC2A11, swissprot: GTR11_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/23506862) Solute carrier family 2, facilitated glucose transporter member 12 (Organism: Homo sapiens, class: Transporter, accessions: Q8TD20, gene: SLC2A12, swissprot: GTR12_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/23506862) Solute carrier family 2, facilitated glucose transporter member 1 (Organism: Homo sapiens, class: Transporter, accessions: P11166, gene: SLC2A1, swissprot: GTR1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/27078104) Glucose is a sugar. The D-isomer (D-glucose), also known as dextrose, occurs widely in nature. Glucose is the human body's key source of energy, through aerobic respiration, providing about 3.75 kilocalories (16 kilojoules) of food energy per gram. Use of glucose as an energy source in cells is by either aerobic respiration, anaerobic respiration, or fermentation. All of these processes follow from an earlier metabolic pathway known as glycolysis. Glucose is synthesized in the liver and kidneys from non-carbohydrate intermediates, such as pyruvate and glycerol, by a process known as gluconeogenesis. D-Glucose is found to be associated with 3-methyl-crotonyl-glycinuria, growth hormone deficiency, and primary hypomagnesemia, which are inborn errors of metabolism. Glucose is used to manage hypoglycemia and for intravenous feeding. Nausea may occur after ingesting glucose, but this also may be an effect of the hypoglycemia which is present just prior to ingestion. Flavoring Agents (Code: D005421) Food Additives (Code: D005503) Sweetening Agents (Code: D013549) 1946-01-17 FDA BGC
GLC
GLO
Click to view iproniazid Amine oxidase [flavin-containing] B (Organism: Homo sapiens, class: Enzyme, accessions: P27338, gene: MAOB, swissprot: AOFB_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19267475) Amine oxidase [flavin-containing] A (Organism: Homo sapiens, class: Enzyme, accessions: P21397, gene: MAOA, swissprot: AOFA_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/24793878) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16669850) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16669850) Iproniazid is an irreversible inhibitor of monoamine oxidase types A and B that is used as an antidepressive agent. It has also been used as an antitubercular agent, but its use is limited by its toxicity. Antidepressive Agents (Code: D000928) Central Nervous System Agents (Code: D002491) Enzyme Inhibitors (Code: D004791) Monoamine Oxidase Inhibitors (Code: D008996) Psychotropic Drugs (Code: D011619) 1991-12-02 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view fudosteine Mucin-5AC (Organism: Homo sapiens, class: Unclassified protein, accessions: P98088, gene: MUC5AC, swissprot: MUC5A_HUMAN) gene expression inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18579549) Fudosteine is a derivative of cysteine. Fudosteine acts as a mucoactive agent, enabling mucin secretion. Fudosteine is a MUC5AC mucin hypersecretion inhibitor. It is indicated for use in patients with chronic respiratory diseases (bronchial asthma, chronic bronchitis, bronchiectasis). 2001-10-01 PMDA
Click to view methylephedrine Methylephedrine is a member of amphetamines. Methylephedrine is one of the ephedra alkaloids that is found in varying amounts in different species of the plant genus Ephedra. Methylephedrine is a sympathomimetic amine that appears in various over-the-counter cough and cold medications throughout the world. 2013 China Food and Drug Administration (CFDA)
Click to view protionamide Polyphenol oxidase 2 (Organism: Agaricus bisporus, class: Enzyme, accessions: O42713, gene: PPO2, swissprot: PPO2_AGABI) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/26544630) Protionamide is a thioamide derivative with antitubercular activity. Protionamide forms a covalent adduct with bacterial nicotinamide adenine dinucleotide (NAD), PTH-NAD, which competitively inhibits 2-trans-enoyl-ACP reductase (inhA), an enzyme essential for mycolic acid synthesis. This results in increased cell wall permeability and decreased resistance against cell injury eventually leading to cell lysis. Protionamide is used for the treatment multidrug resistance tuberculosis and leprosy. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Antitubercular Agents (Code: D000995) 2005-07-09 Ministry of Health of the Russian Federation
Click to view mexiletine Sodium channel protein type 4 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: P35499, gene: SCN4A, swissprot: SCN4A_HUMAN) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/14608007) Sodium channel protein type 9 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q15858, gene: SCN9A, swissprot: SCN9A_HUMAN) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/26068619) Sodium channel protein type 10 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q9Y5Y9, gene: SCN10A, swissprot: SCNAA_HUMAN) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/18501613) Sodium channel protein type 2 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q99250, gene: SCN2A, swissprot: SCN2A_HUMAN) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/18501613) Sodium channel protein type 5 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q14524, gene: SCN5A, swissprot: SCN5A_HUMAN) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/18501613) Sodium channel protein type 11 subunit alpha (Organism: Rattus norvegicus, class: Ion channel, accessions: O88457, gene: Scn11a, swissprot: SCNBA_RAT) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/18501613) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/21300721) Aryl hydrocarbon receptor (Organism: Homo sapiens, class: Transcription factor, accessions: P35869, gene: AHR, swissprot: AHR_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/17327465) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/9690950) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/9690950) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12519691) Cytochrome P450 2E1 (Organism: Homo sapiens, class: Enzyme, accessions: P05181, gene: CYP2E1, swissprot: CP2E1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12519691) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10215663) Mexiletine is a local anesthetic, antiarrhythmic agent (Class Ib), structurally similar to lidocaine, but orally active. Mexiletine, like lidocaine, inhibits the inward sodium current required for the initiation and conduction of impulses, thus reducing the rate of rise of the action potential, Phase 0. Mexiletine is used for the treatment of ventricular tachycardia and symptomatic premature ventricular beats, and prevention of ventricular fibrillation. anti-arrhythmia drug (Code: CHEBI:38070) Antiarrhythmic (Code: N0000175426) Anti-Arrhythmia Agents (Code: D000889) Cardiovascular Agents (Code: D002317) Membrane Transport Modulators (Code: D049990) Sodium Channel Blockers (Code: D026941) Voltage-Gated Sodium Channel Blockers (Code: D061567) 1985-12-30 FDA 505
Click to view methoxyphenamine Methoxyphenamine (2-methoxy-N-methylamphetamine) is an amphetamine methylated on nitrogen and with the phenyl ring methoxylated at C-2. Methoxyphenamine is a beta adrenergic receptor agonist. Methoxyphenamine is used as a bronchodilator to treat asthma, chronic bronchitis, respiratory tract infections with cough and. In addition, methoxyphenamine using is prohibited in sports according to the regulations of the World Anti-Doping Agency (WADA). Adrenergic Agents (Code: D018663) Adrenergic Agonists (Code: D000322) Adrenergic beta-Agonists (Code: D000318) Neurotransmitter Agents (Code: D018377) 1969-12-31 New Zealand Medicines and Medical Devices Safety Authority
Click to view memantine Glutamate receptor ionotropic, NMDA 3A (Organism: Homo sapiens, class: Ion channel, accessions: Q8TCU5, gene: GRIN3A, swissprot: NMD3A_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021487s025lbl.pdf) Glutamate receptor ionotropic, NMDA 1 (Organism: Homo sapiens, class: Ion channel, accessions: Q05586, gene: GRIN1, swissprot: NMDZ1_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021487s025lbl.pdf) Glutamate receptor ionotropic, NMDA 2A (Organism: Homo sapiens, class: Ion channel, accessions: Q12879, gene: GRIN2A, swissprot: NMDE1_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021487s025lbl.pdf) Glutamate receptor ionotropic, NMDA 2B (Organism: Homo sapiens, class: Ion channel, accessions: Q13224, gene: GRIN2B, swissprot: NMDE2_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021487s025lbl.pdf) Glutamate receptor ionotropic, NMDA 2C (Organism: Homo sapiens, class: Ion channel, accessions: Q14957, gene: GRIN2C, swissprot: NMDE3_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021487s025lbl.pdf) Glutamate receptor ionotropic, NMDA 2D (Organism: Homo sapiens, class: Ion channel, accessions: O15399, gene: GRIN2D, swissprot: NMDE4_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021487s025lbl.pdf) Glutamate receptor ionotropic, NMDA 3B (Organism: Homo sapiens, class: Ion channel, accessions: O60391, gene: GRIN3B, swissprot: NMD3B_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021487s025lbl.pdf) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15378224) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15378224) Solute carrier family 22 member 1 (Organism: Homo sapiens, class: Transporter, accessions: O15245, gene: SLC22A1, swissprot: S22A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18788725) Memantine is an oral N-methyl-D-aspartate glutamate receptor antagonist used in the therapy of Alzheimer disease and dementia. dopaminergic agent (Code: CHEBI:48560) antiparkinson drug (Code: CHEBI:48407) neuroprotective agent (Code: CHEBI:63726) antidepressant (Code: CHEBI:35469) Anti-Dyskinesia Agents (Code: D018726) Antiparkinson Agents (Code: D000978) Central Nervous System Agents (Code: D002491) Dopamine Agents (Code: D015259) Excitatory Amino Acid Agents (Code: D018683) Excitatory Amino Acid Antagonists (Code: D018691) Neurotransmitter Agents (Code: D018377) NMDA Receptor Antagonists (Code: N0000020015) N-methyl-D-aspartate Receptor Antagonist (Code: N0000175745) 2003-10-16 FDA 377
Click to view cloxiquine Catechol O-methyltransferase (Organism: Rattus norvegicus, class: Enzyme, accessions: P22734, gene: Comt, swissprot: COMT_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/817025) Methionine aminopeptidase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P50579, gene: METAP2, swissprot: MAP2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22391578) Methionine aminopeptidase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P53582, gene: METAP1, swissprot: MAP11_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22391578) Potassium channel subfamily K member 18 (Organism: Homo sapiens, class: Ion channel, accessions: Q7Z418, gene: KCNK18, swissprot: KCNKI_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/24383077) Cloxyquin is a monohalogenated 8-hydroxyquinoline with activity against bacteria, fungi, and protozoa. Cloxyquin is reported to have activity against Mycobacterium tuberculosis, including strains that show resistance to common first-line antibacterial agents.
Click to view flurotyl Flurothyl is a volatile convulsant acting as a GABAA antagonist that was extensively used historically to induce seizures in severely depressed patients as an alternative to electroconvulsive shock therapy. The main current use of flurothyl is in scientific research for inducing seizures in laboratory animals. Central Nervous System Agents (Code: D002491) Central Nervous System Stimulants (Code: D000697) Convulsants (Code: D003292) 1964 FDA
Click to view inositol Sodium/myo-inositol cotransporter 2 (Organism: Homo sapiens, class: Transporter, accessions: Q8WWX8, gene: SLC5A11, swissprot: SC5AB_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12133831) Inositol is a collection of nine different stereoisomers but the name is usually used to describe only the most common type of inositol, myo-inositol. Myo-inositol is the cis-1,2,3,5-trans-4,6-cyclohexanehexol and it is prepared from an aqueous extract of corn kernels by precipitation and hydrolysis of crude phytate. These molecules have structural similarities to glucose and are involved in cellular signaling. It is considered a pseudovitamin as it is a molecule that does not qualify to be an essential vitamin because even though its presence is vital in the body, a deficiency in this molecule does not translate into disease conditions. Growth Substances (Code: D006133) Micronutrients (Code: D018977) Vitamins (Code: D014815) Vitamin B Complex (Code: D014803) 1949 FDA INS
Click to view galactose An aldohexose that occurs naturally in the D-form in lactose, cerebrosides, gangliosides, and mucoproteins. Deficiency of galactosyl-1-phosphate uridyltransferase (GALACTOSE-1-PHOSPHATE URIDYL-TRANSFERASE DEFICIENCY DISEASE) causes an error in galactose metabolism called GALACTOSEMIA, resulting in elevations of galactose in the blood.
Click to view fructose Solute carrier family 2, facilitated glucose transporter member 2 (Organism: Homo sapiens, class: Transporter, accessions: P11168, gene: SLC2A2, swissprot: GTR2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/23396969) Solute carrier family 2, facilitated glucose transporter member 8 (Organism: Rattus norvegicus, class: Transporter, accessions: Q9JJZ1, gene: Slc2a8, swissprot: GTR8_RAT) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/23396969) Ketohexokinase (Organism: Homo sapiens, class: Enzyme, accessions: P50053, gene: KHK, swissprot: KHK_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12941785) Sorbitol dehydrogenase (Organism: Homo sapiens, class: Enzyme, accessions: Q00796, gene: SORD, swissprot: DHSO_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12962626) Hexokinase-4 (Organism: Homo sapiens, class: Enzyme, accessions: P35557, gene: GCK, swissprot: HXK4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/7742312) Fructose is a monosaccharide in sweet fruits and honey that is soluble in water, alcohol, or ether. Fructose is one of the three dietary monosaccharides, along with glucose and galactose, that are absorbed directly into the bloodstream. It is used as a preservative and an intravenous infusion in parenteral feeding. Flavoring Agents (Code: D005421) Food Additives (Code: D005503) Sweetening Agents (Code: D013549) 1953 FDA Z9N
FRU
Click to view acetylsalicylic acid Prostaglandin G/H synthase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P23219, gene: PTGS1, swissprot: PGH1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/200671s000lbl.pdf) Prostaglandin G/H synthase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P35354, gene: PTGS2, swissprot: PGH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17480099) Solute carrier family 22 member 6 (Organism: Rattus norvegicus, class: Transporter, accessions: O35956, gene: Slc22a6, swissprot: S22A6_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10220563) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/24107783) Solute carrier family 22 member 8 (Organism: Homo sapiens, class: Transporter, accessions: Q8TCC7, gene: SLC22A8, swissprot: S22A8_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/24692216) Endothelin-1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P25101, gene: EDNRA, swissprot: EDNRA_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10727528) Acid-sensing ion channel 3 (Organism: Homo sapiens, class: Ion channel, accessions: Q9UHC3, gene: ASIC3, swissprot: ASIC3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11588175) Acetylsalicylic acid (also known as aspirin) is a prototypical analgesic used in the treatment of mild to moderate pain. It has anti-inflammatory and antipyretic properties and acts as an inhibitor of cyclooxygenase which results in the inhibition of the biosynthesis of prostaglandins. Acetylsalicylic acid is indicated for the relief of pain, fever and inflammation of a variety of conditions such as influenza, common cold, low back and neck pain, dysmenorrhea, headache, toothache, sprains and strains, fractures, myositis, neuralgia, synovitis, arthritis, bursitis, burns, injuries, following surgical and dental procedures. Acetylsalicylic acid also inhibits platelet aggregation and is used in the prevention of arterial and venous thrombosis. plant activator (Code: CHEBI:73182) drug allergen (Code: CHEBI:88188) platelet aggregation inhibitor (Code: CHEBI:50427) antipyretic (Code: CHEBI:35493) prostaglandin antagonist (Code: CHEBI:49023) anticoagulant (Code: CHEBI:50249) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) non-narcotic analgesic (Code: CHEBI:35481) Decreased Prostaglandin Production (Code: N0000008836) Nonsteroidal Anti-inflammatory Compounds (Code: N0000175721) Nonsteroidal Anti-inflammatory Drug (Code: N0000175722) Decreased Platelet Aggregation (Code: N0000008832) Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antipyretics (Code: D058633) Antirheumatic Agents (Code: D018501) Cardiovascular Agents (Code: D002317) Cyclooxygenase Inhibitors (Code: D016861) Enzyme Inhibitors (Code: D004791) Fibrin Modulating Agents (Code: D050299) Fibrinolytic Agents (Code: D005343) Hematologic Agents (Code: D006401) Peripheral Nervous System Agents (Code: D018373) Platelet Aggregation Inhibitors (Code: D010975) Sensory System Agents (Code: D018689) 1898-01-01 YEAR INTRODUCED AIN
Click to view clorindione Arachidonate 5-lipoxygenase (Organism: Rattus norvegicus, class: Enzyme, accessions: P12527, gene: Alox5, swissprot: LOX5_RAT) inhibitor (Source: https://www.sciencedirect.com/science/article/pii/S0960894X0080236X) Clorindione is a vitamin K antagonists, and is a derivative of phenindione. It has been demonstrated as effective in reducing prothrombin levels in humans. Clorindione is used as a long-acting anticoagulant.
Click to view theophylline cAMP-specific 3',5'-cyclic phosphodiesterase 4A (Organism: Homo sapiens, class: Enzyme, accessions: P27815, gene: PDE4A, swissprot: PDE4A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12421478) cGMP-inhibited 3',5'-cyclic phosphodiesterase A (Organism: Homo sapiens, class: Enzyme, accessions: Q14432, gene: PDE3A, swissprot: PDE3A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12887610) Histone deacetylase 1 (Organism: Homo sapiens, class: Enzyme, accessions: Q13547, gene: HDAC1, swissprot: HDAC1_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/12070353) Histone deacetylase 2 (Organism: Homo sapiens, class: Enzyme, accessions: Q92769, gene: HDAC2, swissprot: HDAC2_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/12070353) Histone deacetylase 3 (Organism: Homo sapiens, class: Enzyme, accessions: O15379, gene: HDAC3, swissprot: HDAC3_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/12070353) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/019211s042lbl.pdf) Cytochrome P450 2E1 (Organism: Homo sapiens, class: Enzyme, accessions: P05181, gene: CYP2E1, swissprot: CP2E1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/019211s042lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/019211s042lbl.pdf) Cytochrome P450 1A1 (Organism: Homo sapiens, class: Enzyme, accessions: P04798, gene: CYP1A1, swissprot: CP1A1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/7619675) Solute carrier family 22 member 7 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y694, gene: SLC22A7, swissprot: S22A7_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15708966) Solute carrier family 22 member 7 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y694, gene: SLC22A7, swissprot: S22A7_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15708966) Adenosine receptor A2b (Organism: Homo sapiens, class: GPCR, accessions: P29275, gene: ADORA2B, swissprot: AA2BR_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12014951) Adenosine receptor A1 (Organism: Homo sapiens, class: GPCR, accessions: P30542, gene: ADORA1, swissprot: AA1R_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/6279840) Adenosine receptor A2a (Organism: Homo sapiens, class: GPCR, accessions: P29274, gene: ADORA2A, swissprot: AA2AR_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/6279840) Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform (Organism: Homo sapiens, class: Kinase, accessions: O00329, gene: PIK3CD, swissprot: PK3CD_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12145276) Theophylline is a natural alkaloid derivative of xanthine isolated from the plants Camellia sinensis and Coffea arabica. Theophylline appears to inhibit phosphodiesterase and prostaglandin production, regulate calcium flux and intracellular calcium distribution, and antagonize adenosine. Physiologically, this agent relaxes bronchial smooth muscle, produces vasodilation (except in cerebral vessels), stimulates the CNS, stimulates cardiac muscle, induces diuresis, and increases gastric acid secretion; it may also suppress inflammation and improve contractility of the diaphragm. muscle relaxant (Code: CHEBI:51371) bronchodilator agent (Code: CHEBI:35523) vasodilator agent (Code: CHEBI:35620) immunomodulator (Code: CHEBI:50846) anti-inflammatory agent (Code: CHEBI:67079) anti-asthmatic drug (Code: CHEBI:49167) Anti-Asthmatic Agents (Code: D018927) Autonomic Agents (Code: D001337) Bronchodilator Agents (Code: D001993) Cardiotonic Agents (Code: D002316) Cardiovascular Agents (Code: D002317) Enzyme Inhibitors (Code: D004791) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Phosphodiesterase Inhibitors (Code: D010726) Protective Agents (Code: D020011) Purinergic Agents (Code: D058905) Purinergic Antagonists (Code: D058914) Purinergic P1 Receptor Antagonists (Code: D058915) Respiratory System Agents (Code: D019141) Vasodilator Agents (Code: D014665) Methylxanthine (Code: N0000175790) Xanthines (Code: N0000008118) 1947-10-17 FDA TEP
Click to view theobromine 3,7-Dimethylxanthine. The principle alkaloid in Theobroma cacao (the cacao bean) and other plants. A xanthine alkaloid that is used as a bronchodilator and as a vasodilator. It has a weaker diuretic activity than THEOPHYLLINE and is also a less powerful stimulant of smooth muscle. It has practically no stimulant effect on the central nervous system. It was formerly used as a diuretic and in the treatment of angina pectoris and hypertension. (From Martindale, The Extra Pharmacopoeia, 30th ed, pp1318-9) vasodilator agent (Code: CHEBI:35620) bronchodilator agent (Code: CHEBI:35523) Anti-Asthmatic Agents (Code: D018927) Autonomic Agents (Code: D001337) Bronchodilator Agents (Code: D001993) Cardiovascular Agents (Code: D002317) Peripheral Nervous System Agents (Code: D018373) Respiratory System Agents (Code: D019141) Vasodilator Agents (Code: D014665) 37T
Click to view propylparaben Propylparaben is an ester of p-hydroxybenzoic acid. Propylparaben is a chemical allergen capable of producing immunologically mediated hypersensitivity reactions. It is used as a bacteriostatic, fungistatic agent and preservative in cosmetic products, food and drugs. It has the number E216 as a food additive. Also propylparaben is used in allergenic testing. Standardized Chemical Allergen (Code: N0000185508) Increased Histamine Release (Code: N0000175629) Cell-mediated Immunity (Code: N0000184306) Allergens (Code: N0000171131) Pharmaceutic Aids (Code: D010592) Preservatives, Pharmaceutical (Code: D011310) 36M
Click to view mephenesin Mephenesin is a centrally acting muscle relaxant with a short duration of action. The exact mechanism of action of mephenesin is not known. It has been observed to block both inward sodium and inward calcium currents in neurons. It is used as an adjunctive treatment of muscle pain. Central Nervous System Agents (Code: D002491) Muscle Relaxants, Central (Code: D009125) Neuromuscular Agents (Code: D009465) Peripheral Nervous System Agents (Code: D018373) 1996-06-24 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view rilmenidine Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/27265687) Nischarin (Organism: Homo sapiens, class: Cytosolic other, accessions: Q9Y2I1, gene: NISCH, swissprot: NISCH_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12065769) Rilmenidine is a centrally-acting antihypertensive. It acts through stimulation of central imidazoline receptors and has alpha2-adrenoceptor agonist activity. Rilmenidine is used for the treatment of hypertension. Adrenergic Agents (Code: D018663) Adrenergic Agonists (Code: D000322) Adrenergic alpha-Agonists (Code: D000316) Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377) 1995-02-21 CDSCO (INDIA)
Click to view tyrosine A non-essential amino acid. In animals it is synthesized from PHENYLALANINE. It is also the precursor of EPINEPHRINE; THYROID HORMONES; and melanin. 1975 FDA DTY
TYR
Click to view styramate Styramate is a centrally acting skeletal muscle relaxant that was used in the symptomatic treatment of painful muscle spasm associated with musculoskeletal conditions.
Click to view adrenalone Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/21885739) Adrenalone is a keton form of the natural epinephrine. It is an adrenergic receptor agonist. Adrenalone inhibits the norepinephrine synthesis and dopamine beta oxidase. Adrenalone has the high radioprotective effect. Adrenalone has hemostatic, sympathomimetic and vasoconstrictor properties. It was used as a topical nasal decongestant. Cardiovascular Agents (Code: D002317) Coagulants (Code: D003029) Hematologic Agents (Code: D006401) Hemostatics (Code: D006490) Vasoconstrictor Agents (Code: D014662)
Click to view acamprosate Glutamate NMDA receptor; GRIN1/GRIN2A (Organism: Homo sapiens, class: Ion channel, accessions: Q05586|Q12879, gene: GRIN1|GRIN2A, swissprot: NMDE1_HUMAN|NMDZ1_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/11369029) Glutamate NMDA receptor; GRIN1/GRIN2B (Organism: Homo sapiens, class: Ion channel, accessions: Q05586|Q13224, gene: GRIN1|GRIN2B, swissprot: NMDE2_HUMAN|NMDZ1_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/11369029) Acamprosate is a synthetic compound with a chemical structure similar to that of the endogenous amino acid homotaurine, which is a structural analogue of the amino acid neurotransmitter gamma-aminobutyric acid and the amino acid neuromodulator taurine. The mechanism of action of acamprosate in maintenance of alcohol abstinence is not completely understood. In vitro and in vivo studies in animals have provided evidence to suggest acamprosate may interact with glutamate and GABA neurotransmitter systems centrally, and has led to the hypothesis that acamprosate restores balance between neuronal excitation and inhibition. Acamprosate is indicated for the maintenance of abstinence from alcohol in patients with alcohol dependence who are abstinent at treatment initiation. neurotransmitter agent (Code: CHEBI:35942) Alcohol Deterrents (Code: D000427) Central Nervous System Agents (Code: D002491) 2004-07-29 FDA
Click to view pyridostigmine Acetylcholinesterase (Organism: Homo sapiens, class: Enzyme, accessions: P22303, gene: ACHE, swissprot: ACES_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2004/17398s015lbl.pdf) Cholinesterase (Organism: Homo sapiens, class: Enzyme, accessions: P06276, gene: BCHE, swissprot: CHLE_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/2738887) Pyridostigmine is a cholinesterase inhibitor with a slightly longer duration of action than neostigmine. It is used in the treatment of myasthenia gravis and to reverse the actions of muscle relaxants. Cholinesterase Inhibitor (Code: N0000175723) Cholinergic Agents (Code: D018678) Cholinesterase Inhibitors (Code: D002800) Enzyme Inhibitors (Code: D004791) Neurotransmitter Agents (Code: D018377) 1955-04-06 FDA
Click to view oxilofrine Oxilofrine is a metabolite of p-methoxymethamphetamine. Oxilofrine is a stimulant and a sympathomimetic. It was used to treat hypotensive states, with actions similar to those of ephedrine.
Click to view hexapropymate Hexapropymate is a carbamate hypnotic substance with properties similar to those of the barbiturates. Hexapropymate produces CNS depressant effects through an unknown mechanism. Hexapropymate was used as a hypnotic and sedative drug.
Click to view etilefrine Beta-1 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08588, gene: ADRB1, swissprot: ADRB1_HUMAN) agonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/4396765) A phenylephrine-related beta-1 adrenergic and alpha adrenergic agonist used as a cardiotonic and antihypotensive agent. Adrenergic Agents (Code: D018663) Adrenergic Agonists (Code: D000322) Adrenergic alpha-Agonists (Code: D000316) Adrenergic beta-1 Receptor Agonists (Code: D058665) Adrenergic beta-Agonists (Code: D000318) Autonomic Agents (Code: D001337) Cardiotonic Agents (Code: D002316) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Protective Agents (Code: D020011) Sympathomimetics (Code: D013566) Vasoconstrictor Agents (Code: D014662) 1929-01-01 YEAR INTRODUCED
Click to view eflornithine Ornithine decarboxylase (Organism: Homo sapiens, class: Enzyme, accessions: P11926, gene: ODC1, swissprot: DCOR_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2000/21145lbl.pdf) Eflornithine is a difluoromethylated ornithine compound with antineoplastic activity. Eflornithine irreversibly inhibits skin ODC activity. This enzyme is necessary in the synthesis of polyamines. Animal data indicate that inhibition of ornithine decarboxylase inhibits cell division and synthetic functions, which affect the rate of hair growth. Eflornithine is indicated for the reduction of unwanted facial hair in women. Eflornithine is on the World Health Organization's List of Essential Medicines as the drug for the treatment of Trypanosoma brucei gambiense infection. Antiprotozoal (Code: N0000175485) Decarboxylase Inhibitor (Code: N0000175845) Decarboxylase Inhibitors (Code: N0000175844) Anti-Infective Agents (Code: D000890) Antineoplastic Agents (Code: D000970) Antiparasitic Agents (Code: D000977) Antiprotozoal Agents (Code: D000981) Enzyme Inhibitors (Code: D004791) Ornithine Decarboxylase Inhibitors (Code: D065108) Trypanocidal Agents (Code: D014344) 1990-11-28 FDA DMO
Click to view mannitol Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12954186) Mannitol is an osmotic diuretic that is metabolically inert in humans and occurs naturally, as a sugar or sugar alcohol, in fruits and vegetables. Mannitol elevates blood plasma osmolality, resulting in enhanced flow of water from tissues, including the brain and cerebrospinal fluid, into interstitial fluid and plasma. As a result, cerebral edema, elevated intracranial pressure, and cerebrospinal fluid volume and pressure may be reduced. Sorbitol is an isomer of mannitol, the two differ only in the orientation of the hydroxyl group on carbon 2. While similar, the two sugar alcohols have very different uses. Mannitol is used for the promotion of diuresis before irreversible renal failure becomes established, the reduction of intracranial pressure, the treatment of cerebral edema, and the promotion of urinary excretion of toxic substances. Also mannitol is indicated for the assessment of bronchial hyperresponsiveness in patients 6 years of age or older who do not have clinically apparent asthma. Sorbitol is used as a non-stimulant laxative via an oral suspension or enema. In addition, sorbitol has one-third fewer calories and 60 % the sweetening activity of sucrose and is used as a sugar replacement in diabetes. Increased Diuresis (Code: N0000175359) Osmotic Activity (Code: N0000010288) Osmotic Diuretic (Code: N0000175810) Diuretics (Code: D004232) Diuretics, Osmotic (Code: D004234) Flavoring Agents (Code: D005421) Food Additives (Code: D005503) Natriuretic Agents (Code: D045283) Sweetening Agents (Code: D013549) mannitol: 1964-06-08 FDA sorbitol: 1971-08-20 FDA MTL
SOR
Click to view glycol salicylate component of Piadar; topical ointment of the above including 1% methanol in base FDA
Click to view sparteine A quinolizidine alkaloid isolated from several FABACEAE including LUPINUS; SPARTIUM; and CYTISUS. It has been used as an oxytocic and an anti-arrhythmia agent. It has also been of interest as an indicator of CYP2D6 genotype. Anti-Arrhythmia Agents (Code: D000889) Cardiovascular Agents (Code: D002317) Oxytocics (Code: D010120) Reproductive Control Agents (Code: D012102)
Click to view flopropione Catechol O-methyltransferase (Organism: Homo sapiens, class: Enzyme, accessions: P21964, gene: COMT, swissprot: COMT_HUMAN) inhibitor (Source: http://eisai.jp/medical/products/di/EPI/CSP_C_EPI.pdf) The mechanism of action is considered to be based on the inhibition of catechol-o-methyl-transferase (COMT), resulting in an adrenergic action, and anti-serotonin action
Click to view dacarbazine 6-phosphogluconate dehydrogenase, decarboxylating (Organism: Homo sapiens, class: Enzyme, accessions: P52209, gene: PGD, swissprot: 6PGD_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20235752) Cytochrome P450 1A1 (Organism: Homo sapiens, class: Enzyme, accessions: P04798, gene: CYP1A1, swissprot: CP1A1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10473105) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10473105) Cytochrome P450 2E1 (Organism: Homo sapiens, class: Enzyme, accessions: P05181, gene: CYP2E1, swissprot: CP2E1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10473105) Dacarbazine is a cell-cycle, non-specific antineoplastic agent. It is a structural analogue of 5-amino-imidazole-4-carboxamide which is an intermediate in purine biosynthesis. The exact mechanism of action of dacarbazine is not known. It may function as an alkylating agent, possibly after activation by metabolism in the liver, but other hypotheses, including inhibition of DNA synthesis by acting as a purine analogue and interaction with sulfhydryl groups, have also been proposed. Dacarbazine is inactive until metabolized in the liver by cytochromes P450 to form the reactive N-demethylated species 5-[3-hydroxymethyl-3-methyl-triazen-1-yl]-imidazole-4-carboxamide (HMMTIC) and 5-[3-methyl-triazen-1-yl]-imidazole-4-carboxamide (MTIC). Dacarbazine is used for the palliative therapy of metastatic malignant melanoma. In addition, this drug also is indicated for Hodgkin’s disease as a second-line therapy when used in combination with other effective agents. antineoplastic agent (Code: CHEBI:35610) prodrug (Code: CHEBI:50266) Alkylating Activity (Code: N0000000236) Alkylating Drug (Code: N0000175558) Alkylating Agents (Code: D000477) Antineoplastic Agents (Code: D000970) Antineoplastic Agents, Alkylating (Code: D018906) Noxae (Code: D009676) 1975-05-27 FDA
Click to view succimer lead (Organism: None, class: Inorganic material, accessions: None, gene: None, swissprot: None) chelating agent (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2007/019998s013lbl.pdf) Succimer is a mercaptodicarboxylic acid used as an antidote to heavy metal poisoning because it forms strong chelates with them. Succimer is an analogue of dimercaprol. The advantages of succimer are that it is effective by oral administration because it is soluble in water, it is well-tolerated, has relatively low toxicity and can be given at the same time as iron supplements to treat iron deficiency anaemia. It is used in the management of poisoning by lead and other heavy metals. Lead Chelating Activity (Code: N0000175962) Lead Chelator (Code: N0000175963) Antidotes (Code: D000931) Chelating Agents (Code: D002614) Protective Agents (Code: D020011) Sequestering Agents (Code: D064449) 1991-01-30 FDA
Click to view guanacline Guanacline is a sympatholytic agent with limited post-ganglionic sympathetic blocking action and prolonged catecholamine depletion. It was used for the treatment of hypotension. Its use was discontinued due to cases of persistent orthostatic hypotension after treatment with guanacline.
Click to view chlorphentermine Chlorphentermine is a synthetic amphetamine derivative which exerts anorectic properties. Chlorphentermine is a relatively weak stimulant with little abuse potential. It presents a prominent serotonergic profile leading to pulmonary hypertension and cardiac fibrosis after prolonged use. It was used as an appetite suppressant but is no longer used. Autonomic Agents (Code: D001337) Peripheral Nervous System Agents (Code: D018373) Sympathomimetics (Code: D013566) 1982-01-01 FDA
Click to view epinephrine Alpha-1D adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P25100, gene: ADRA1D, swissprot: ADA1D_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/019430s074lbl.pdf) Alpha-1B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35368, gene: ADRA1B, swissprot: ADA1B_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/019430s074lbl.pdf) Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/019430s074lbl.pdf) Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/019430s074lbl.pdf) Alpha-2C adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18825, gene: ADRA2C, swissprot: ADA2C_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/019430s074lbl.pdf) Beta-2 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P07550, gene: ADRB2, swissprot: ADRB2_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/019430s074lbl.pdf) Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/019430s074lbl.pdf) Beta-1 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08588, gene: ADRB1, swissprot: ADRB1_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/019430s074lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19356039) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19356039) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19356039) Amine oxidase [flavin-containing] A (Organism: Rattus norvegicus, class: Enzyme, accessions: P21396, gene: Maoa, swissprot: AOFA_RAT) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/8138937) Amine oxidase [flavin-containing] B (Organism: Rattus norvegicus, class: Enzyme, accessions: P19643, gene: Maob, swissprot: AOFB_RAT) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/8138937) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/9812985) Solute carrier family 22 member 1 (Organism: Homo sapiens, class: Transporter, accessions: O15245, gene: SLC22A1, swissprot: S22A1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/9776363) Carbonic anhydrase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P00915, gene: CA1, swissprot: CAH1_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/17127057) Carbonic anhydrase 14 (Organism: Homo sapiens, class: Enzyme, accessions: Q9ULX7, gene: CA14, swissprot: CAH14_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/17127057) Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/17127057) Carbonic anhydrase 3 (Organism: Homo sapiens, class: Enzyme, accessions: P07451, gene: CA3, swissprot: CAH3_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/17127057) Carbonic anhydrase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P22748, gene: CA4, swissprot: CAH4_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/17127057) Carbonic anhydrase 5A, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P35218, gene: CA5A, swissprot: CAH5A_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/17127057) Carbonic anhydrase 7 (Organism: Homo sapiens, class: Enzyme, accessions: P43166, gene: CA7, swissprot: CAH7_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/17127057) Chromaffin granule amine transporter (Organism: Homo sapiens, class: Transporter, accessions: P54219, gene: SLC18A1, swissprot: VMAT1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/8643547) Synaptic vesicular amine transporter (Organism: Homo sapiens, class: Transporter, accessions: Q05940, gene: SLC18A2, swissprot: VMAT2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/8643547) Epinephrine (adrenaline) is a sympathomimetic catecholamine. Epinephrine is produced by the adrenal glands and used as a drug due to its various important functions.Epinephrine acts on both alpha-and beta-adrenergic receptors. Through its action on alpha-adrenergic receptors, epinephrine lessens the vasodilation and increased vascular permeability that occurs during anaphylaxis, which can lead to loss of intravascular fluid volume and hypotension. Through its action on beta-adrenergic receptors, epinephrine causes bronchial smooth muscle relaxation and helps alleviate bronchospasm, wheezing and dyspnea that may occur during anaphylaxis. Racepinephrine is a racemic mixture consisting of inactive d-Epinephrine and active l-Epinephrine enantiomers. Epinephrine is indicated in the emergency treatment of allergic reactions (Type I) including anaphylaxis. Epinephrine's cardiac effects may be of use in restoring cardiac rhythm in cardiac arrest due to various causes but is not used in cardiac failure or in hemorrhagic, traumatic, or cardiogenic shock. Epinephrine also is used as a hemostatic agent. It is also used in treating mucosal congestion of hay fever, rhinitis, and acute sinusitis; to relieve bronchial asthmatic paroxysms; in syncope due to complete heart block or carotid sinus hypersensitivity; for symptomatic relief of serum sickness, urticaria, angioneurotic edema; for resuscitation in cardiac arrest following anesthetic accidents; in simple (open angle) glaucoma; for relaxation of uterine musculature and to inhibit uterine contractions. Epinephrine injection can be utilized to prolong the action of local anesthetics. alpha-Adrenergic Agonist (Code: N0000175552) beta-Adrenergic Agonist (Code: N0000175555) Catecholamine (Code: N0000175570) Catecholamines (Code: N0000007715) Adrenergic Agents (Code: D018663) Adrenergic Agonists (Code: D000322) Adrenergic alpha-Agonists (Code: D000316) Adrenergic beta-Agonists (Code: D000318) Anti-Asthmatic Agents (Code: D018927) Autonomic Agents (Code: D001337) Bronchodilator Agents (Code: D001993) Cardiovascular Agents (Code: D002317) Mydriatics (Code: D009184) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Respiratory System Agents (Code: D019141) Sympathomimetics (Code: D013566) Vasoconstrictor Agents (Code: D014662) 1948-11-19 FDA ALE
XDE
Click to view methyprylon Methyprylon, a piperidinedione CNS depressant, is close to barbituric acid in structure, but different enough to be called a "non-barbiturate" sedative-hynotic. Methyprylon depresses the activity of muscle tissues, the heart, and the respiratory system. Methyprylon binds at a distinct binding site associated with a Cl- ionopore at the GABAA receptor, increasing the duration of time for which the Cl- ionopore is open. The post-synaptic inhibitory effect of GABA in the thalamus is, therefore, prolonged. Methyprylon was used for the treatment of insomnia and daytime tension but was withdrawn from the market due to adverse events. 1955-01-18 FDA
Click to view epomediol marked choleretic activity in Wistar rats; mechanism of action may be related to increases in both the bile salt dependent & independent fractions of bile Cholagogues and Choleretics (Code: D002756) Gastrointestinal Agents (Code: D005765)
Click to view clortermine Clortermine is a sympathomimetic amine with infrequent and mild CNS stimulant activity. Clortermine is an appetite suppressant. It was used for the adjunctivetreatment of exogenous obesity. Now it is a a "controlled substance" in schedule II of the US Federal Controlled Substances Act.
Click to view domiodol Domiodol (4-hydroxymethyl-2-indomethyl-2,3-dioxolane) is a compound containing organically bound iodine. In animal studies domiodol induced a dose-related increase in respiratory tract fluid and reduced the viscosity of sputum.
Click to view phosphorylcholine Phosphorylcholine (PC) is a small zwitterionic amino alcohol, which is composed of a negatively charged phosphate bonded to a small, positively charged choline group. Phosphorylcholine is the precursor metabolite of choline in the glycine, serine, and threonine metabolism pathways and in intermediate between choline and cytidine-diphosphate choline in the glycerophospholipid metabolism pathway. Phosphorylcholine is an immunodominant determinant of pneumococcal teichoic acids and also a major prerequisite for proinflammatory effects of PAF and PAF-like lipids. PC is also a component of some bacteria, apoptotic cells, and OxLDL, which, if exposed, is immunogenic. PC has several properties that could in principle both promote and protect against disease, depending on the pathogen and type of inflammatory reaction. In the field of interventional cardiology, phosphorylcholine is used as a synthetic polymer-based coating, applied to drug-eluting stents, to prevent the occurrence of coronary artery restenosis. PC
Click to view azelaic acid 3-oxo-5-alpha-steroid 4-dehydrogenase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P31213, gene: SRD5A2, swissprot: S5A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/3207614) Azelaic acid is a naturally occurring dicarboxylic acid produced by Malassezia furfur and found in whole grain cereals, rye, barley and animal products. Azelaic acid possesses antibacterial, keratolytic, comedolytic, and anti-oxidant activity. Azelaic acid is bactericidal against Proprionibacterium acnes and Staphylococcus epidermidis due to its inhibitory effect on the synthesis of microbial cellular proteins. Azelaic acid exerts its keratolytic and comedolytic effects by reducing the thickness of the stratum corneum and decreasing the number of keratohyalin granules by reducing the amount and distribution of filaggrin in epidermal layers. Azelaic acid also possesses a direct anti-inflammatory effect due to its scavenger activity of free oxygen radical. This drug is used topically to reduce inflammation associated with acne and rosacea. antineoplastic agent (Code: CHEBI:35610) dermatologic drug (Code: CHEBI:50177) Decreased Protein Synthesis (Code: N0000008841) Decreased Sebaceous Gland Activity (Code: N0000009982) Antineoplastic Agents (Code: D000970) Dermatologic Agents (Code: D003879) 1995-09-13 FDA AZ1
Click to view barbital A long-acting barbiturate that depresses most metabolic processes at high doses. It is used as a hypnotic and sedative and may induce dependence. Barbital is also used in veterinary practice for central nervous system depression. Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) GABA Agents (Code: D018682) GABA Modulators (Code: D018757) Hypnotics and Sedatives (Code: D006993) Neurotransmitter Agents (Code: D018377)
Click to view mitoguazone S-adenosylmethionine decarboxylase proenzyme (Organism: Rattus norvegicus, class: Enzyme, accessions: P17708, gene: Amd1, swissprot: DCAM_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/8421290) Amiloride-sensitive amine oxidase [copper-containing] (Organism: Rattus norvegicus, class: Enzyme, accessions: P36633, gene: Aoc1, swissprot: AOC1_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/8421290) Mitoguazone is a guanylhydrazone with potential antineoplastic activity. Mitoguazone is obtained by formal condensation of the two carbonyl groups of methylglyoxal with the primary amino groups of two molecules of aminoguanidine. Mitoguazone competitively inhibits S-adenosyl-L-methionine decarboxylase (SAMD), an enzyme involved in the synthesis of polyamines, resulting in decreased proliferation of tumor cells, antimitochondrial effects, and p53-independent apoptosis. Mitoguazone has been used for the treatment of Hodgkin's disease, Non-Hodgkin's leukemias and malignant lymphomas and of Squamous cell carcinomas of the upper respiratory tract. Mitoguazone is no longer available. antineoplastic agent (Code: CHEBI:35610) Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) 1998-04-17 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view enflurane Cytochrome P450 2E1 (Organism: Homo sapiens, class: Enzyme, accessions: P05181, gene: CYP2E1, swissprot: CP2E1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/8689955) Enflurane is a general inhalation anesthetic drug. Induction of and recovery from anesthesia with enflurane are rapid. Enflurane has a mild, sweet odor. Enflurane may provide a mild stimulus to salivation or tracheobronchial secretions. Pharyngeal and laryngeal reflexes are readily obtunded. The level of anesthesia can be changed rapidly by changing the inspired enflurane concentration. Enflurane reduces ventilation as depth of anesthesia increases. Enflurane may be used for induction and maintenance of general anesthesia. Enflurane may be used to provide analgesia for vaginal delivery. Low concentrations of enflurane may also be used to supplement other general anesthetic agents during delivery by Cesarean section. Higher concentrations of enflurane may produce uterine relaxation and an increase in uterine bleeding. It was increasingly used for inhalational anesthesia during the 1970s and 1980s but is no longer in common use. anaesthetic (Code: CHEBI:38867) General Anesthesia (Code: N0000175975) General Anesthetic (Code: N0000175681) Anesthetics (Code: D000777) Anesthetics, General (Code: D018681) Anesthetics, Inhalation (Code: D018685) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) 1972-08-28 FDA
Click to view apronal Apronal was used as a hypnotic drug. It has been withdrawn due to patient development of thrombocytopenic purpura.
Click to view undecylenic acid a fatty acid with a terminal double bond FDA
Click to view piroctone 2(1H)-pyridinone, 1-hydroxy-4-methyl-6-(2,4,4-trimethylpentyl)- combined with 2-aminoethanol; used to treat pityriasis; structure given in first source antiseborrheic (Code: CHEBI:59010)
Click to view guanazodine synonyms EGYT-739 & Sanegyt (Sanegit) refers to sulfate; RN given refers to parent cpd
Click to view isoflurane Potassium channel subfamily K member 17 (Organism: Homo sapiens, class: Ion channel, accessions: Q96T54, gene: KCNK17, swissprot: KCNKH_HUMAN) opener (Source: https://www.ncbi.nlm.nih.gov/pubmed/11263999) Transient receptor potential cation channel subfamily A member 1 (Organism: Rattus norvegicus, class: Ion channel, accessions: Q6RI86, gene: Trpa1, swissprot: TRPA1_RAT) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/18574153) Potassium channel subfamily K member 3 (Organism: Homo sapiens, class: Ion channel, accessions: O14649, gene: KCNK3, swissprot: KCNK3_HUMAN) opener (Source: https://www.ncbi.nlm.nih.gov/pubmed/10321245) Potassium channel subfamily K member 2 (Organism: Mus musculus, class: Ion channel, accessions: P97438, gene: Kcnk2, swissprot: KCNK2_MOUSE) opener (Source: https://www.ncbi.nlm.nih.gov/pubmed/10321245) GABA-A receptor; anion channel (Organism: Homo sapiens, class: Ion channel, accessions: O00591|O14764|P14867|P18505|P18507|P28472|P31644|P34903|P47869|P47870|P48169|P78334|Q16445|Q8N1C3|Q99928|Q9UN88, gene: GABRA1|GABRA2|GABRA3|GABRA4|GABRA5|GABRA6|GABRB1|GABRB2|GABRB3|GABRD|GABRE|GABRG1|GABRG2|GABRG3|GABRP|GABRQ, swissprot: GBRA1_HUMAN|GBRA2_HUMAN|GBRA3_HUMAN|GBRA4_HUMAN|GBRA5_HUMAN|GBRA6_HUMAN|GBRB1_HUMAN|GBRB2_HUMAN|GBRB3_HUMAN|GBRD_HUMAN|GBRE_HUMAN|GBRG1_HUMAN|GBRG2_HUMAN|GBRG3_HUMAN|GBRP_HUMAN|GBRT_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/23364597) Cytochrome P450 2E1 (Organism: Homo sapiens, class: Enzyme, accessions: P05181, gene: CYP2E1, swissprot: CP2E1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/8214760) Isoflurane is a fluorinated ether with general anesthetic and muscle relaxant activities. Although the exact mechanism of action has not been established, inhaled isoflurane, appears to act on the lipid matrix of the neuronal cell membrane, which results in disruption of neuronal transmission. Isoflurane is a stable, non-explosive inhalation anesthetic, relatively free from significant side effects. inhalation anaesthetic (Code: CHEBI:38870) Anesthetics (Code: D000777) Anesthetics, General (Code: D018681) Anesthetics, Inhalation (Code: D018685) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) General Anesthesia (Code: N0000175975) General Anesthetic (Code: N0000175681) 1979-12-18 FDA 4LE
ICF
Click to view ribavirin Inosine-5'-monophosphate dehydrogenase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P20839, gene: IMPDH1, swissprot: IMDH1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020903s055,021546s011lbl.pdf) Inosine-5'-monophosphate dehydrogenase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P12268, gene: IMPDH2, swissprot: IMDH2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020903s055,021546s011lbl.pdf) Adenosine kinase (Organism: Homo sapiens, class: Kinase, accessions: P55263, gene: ADK, swissprot: ADK_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/17379518) Solute carrier family 28 member 3 (Organism: Homo sapiens, class: Transporter, accessions: Q9HAS3, gene: SLC28A3, swissprot: S28A3_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/20096989) Equilibrative nucleoside transporter 1 (Organism: Homo sapiens, class: Transporter, accessions: Q99808, gene: SLC29A1, swissprot: S29A1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/20096989) Ribavirin is a synthetic nucleoside analog of ribofuranose with activity against hepatitis C virus and other RNA viruses. Ribavirin increases the mutation frequency in the genomes of several RNA viruses and ribavirin triphosphate inhibits HCV polymerase in a biochemical reaction. Ribavirin is indicated for the treatment of chronic hepatitis C (CHC) virus infection in patients 5 years of age and older with compensated liver disease not previously treated with interferon alpha, and in adult CHC patients coinfected with HIV. Nucleoside Analog (Code: N0000175459) Nucleoside Analog Antiviral (Code: N0000175466) antiinfective agent (Code: CHEBI:35441) Anti-Infective Agents (Code: D000890) Antimetabolites (Code: D000963) Antiviral Agents (Code: D000998) Noxae (Code: D009676) 1985-12-31 FDA RBV
Click to view secnidazole Secnidazole is a 5-nitroimidazole antimicrobial. 5-nitroimidazoles enter the bacterial cell as an inactive prodrug where the nitro group is reduced by bacterial enzymes to radical anions. It is believed that these radical anions interfere with bacterial DNA synthesis of susceptible isolates. Secnidazole is active in vitro against most isolates of the following organisms reported to be associated with bacterial vaginosis: Bacteroides spp., Gardnerella vaginalis, Prevotella spp., Mobiluncus spp., Megasphaera-like type I/II. Secnidazole is indicated for the treatment of bacterial vaginosis in adult women. Nitroimidazole Antimicrobial (Code: N0000175435) Nitroimidazoles (Code: N0000007663) Anti-Infective Agents (Code: D000890) Antiparasitic Agents (Code: D000977) Antiprotozoal Agents (Code: D000981) 2017-09-15 FDA
Click to view amanozine Amanozine is a triazine-based diuretic agent. Amanozine is structurally similar to the diuretic agent chlorazanil. 7ZF
Click to view procymate Procymate is an anxiolytic.
Click to view amphenidone Amphenidone is a CNS depressant. Amphenidone was used as a mild tranquilizer. It was withdrawn in 1961 due to patient development of agranulocytosis.
Click to view selenomethionine Selenomethionine is the racemic mixture of the D and L enantiomers of Selenomethionine, that used as animal’s dietary supplement. L-isomer of selenomethionine is a major natural food-form of selenium. Selenomethionine is either metabolized directly to reactive forms of selenium or stored in place of methionine in body proteins. Se-met metabolism is closely linked to protein turnover. Selenium, which is nutritionally essential for humans, is a constituent of more than two dozen selenoproteins that play critical roles in reproduction, thyroid hormone metabolism, DNA synthesis, and protection from oxidative damage and infection. Selenomethionine is indicated in combinations with other vitamins for prophylactic or therapeutic nutritional supplementation in physiologically stressful conditions. 2007-10-01 FDA MSE
Click to view mafenide Carbonic anhydrase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P00915, gene: CA1, swissprot: CAH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22370338) Carbonic anhydrase 12 (Organism: Homo sapiens, class: Enzyme, accessions: O43570, gene: CA12, swissprot: CAH12_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22370338) Carbonic anhydrase 14 (Organism: Homo sapiens, class: Enzyme, accessions: Q9ULX7, gene: CA14, swissprot: CAH14_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22370338) Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22370338) Carbonic anhydrase 9 (Organism: Homo sapiens, class: Enzyme, accessions: Q16790, gene: CA9, swissprot: CAH9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22370338) Carbonic anhydrase (Organism: Methanosarcina thermophila, class: Enzyme, accessions: P40881, gene: None, swissprot: CAH_METTE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15546717) Carbonic anhydrase 15 (Organism: Mus musculus, class: Enzyme, accessions: Q99N23, gene: Ca15, swissprot: CAH15_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19193158) Carbonic anhydrase 9 (Organism: Homo sapiens, class: Enzyme, accessions: Q16790, gene: CA9, swissprot: CAH9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12643899) Carbonic anhydrase 4 (Organism: Bos taurus, class: Enzyme, accessions: Q95323, gene: CA4, swissprot: CAH4_BOVIN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12643899) Carbonic anhydrase 5A, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P35218, gene: CA5A, swissprot: CAH5A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16302824) Carbonic anhydrase 5B, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: Q9Y2D0, gene: CA5B, swissprot: CAH5B_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16302824) Carbonic anhydrase 6 (Organism: Homo sapiens, class: Enzyme, accessions: P23280, gene: CA6, swissprot: CAH6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17228881) Carbonic anhydrase (Organism: Candida albicans (strain SC5314 / ATCC MYA-2876), class: Enzyme, accessions: Q5AJ71, gene: NCE103, swissprot: CAN_CANAL) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19450983) Carbonic anhydrase 13 (Organism: Mus musculus, class: Enzyme, accessions: Q9D6N1, gene: Ca13, swissprot: CAH13_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15203157) Beta-carbonic anhydrase 1 (Organism: Mycobacterium tuberculosis (strain ATCC 25618 / H37Rv), class: Enzyme, accessions: P9WPJ7, gene: mtcA1, swissprot: MTCA1_MYCTU) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19338333) Carbonic anhydrase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P22748, gene: CA4, swissprot: CAH4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15686931) Carbonic anhydrase 7 (Organism: Homo sapiens, class: Enzyme, accessions: P43166, gene: CA7, swissprot: CAH7_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15686895) Carbonic anhydrase 2 (Organism: Mycobacterium tuberculosis (strain ATCC 25618 / H37Rv), class: Enzyme, accessions: P9WPJ9, gene: mtcA2, swissprot: MTCA2_MYCTU) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19846301) Mafenide is a synthetic antimicrobial agent designated chemically as "-amino-p-toluenesulfonamide monoacetate. The mechanism of action of mafenide is not known, but is different from that of the sulfonamides. Mafenide is not antagonized by pABA, serum, pus or tissue exudates, and there is no correlation between bacterial sensitivities to mafenide and to the sulfonamides. Mafenide acetate exerts broad bacteriostatic action against many gramnegative and gram-positive organisms, including Pseudomonas aeruginosa and certain strains of anaerobes. is indicated for use as an adjunctive topical antimicrobial agent to control bacterial infection when used under moist dressings over meshed autografts on excised burn wounds. Methylated Sulfonamide Antibacterial (Code: N0000175511) Methylated Sulfonamides (Code: N0000175512) Anti-Infective Agents (Code: D000890) Anti-Infective Agents, Local (Code: D000891) 1969-01-24 FDA 6LH
Click to view carbimazole Lactoperoxidase (Organism: Homo sapiens, class: Enzyme, accessions: P22079, gene: LPO, swissprot: PERL_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18954039) Carbimazole (thionamide) is is a sulfur-containing imidazole derivatives. Carbimazole acts as a pro-drug which undergoes rapid and virtually complete metabolism to the active metabolite, thiamazole. (See: thiamazole) prodrug (Code: CHEBI:50266) antithyroid drug (Code: CHEBI:50671) Antithyroid Agents (Code: D013956) Hormone Antagonists (Code: D006727) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) 1958-03-01 Spanish Agency of Medicines and Medical Products (AEMPS)
Click to view cyclobutyrol Cyclobutyrol is a synthetic choleretic agent. It induces a transient choleresis which is accompanied by a marked reduction in cholesterol and phospholipid biliary secretion and in the biliary output of plasma-membrane enzymes. bile therapy drug (Code: CHEBI:61026)
Click to view capuride Capuride is an N-acylurea. Capuride is a monoureide sedative. Capuride has a duration of hypnotic effect similar to that of the short-acting barbiturates. It has a role as a sedative.
Click to view aminitrozole Aminitrozole is an orally available antiprotozoal agent used in the treatment of vaginal trichomoniasis. 1971-05-27 Ministry of Health of the Russian Federation
Click to view amrinone cGMP-inhibited 3',5'-cyclic phosphodiesterase A (Organism: Homo sapiens, class: Enzyme, accessions: Q14432, gene: PDE3A, swissprot: PDE3A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10644042) cGMP-inhibited 3',5'-cyclic phosphodiesterase B (Organism: Homo sapiens, class: Enzyme, accessions: Q13370, gene: PDE3B, swissprot: PDE3B_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10644042) cGMP-specific 3',5'-cyclic phosphodiesterase (Organism: Bos taurus, class: Enzyme, accessions: Q28156, gene: PDE5A, swissprot: PDE5A_BOVIN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10644042) Amrinone is a synthetic bipyridine phosphodiesterase inhibitor with inotropic and vasodilator properties. Amrinone inhibits type III phosphodiesterase, which is abundant in cardiac and vascular tissues, thereby preventing the degradation of cyclic adenosine monophosphate (cAMP) and increasing intracellular concentrations of this secondary messenger. Elevated levels of cAMP increase the contractile force of the cardiac muscle and produce positive inotropic effects. Although the mechanism of action is not fully understood, amrinone causes smooth muscle relaxation, resulting in peripheral vasodilation (reduced afterload) and a decreased pulmonary vascular resistance (reduced preload). It is used in the treatment of congestive heart failure. Calcium Channel Blockers (Code: D002121) Cardiotonic Agents (Code: D002316) Cardiovascular Agents (Code: D002317) Enzyme Inhibitors (Code: D004791) Membrane Transport Modulators (Code: D049990) Phosphodiesterase 3 Inhibitors (Code: D058987) Phosphodiesterase Inhibitors (Code: D010726) Protective Agents (Code: D020011) Vasodilator Agents (Code: D014665) 1984-07-31 FDA
Click to view phendimetrazine Sodium-dependent dopamine transporter (Organism: Homo sapiens, class: Transporter, accessions: Q01959, gene: SLC6A3, swissprot: SC6A3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/27514281) Phendimetrazine is a phenylalkylamine sympathomimetic amine with pharmacological activity similar to the prototype drugs of this class used in obesity, the amphetamines. Actions include central nervous system stimulation and elevation of blood pressure. Phendimetrazine is indicated in the management of exogenous obesity as a short term adjunct (a few weeks) in a regimen of weight reduction based on caloric restriction. Appetite Suppression (Code: N0000175372) Increased Sympathetic Activity (Code: N0000175651) Sympathomimetic Amine Anorectic (Code: N0000175423) Central Nervous System Agents (Code: D002491) Central Nervous System Stimulants (Code: D000697) 1976-07-28 FDA
Click to view pivagabine Pivagabine is a hydrophobic 4-aminobutyric acid derivative with neuromodulatory activity. The effects of pivagabine are mediated by inhibition of release of corticotropin-releasing factor, a neurohormone involved in stress-generating mechanisms. Pivagabine was used as an antidepressant. It was discontinued from the market.
Click to view selegiline Amine oxidase [flavin-containing] A (Organism: Homo sapiens, class: Enzyme, accessions: P21397, gene: MAOA, swissprot: AOFA_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021336s014lbl.pdf) Amine oxidase [flavin-containing] B (Organism: Homo sapiens, class: Enzyme, accessions: P27338, gene: MAOB, swissprot: AOFB_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021336s014lbl.pdf) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021336s014lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021336s014lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021336s014lbl.pdf) Cytochrome P450 3A5 (Organism: Homo sapiens, class: Enzyme, accessions: P20815, gene: CYP3A5, swissprot: CP3A5_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021336s014lbl.pdf) Cytochrome P450 2A6 (Organism: Homo sapiens, class: Enzyme, accessions: P11509, gene: CYP2A6, swissprot: CP2A6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021336s014lbl.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11996015) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11996015) Cytochrome P450 2E1 (Organism: Homo sapiens, class: Enzyme, accessions: P05181, gene: CYP2E1, swissprot: CP2E1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11996015) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021336s014lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021336s014lbl.pdf) Cytochrome P450 3A5 (Organism: Homo sapiens, class: Enzyme, accessions: P20815, gene: CYP3A5, swissprot: CP3A5_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021336s014lbl.pdf) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021336s014lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021336s014lbl.pdf) Selegiline is a selective, irreversible inhibitor of Type B monoamine oxidase. Selegiline is used in the treatment of depression and as adjunctive therapy in combination with levodopa and carbidopa in the therapy of Parkinson disease. Monoamine Oxidase Inhibitor (Code: N0000175744) Monoamine Oxidase Type B Inhibitor (Code: N0000175762) Monoamine Oxidase-B Inhibitors (Code: N0000175761) Anti-Dyskinesia Agents (Code: D018726) Antiparkinson Agents (Code: D000978) Central Nervous System Agents (Code: D002491) Enzyme Inhibitors (Code: D004791) Monoamine Oxidase Inhibitors (Code: D008996) Neuroprotective Agents (Code: D018696) Protective Agents (Code: D020011) 1989-06-05 FDA
Click to view clavulanic acid Beta-lactamase TEM (Organism: Escherichia coli, class: Enzyme, accessions: P62593, gene: bla; blaT-3; blaT-4;, swissprot: BLAT_ECOLX) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/050590s069,050658s031lbl.pdf) Beta-lactamase (Organism: Escherichia coli, class: Enzyme, accessions: Q6GWS8, gene: blaTEM-125, swissprot: Q6GWS8_ECOLX) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/050590s069,050658s031lbl.pdf) Beta-lactamase (Organism: Enterobacter cloacae, class: Enzyme, accessions: P05364, gene: ampC, swissprot: AMPC_ENTCL) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/050590s069,050658s031lbl.pdf) Beta-lactamase (Organism: Klebsiella pneumoniae, class: Enzyme, accessions: A0ZX81, gene: blaSHV-72, swissprot: A0ZX81_KLEPN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/050590s069,050658s031lbl.pdf) Beta-lactamase (Organism: Pseudomonas aeruginosa (strain ATCC 15692 / PAO1 / 1C / PRS 101 / LMG 12228), class: Enzyme, accessions: P24735, gene: ampC, swissprot: AMPC_PSEAE) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/050590s069,050658s031lbl.pdf) Beta-lactamase (Organism: Staphylococcus aureus, class: Enzyme, accessions: P00807, gene: blaZ, swissprot: BLAC_STAAU) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/050785s015lbl.pdf) Clavulanic acid is a ?-lactam structurally related to the penicillins which is produced by the fermentation of Streptomyces clavuligerus. Clavulanic acid has the ability to inactivate a wide variety of ?-lactamases by blocking the active sites of these enzymes. Clavulanic acid is particularly active against the clinically important plasmid-mediated ?-lactamases frequently responsible for transferred drug resistance to penicillins and cephalosporins. Clavulanic acid is used in conjunction with amoxicillin for the treatment of bronchitis and urinary tract, skin, and soft tissue infections caused by beta-lactamase producing organisms. antibacterial drug (Code: CHEBI:36047) anxiolytic drug (Code: CHEBI:35474) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) beta-Lactamase Inhibitors (Code: D065093) Enzyme Inhibitors (Code: D004791) beta Lactamase Inhibitor (Code: N0000175930) beta Lactamase Inhibitors (Code: N0000000202) 1984-08-06 FDA J01
Click to view aceglutamide Aceglutamide is an acetyl derivative of the amino acid L-glutamine. Aceglutamide is a psychostimulant and nootropic used to improve memory and concentration. Also aceglutamide aluminium salt is used for the treatment and prevention of peptic ulcers. 2013 China Food and Drug Administration (CFDA) NLQ
Click to view fluoresone Fluoresone was used as an adjunct treatment of epilepsy.
Click to view phenazone Transient receptor potential cation channel subfamily A member 1 (Organism: Homo sapiens, class: Ion channel, accessions: O75762, gene: TRPA1, swissprot: TRPA1_HUMAN) antagonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/25765567) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/8681486) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/8681486) Cytochrome P450 2C18 (Organism: Homo sapiens, class: Enzyme, accessions: P33260, gene: CYP2C18, swissprot: CP2CI_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/8681486) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/8681486) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/8681486) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/8681486) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/8801065) Cytochrome P450 2E1 (Organism: Homo sapiens, class: Enzyme, accessions: P05181, gene: CYP2E1, swissprot: CP2E1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/8801065) Phenazone is an analgesic and antipyretic that has been given by mouth and as ear drops. It inhibits cyclooxygenases and shows little anti-inflammatory activity. Phenazone is often used in testing the effects of other drugs or diseases on drug-metabolizing enzymes in the liver. (From Martindale, The Extra Pharmacopoeia, 30th ed, p29) opioid analgesic (Code: CHEBI:35482) non-narcotic analgesic (Code: CHEBI:35481) antipyretic (Code: CHEBI:35493) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1964-01-01 YEAR INTRODUCED
Click to view promoxolane Promoxolane is a cyclic derivative of glycerol. Promoxolane produces skeletal-muscle-relaxing effects due to its depressant action on spinal inter-neural connections which relives tension and spasm without central depression. Promoxolane was used for the treatment of neuroses as a minor tranquilizer to produce sedation. Also promoxolane was used for dysmenorrhea and the menopausal syndrome.
Click to view droxidopa Catechol O-methyltransferase (Organism: Homo sapiens, class: Enzyme, accessions: P21964, gene: COMT, swissprot: COMT_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/203202s007lbl.pdf) Aromatic-L-amino-acid decarboxylase (Organism: Homo sapiens, class: Enzyme, accessions: P20711, gene: DDC, swissprot: DDC_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/203202s007lbl.pdf) Nuclear receptor subfamily 1 group I member 2 (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: O75469, gene: NR1I2, swissprot: NR1I2_HUMAN) agonist (Source: https://pubmed.ncbi.nlm.nih.gov/20966043/) Droxidopa is a synthetic amino acid precursor of norepinephrine. The exact mechanism of action of droxidopa in the treatment of neurogenic orthostatic hypotension is unknown. Droxidopa is a synthetic amino acid analog that is directly metabolized to norepinephrine by dopa-decarboxylase, which is extensively distributed throughout the body. Droxidopa is believed to exert its pharmacological effects through norepinephrine and not through the parent molecule or other metabolites. Norepinephrine increases blood pressure by inducing peripheral arterial and venous vasoconstriction. Droxidopa is indicated for the treatment of orthostatic dizziness, lightheadedness, or the “feeling that you are about to black out” in adult patients with symptomatic neurogenic orthostatic hypotension caused by primary autonomic failure (Parkinson's disease, multiple system atrophy, and pure autonomic failure), dopamine beta-hydroxylase deficiency, and non-diabetic autonomic neuropathy. prodrug (Code: CHEBI:50266) vasoconstrictor agent (Code: CHEBI:50514) antihypertensive agent (Code: CHEBI:35674) Catecholamines (Code: N0000007715) Increased Blood Pressure (Code: N0000178478) Anti-Dyskinesia Agents (Code: D018726) Antiparkinson Agents (Code: D000978) Central Nervous System Agents (Code: D002491) 2014-02-18 FDA
Click to view fenproporex an anorectic drug used in the treatment of obesity 1975 YEAR INTRODUCED
Click to view etryptamine Ethyltryptamine is a non hydrazine reversible monoamine oxidase inhibitor. It is used as an antidepressant. However, in 1962, after the discovery of an unacceptable incidence of agranulocytosis, the development of ethyltryptamine was halted and the drug was withdrawn from potential market use. Currently, ethyltryptamine is an illegal substance. 1961 YEAR INTRODUCED
Click to view unithiol Unithiol is a chelating agent used as an antidote to heavy metal poisoning. Its active sulfhydryl groups enter into reactions with thiol poisons present in blood and tissues, form not toxic complex with them eliminated with urine. The poisons fixation results in the body enzyme systems changed under the poisons effect functions restoration. It is efficient as an antidote in case of intoxications by arsenic and heavy metals salts. Antidotes (Code: D000931) Chelating Agents (Code: D002614) Protective Agents (Code: D020011) Sequestering Agents (Code: D064449) 1964-04-30 Ministry of Health of the Russian Federation
Click to view phensuximide Phensuximide is an anticonvulsant in the succinimide class. It suppresses the paroxysmal three cycle per second spike and wave EEG pattern associated with lapses of consciousness in petit mal seizures. The frequency of attacks is reduced by depression of nerve transmission in the motor cortex. IT is used for the treatment of epilepsy. 1953-09-08 FDA
Click to view azacitidine Azacitidine is a pyrimidine nucleoside analog of cytidine. Azacitidine is believed to exert its antineoplastic effects by causing hypomethylation of DNA and direct cytotoxicity on abnormal hematopoietic cells in the bone marrow. The concentration of azacitidine required for maximum inhibition of DNA methylation in vitro does not cause major suppression of DNA synthesis. The cytotoxic effects of azacitidine cause the death of rapidly dividing cells, including cancer cells that are no longer responsive to normal growth control mechanisms. Non-proliferating cells are relatively insensitive to azacitidine. Azacitidine is indicated for the treatment of patients with the following FAB myelodysplastic syndrome subtypes: Refractory anemia or refractory anemia with ringed sideroblasts (if accompanied by neutropenia or thrombocytopenia or requiring transfusions), refractory anemia with excess blasts, refractory anemia with excess blasts in transformation, and chronic myelomonocytic leukemia. Nucleic Acid Synthesis Inhibitors (Code: N0000000233) Nucleoside Metabolic Inhibitor (Code: N0000175595) Antimetabolites (Code: D000963) Antimetabolites, Antineoplastic (Code: D000964) Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Noxae (Code: D009676) 2004-05-19 FDA 5AE
Click to view thiotepa Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208264s000lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208264s000lbl.pdf) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208264s000lbl.pdf) Thiotepa is a cytotoxic agent of the polyfunctional type, related chemically and pharmacologically to the nitrogen mustard. The radiomimetic action of thiotepa is believed to occur through the release of ethyleneimine radicals which, like irradiation, disrupt the bonds of DNA. One of the principle bond disruptions is initiated by alkylation of guanine at the N-7 position, which severs the linkage between the purine base and the sugar and liberates alkylated guanines. Thiotepa is a very toxic alkylating antineoplastic agent also used as an insect sterilant. Thiotepa causes skin, gastrointestinal, CNS, and bone marrow damage. Thiotepa may reasonably be anticipated to be a carcinogen. Alkylating Activity (Code: N0000000236) Alkylating Drug (Code: N0000175558) Alkylating Agents (Code: D000477) Antineoplastic Agents (Code: D000970) Antineoplastic Agents, Alkylating (Code: D018906) Immunologic Factors (Code: D007155) Immunosuppressive Agents (Code: D007166) Myeloablative Agonists (Code: D019653) Noxae (Code: D009676) 1959-03-09 FDA
Click to view chromocarb treatment for certain forms of hemorrhagic anal inflammations
Click to view pentamethonium bromide Pentamethonium bromide is an anglioplegic agent which produces arterial vasodilation. It was used for the treatment of hypertension and circulation diseases. It is no longer available.
Click to view carglumic acid Carbamoyl-phosphate synthase [ammonia], mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P31327, gene: CPS1, swissprot: CPSM_HUMAN) activator (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022562s005lbl.pdf) Carglumic acid ( N-carbamoyl-L-glutamic acid or (2S)-2-(carbamoylamino) pentanedioic acid) is a carbamoyl phosphate synthetase 1 (CPS 1) activator. Carglumic acid is a synthetic structural analogue of N-acetylglutamate (NAG) which is produced from glutamate and acetyl-CoA in a reaction catalyzed by N-acetylglutamate synthase (NAGS), a mitochondrial liver enzyme. NAG acts as an essential allosteric activator of Carbamoyl Phosphate Synthetase 1 (CPS 1), a mitochondrial liver enzyme which catalyzes the first reaction of the urea cycle. The urea cycle, whose role is the disposition of ammonia, includes a series of biochemical reactions in the liver resulting in the conversion of ammonia into urea, which is then excreted through the urine. Carglumic acid acts as a CPS1 activator in patients with NAGS deficiency, thereby removing the block in the urea cycle and facilitating ammonia detoxification and urea production. Carglumic acid is indicated as adjunctive therapy for the treatment of acute hyperammonemia or as maintenance therapy for the treatment of chronic hyperammonemia due to the deficiency of the hepatic enzyme N-acetylglutamate synthase. orphan drug (Code: CHEBI:71031) Carbamoyl Phosphate Synthetase 1 Activator (Code: N0000184144) Carbamoyl Phosphate Synthetase 1 Activators (Code: N0000184143) 2010-03-18 FDA
Click to view dioxybenzone Dioxybenzone is a derivative of benzophenone used in sunscreen to block UVB and short-wave UVA rays. FDA
Click to view nitroxoline Methionine aminopeptidase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P50579, gene: METAP2, swissprot: MAP2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21088277) Cathepsin B (Organism: Homo sapiens, class: Enzyme, accessions: P07858, gene: CTSB, swissprot: CATB_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21598397) Prostaglandin G/H synthase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P35354, gene: PTGS2, swissprot: PGH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/24088053) Catechol O-methyltransferase (Organism: Rattus norvegicus, class: Enzyme, accessions: P22734, gene: Comt, swissprot: COMT_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/817025) Nitroxoline is a urinary antibacterial agent active against susceptible gram-positive and gram-negative organisms commonly found in urinary tract infections. Its antibacterial activity may stem from the metal ion complexation vital for bacterial growth. This drug may also have antitumor activity by inhibition of type 2 methionine aminopeptidase (MetAP2) protein which is involved in angiogenesis. Anti-Infective Agents (Code: D000890) Anti-Infective Agents, Urinary (Code: D000892) Antifungal Agents (Code: D000935) Renal Agents (Code: D012076) 2006-06-09 Ministry of Health of the Russian Federation HNQ
Click to view procodazole Procodazole (1H-benzimidazole-2-propanoic acid) is an immunomodulator. Procodazole enhances the phagocytic activity in the liver and the spleen. 4BX
Click to view dihydralazine Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10525281) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10525281) Dihydralazine belongs to thehydrazinophthalazine chemical class and has very similar effects to hydralazine. Dihydralazine is the most frequently used antihypertensive drug in the treatment of severe hypertension in pregnancy. Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) 1979-02-13 Hungary National Institute of Pharmacy and Nutrition
Click to view isosorbide mononitrate Isosorbide mononitrate is a vasodilator with effects on both arteries and veins. The principal pharmacological action of isosorbide mononitrate is relaxation of vascular smooth muscle and consequent dilatation of peripheral arteries and veins, especially the latter. Similar to other nitrites and organic nitrates, Isosorbide Mononitrate is converted to nitric oxide (NO), an active intermediate compound that activates the enzyme guanylate cyclase. Isosorbide mononitrate is rapidly and completely absorbed from the gastrointestinal tract. In humans, is not subject to first pass metabolism in the liver. Isosorbide mononitrate is indicated for the prevention and treatment of angina pectoris due to coronary artery disease. vasodilator agent (Code: CHEBI:35620) Nitrate Vasodilator (Code: N0000175415) Nitrates (Code: N0000007647) Vasodilation (Code: N0000009909) Cardiovascular Agents (Code: D002317) Nitric Oxide Donors (Code: D020030) Vasodilator Agents (Code: D014665) 1991-12-30 FDA
Click to view idrocilamide Idrocilamide is a skeletal muscle relaxant and anti-inflammatory agent. Idrocilamide is used as a topical cream to treat lumbago and other kinds of muscular pain. 1998-05-11 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view amiphenazole used as a respiratory tonic, morphine antagonist, & antidote in barbiturate poisoning; RN given refers to parent cpd; sturcture Respiratory System Agents (Code: D019141)
Click to view oxidronic acid Oxidronic acid is a calcium regulator. In complex with Technetium Tc 99m is used as diagnostic skeletal imaging agent used to demonstrate areas of altered osteogenesis in adult and pediatric patients. 1982-01-01 FDA
Click to view citric acid pH (H+ ion activity) (Organism: None, class: Unclassified, accessions: None, gene: None, swissprot: None) other (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/019481s013lbl.pdf) Solute carrier organic anion transporter family member 2B1 (Organism: Homo sapiens, class: Transporter, accessions: O94956, gene: SLCO2B1, swissprot: SO2B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12724351) Citric acid is a key intermediate in metabolism. It is an acid compound found in citrus fruits. Citric acid is a natural preservative and is also used to add an acidic (sour) taste to foods and soft drinks. The salts of citric acid (citrates) can be used as anticoagulants due to their calcium chelating ability. It is also used as an acidulant to control pH. food acidity regulator (Code: CHEBI:64049) Acidifying Activity (Code: N0000175833) Calculi Dissolution Agent (Code: N0000175835) Anti-coagulant (Code: N0000175980) Decreased Coagulation Factor Activity (Code: N0000008556) Calcium Chelating Activity (Code: N0000175089) Anticoagulants (Code: D000925) Calcium Chelating Agents (Code: D065096) Chelating Agents (Code: D002614) Hematologic Agents (Code: D006401) Sequestering Agents (Code: D064449) 1982-06-22 FDA CIT
FLC
Click to view clonitrate Clonitrate (chloroglyceryl dinitrate) is an oily liquid. It has coronary-dilator effect on isolated heart and therapeutic effect on the angina pectoris patient. Chloroglyceryl dinitrate is a more potent coronary dilator than nitroglycerin. It is no longer availible.
Click to view ibufenac Amine oxidase [flavin-containing] B (Organism: Mus musculus, class: Enzyme, accessions: Q8BW75, gene: Maob, swissprot: AOFB_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22984634) Ibufenac is a nonsteroidal anti-inflammatory drug. Ibufenac has anti-inflammatory, antipyretic and analgesic properties. It was used for the treatment of rheumatoid arthritis. It was withdrawn from the market due to hepatotoxicity. non-steroidal anti-inflammatory drug (Code: CHEBI:35475) non-narcotic analgesic (Code: CHEBI:35481)
Click to view tocainide Tocainide is an antiarrhythmic agent which exerts a potential- and frequency-dependent block of sodium channels. Tocainide acts on sodium channels on the neuronal cell membrane, limiting the spread of seizure activity and reducing seizure propagation. Tocainide binds preferentially to the inactive state of the sodium channels. The antiarrhythmic actions are mediated through effects on sodium channels in Purkinje fibers. It is used in the treatment of ventricular arrhythmias. anti-arrhythmia drug (Code: CHEBI:38070) local anaesthetic (Code: CHEBI:36333) Anti-Arrhythmia Agents (Code: D000889) Cardiovascular Agents (Code: D002317) Membrane Transport Modulators (Code: D049990) Sodium Channel Blockers (Code: D026941) Voltage-Gated Sodium Channel Blockers (Code: D061567) 1984-11-09 FDA
Click to view bitoscanate Bitoscanate is a tasteless, odorless, colorless, needle-like crystalline solid material prepared from mustard powder acid. Bitoscanate was used as an anthelmintic against nematodes, especially hookworms (Necator sp.) and Ancylostoma duodenale. Bitoscanate is an extremely hazardous substance. 1970-04-01 CDSCO (INDIA)
Click to view glucuronamide Glucuronamide is a hexose related to glucuronic acid. Glucuronamide in combination with caffeine and ascorbic acid has antiasthenic properties and is used against fatigue. 1996-08-28 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view carbaryl Acetylcholinesterase (Organism: Homo sapiens, class: Enzyme, accessions: P22303, gene: ACHE, swissprot: ACES_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23632007) Carbaryl is a carbamate insecticide and parasiticide. It is a potent anticholinesterase agent belonging to the carbamate group of reversible cholinesterase inhibitors. It has a particularly low toxicity from dermal absorption and is used for control of head lice in some countries. carbamate insecticide (Code: CHEBI:38461) acaricide (Code: CHEBI:22153) agrochemical (Code: CHEBI:33286) Cholinergic Agents (Code: D018678) Cholinesterase Inhibitors (Code: D002800) Enzyme Inhibitors (Code: D004791) Insecticides (Code: D007306) Neurotransmitter Agents (Code: D018377) Pesticides (Code: D010575)
Click to view betamipron Solute carrier family 22 member 8 (Organism: Homo sapiens, class: Transporter, accessions: Q8TCC7, gene: SLC22A8, swissprot: S22A8_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11426832) Solute carrier family 22 member 6 (Organism: Homo sapiens, class: Transporter, accessions: Q4U2R8, gene: SLC22A6, swissprot: S22A6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11426832) Betamipron is an amino acid derivative. Betamipron reduces the nephrotoxicity by carbapenem antibiotics by inhibiting the intracellular accumulation in renal tubules. It is used in combination with panipenem for inhibition renal uptake of panipenem and also from panipenem's nephrotoxicity. 1993 PMDA BYA
Click to view actarit immunomodulator 2008-07-22 CDSCO (INDIA)
Click to view butamben Butamben is the ester of 4-aminobenzoic acid and butanol. It is used as a local anesthetic. It is one of three components in the topical anesthetic Cetacaine local anaesthetic (Code: CHEBI:36333) Anesthetics (Code: D000777) Anesthetics, Local (Code: D000779) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) FDA
Click to view fenozolone Fenozolone is a psychostimulant drug. It exhibits an amphetamine-like effect and increases transmission of all monoamines. It was used as a psychostimulant and antidepressant. Autonomic Agents (Code: D001337) Peripheral Nervous System Agents (Code: D018373) Sympathomimetics (Code: D013566)
Click to view tryptophan Extracellular calcium-sensing receptor (Organism: Homo sapiens, class: GPCR, accessions: P41180, gene: CASR, swissprot: CASR_HUMAN) allosteric modulator (Source: ) Probable G-protein coupled receptor 139 (Organism: Homo sapiens, class: Unclassified, accessions: Q6DWJ6, gene: GPR139, swissprot: GP139_HUMAN) agonist (Source: ) An essential amino acid that is necessary for normal growth in infants and for NITROGEN balance in adults. It is a precursor of INDOLE ALKALOIDS in plants. It is a precursor of SEROTONIN (hence its use as an antidepressant and sleep aid). It can be a precursor to NIACIN, albeit inefficiently, in mammals. Antidepressive Agents (Code: D000928) Antidepressive Agents, Second-Generation (Code: D018687) Central Nervous System Agents (Code: D002491) Psychotropic Drugs (Code: D011619) 1975 FDA TRP
DTR
Click to view sabcomeline Muscarinic acetylcholine receptor M5 (Organism: Homo sapiens, class: GPCR, accessions: P08912, gene: CHRM5, swissprot: ACM5_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10323594) Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10323594) Muscarinic acetylcholine receptor M4 (Organism: Homo sapiens, class: GPCR, accessions: P08173, gene: CHRM4, swissprot: ACM4_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10323594) Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10323594) Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10323594) Sabcomeline is a selective M1 partial agonist. Sabcomeline improves cognitive performance. It was under development for the treatment of Alzheimer's disease, but later it was discontinued due to poor results.
Click to view etafedrine Etafedrine is a sympathomimetic agent. It acts on the sympathetic receptors of the bronchial tree relaxing spasm. Etafedrine is used in combination with hydrocodone, doxylamine, sodium citrate and alcohol for the treatment of cough associated with inflamed mucosa, which does not respond to products of lesser potency. 1983-12-31 Health Canada
Click to view temozolomide Temozolomide is not directly active but undergoes rapid nonenzymatic conversion at physiologic pH to the reactive compound 5-(3-methyltriazen1-yl)-imidazole-4-carboxamide (MTIC). The cytotoxicity of MTIC is thought to be primarily due to alkylation of DNA. It is indicated for the treatment of glioblastoma multiforme, refractory anaplastic astrocytoma. antineoplastic agent (Code: CHEBI:35610) prodrug (Code: CHEBI:50266) Alkylating Agents (Code: D000477) Antineoplastic Agents (Code: D000970) Antineoplastic Agents, Alkylating (Code: D018906) Noxae (Code: D009676) Alkylating Activity (Code: N0000000236) Alkylating Drug (Code: N0000175558) 1999-08-11 FDA
Click to view ibuprofen tidrug resistance-associated protein 4 (Organism: Homo sapiens, class: Transporter, accessions: O15439, gene: ABCC4, swissprot: MRP4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12835412) Multidrug resistance-associated protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P33527, gene: ABCC1, swissprot: MRP1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12835412) Solute carrier family 22 member 6 (Organism: Homo sapiens, class: Transporter, accessions: Q4U2R8, gene: SLC22A6, swissprot: S22A6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12130730) Solute carrier family 22 member 11 (Organism: Homo sapiens, class: Transporter, accessions: Q9NSA0, gene: SLC22A11, swissprot: S22AB_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12130730) Solute carrier family 22 member 8 (Organism: Homo sapiens, class: Transporter, accessions: Q8TCC7, gene: SLC22A8, swissprot: S22A8_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12130730) Acid-sensing ion channel 1 (Organism: Homo sapiens, class: Ion channel, accessions: P78348, gene: ASIC1, swissprot: ASIC1_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/28949138) Sodium-coupled monocarboxylate transporter 1 (Organism: Homo sapiens, class: Transporter, accessions: Q8N695, gene: SLC5A8, swissprot: SC5A8_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16729224) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/9296349) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/9296349) Multidrug resistance-associated protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P33527, gene: ABCC1, swissprot: MRP1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12954186) Ibuprofen is a nonsteroidal anti-inflammatory agent with analgesic and antipyretic properties. It’s used temporarily relieves minor aches and pains due to: headache; the common cold; muscular aches; backache; toothache; minor pain of arthritis; menstrual cramps and temporarily reduces fever. The exact mechanism of action of ibuprofen is unknown. Ibuprofen is administered as a racemic mixture. The R-enantiomer undergoes extensive interconversion to the S-enantiomer in vivo. The S-enantiomer (dexibuprofen) is believed to be the more pharmacologically active enantiomer. Nonsteroidal Anti-inflammatory Compounds (Code: N0000175721) Nonsteroidal Anti-inflammatory Drug (Code: N0000175722) Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Central Nervous System Agents (Code: D002491) Cyclooxygenase Inhibitors (Code: D016861) Enzyme Inhibitors (Code: D004791) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1974-08-27 FDA IBP
IZP
Click to view aminohippuric acid Solute carrier family 22 member 6 (Organism: Homo sapiens, class: Transporter, accessions: Q4U2R8, gene: SLC22A6, swissprot: S22A6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/9950961) Solute carrier family 22 member 6 (Organism: Homo sapiens, class: Transporter, accessions: Q4U2R8, gene: SLC22A6, swissprot: S22A6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11669456) Solute carrier family 22 member 8 (Organism: Homo sapiens, class: Transporter, accessions: Q8TCC7, gene: SLC22A8, swissprot: S22A8_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11669456) Canalicular multispecific organic anion transporter 1 (Organism: Homo sapiens, class: Transporter, accessions: Q92887, gene: ABCC2, swissprot: MRP2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10760098) Solute carrier organic anion transporter family member 3A1 (Organism: Homo sapiens, class: Transporter, accessions: Q9UIG8, gene: SLCO3A1, swissprot: SO3A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/14631946) Monocarboxylate transporter 1 (Organism: Rattus norvegicus, class: Transporter, accessions: P53987, gene: Slc16a1, swissprot: MOT1_RAT) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10579682) Aminohippuric acid is a glycine amide of 4-aminobenzoic acid. Renal proximal tubules secrete various organic anions, including drugs and p-aminohippurate (PAH). Uptake of PAH from blood into tubule cells occurs by exchange with intracellular alpha-ketoglutarate and is mediated by the organic anion transporter 1. PAH exit into tubule lumen is species specific and may involve ATP-independent and -dependent transporters. Enhanced secretion of p-aminohippuric acid occurs in Fanconi's syndrome. It is used as a diagnostic aid to measure effective renal plasma flow and excretory capacity. Indicators and Reagents (Code: D007202) 1944-12-30 FDA
Click to view enprofylline Adenosine receptor A1 (Organism: Rattus norvegicus, class: GPCR, accessions: P25099, gene: Adora1, swissprot: AA1R_RAT) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/3002801) Adenosine A2 receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P29276|P30543, gene: Adora2a|Adora2b, swissprot: AA2AR_RAT|AA2BR_RAT) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/3002801) Adenosine receptor A2b (Organism: Homo sapiens, class: GPCR, accessions: P29275, gene: ADORA2B, swissprot: AA2BR_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10496952) Adenosine receptor A3 (Organism: Homo sapiens, class: GPCR, accessions: P0DMS8, gene: ADORA3, swissprot: AA3R_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10496952) Adenosine receptor A2a (Organism: Homo sapiens, class: GPCR, accessions: P29274, gene: ADORA2A, swissprot: AA2AR_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10496952) Adenosine receptor A1 (Organism: Homo sapiens, class: GPCR, accessions: P30542, gene: ADORA1, swissprot: AA1R_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10496952) Enprofylline is a derivative of theophylline which shares bronchodilator properties. iI was used for the symptomatic treatment of asthma and chronic obstructive pulmonary disease, and in the management of cerebrovascular insufficiency, sickle cell disease, and diabetic neuropathy. bronchodilator agent (Code: CHEBI:35523) anti-asthmatic drug (Code: CHEBI:49167) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) anti-arrhythmia drug (Code: CHEBI:38070) Adenosine A2 Receptor Antagonists (Code: D058917) Anti-Asthmatic Agents (Code: D018927) Autonomic Agents (Code: D001337) Bronchodilator Agents (Code: D001993) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Purinergic Agents (Code: D058905) Purinergic Antagonists (Code: D058914) Purinergic P1 Receptor Antagonists (Code: D058915) Respiratory System Agents (Code: D019141)
Click to view caffeine Adenosine receptor A3 (Organism: Homo sapiens, class: GPCR, accessions: P0DMS8, gene: ADORA3, swissprot: AA3R_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10049999) Adenosine receptor A2b (Organism: Homo sapiens, class: GPCR, accessions: P29275, gene: ADORA2B, swissprot: AA2BR_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10049999) Adenosine receptor A1 (Organism: Homo sapiens, class: GPCR, accessions: P30542, gene: ADORA1, swissprot: AA1R_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10049999) Adenosine receptor A2a (Organism: Homo sapiens, class: GPCR, accessions: P29274, gene: ADORA2A, swissprot: AA2AR_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10049999) cGMP-specific 3',5'-cyclic phosphodiesterase (Organism: Homo sapiens, class: Enzyme, accessions: O76074, gene: PDE5A, swissprot: PDE5A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20164566) Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform (Organism: Homo sapiens, class: Kinase, accessions: O00329, gene: PIK3CD, swissprot: PK3CD_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12145276) Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (Organism: Homo sapiens, class: Kinase, accessions: P42336, gene: PIK3CA, swissprot: PK3CA_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12145276) Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform (Organism: Homo sapiens, class: Kinase, accessions: P42338, gene: PIK3CB, swissprot: PK3CB_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12145276) Serine-protein kinase ATM (Organism: Homo sapiens, class: Kinase, accessions: Q13315, gene: ATM, swissprot: ATM_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10531013) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/14616429) Guanine deaminase (Organism: Homo sapiens, class: Enzyme, accessions: Q9Y2T3, gene: GDA, swissprot: GUAD_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20716488) Caffeine is a methylxanthine alkaloid found in the seeds, nuts, or leaves of a number of plants native to South America and East Asia that is structurally related to adenosine and acts primarily as an adenosine receptor antagonist with psychotropic and anti-inflammatory activities. The anti-inflammatory effects of caffeine are due the nonselective competitive inhibition of phosphodiesterases. Caffeine is used by mouth or rectally in combination with painkillers (such as aspirin and acetaminophen) and a chemical called ergotamine for treating migraineheadaches. It is also used with painkillers for simple headaches and preventing and treating headaches after epidural anesthesia. Caffeine creams are applied to the skin to reduce redness and itching in dermatitis. Healthcare providers sometimes give caffeine intravenously (by IV) for headache after epidural anesthesia, breathing problems in newborns, and to increase urine flow. In foods, caffeine is used as an ingredient in soft drinks, energy drinks, and other beverages. psychotropic drug (Code: CHEBI:35471) diuretic (Code: CHEBI:35498) food additive (Code: CHEBI:64047) adjuvant (Code: CHEBI:60809) central nervous system stimulant (Code: CHEBI:35337) Central Nervous System Stimulation (Code: N0000175729) Methylxanthine (Code: N0000175790) Xanthines (Code: N0000008118) Central Nervous System Agents (Code: D002491) Central Nervous System Stimulants (Code: D000697) Enzyme Inhibitors (Code: D004791) Neurotransmitter Agents (Code: D018377) Phosphodiesterase Inhibitors (Code: D010726) Purinergic Agents (Code: D058905) Purinergic Antagonists (Code: D058914) Purinergic P1 Receptor Antagonists (Code: D058915) 1948-11-26 FDA CFF
Click to view phenamine Phenocoll is an antineuralgic, analgesic and antipyretic drug. It is a derivative of phenacetin and thus has the same mechanism of action (COX-2 inhibition). It used to control inflammation in such diseases as gout, influenza, malaria, rheumatism and pleuritis.
Click to view ethotoin Ethotoin is a hydantoin derivative and anticonvulsant. Ethotoin exerts an antiepileptic effect without causing general central nervous system depression. The mechanism of action is probably very similar to that of phenytoin. The latter drug appears to stabilize rather than to raise the normal seizure threshold, and to prevent the spread of seizure activity rather than to abolish the primary focus of seizure discharges. It is indicated for the control of tonic-clonic (grand mal) and complex partial (psychomotor) seizures. anticonvulsant (Code: CHEBI:35623) Anti-epileptic Agent (Code: N0000175753) Decreased Central Nervous System Disorganized Electrical Activity (Code: N0000008486) Anticonvulsants (Code: D000927) Central Nervous System Agents (Code: D002491) 1957-04-22 FDA
Click to view aminoacridine Trypanothione reductase (Organism: Trypanosoma cruzi, class: Enzyme, accessions: P28593, gene: TPR, swissprot: TYTR_TRYCR) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10639286) Aminoacridine is a highly fluorescent anti-infective dye used experimentally as a mutagen, due to its interaction with DNA. It is also used as an intracellular pH indicator. It is used in combination with lidocaine for the quick, effective relief from the pain of common mouth ulcers and denture rubbing. Anti-Infective Agents (Code: D000890) Anti-Infective Agents, Local (Code: D000891) Coloring Agents (Code: D004396) Fluorescent Dyes (Code: D005456) Indicators and Reagents (Code: D007202) Luminescent Agents (Code: D049408) Mutagens (Code: D009153) Noxae (Code: D009676) 1988-09-08 New Zealand Medicines and Medical Devices Safety Authority AA
Click to view hexylresorcinol Polyphenol oxidase 2 (Organism: Agaricus bisporus, class: Enzyme, accessions: O42713, gene: PPO2, swissprot: PPO2_AGABI) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19054671) Arachidonate 5-lipoxygenase (Organism: Homo sapiens, class: Enzyme, accessions: P09917, gene: ALOX5, swissprot: LOX5_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23871907) Hexylresorcinol is a local anaesthetic for topical use on the mucous membranes of the mouth and throat. Mild antiseptic activity has also been demonstrated. Hexylresorcinol is used as an antiseptic and local anaesthetic for the relief of sore throat and its associated pain. Anthelmintics (Code: D000871) Anti-Infective Agents (Code: D000890) Antiparasitic Agents (Code: D000977) FDA
Click to view salamidacetic acid salamidacetic acid (salicylamide O-acetic acid) is a nonsteroidal anti-inflammatory drug.
Click to view buramate Buramate is a member of benzenes. Buramate was used for the treatment of epilepsy, espesially in Petit Mal.
Click to view phenallymal Phenallymal (alphenal) is a barbiturate derivative. It has primarily anticonvulsant properties, and was used occasionally for the treatment of epilepsy or convulsions.
Click to view metirosine Metirosine is an antihypertensive drug. Metyrosine inhibits tyrosine hydroxylase, which catalyzes the first transformation in catecholamine biosynthesis, i.e., the conversion of tyrosine to dihydroxyphenylalanine (DOPA). Metirosine is used for the treatment of patients with pheochromocytoma, for preoperative preparation of patients for surgery, management of patients when surgery is contraindicated, and chronic treatment of patients with malignant pheochromocytoma. antihypertensive agent (Code: CHEBI:35674) Catecholamine Synthesis Inhibitor (Code: N0000175569) Catecholamine Synthesis Inhibitors (Code: N0000175361) 1979-10-03 FDA
Click to view amisometradine Amisometradine is a pyrimidinedione-based diuretic and isomer of aminometradine with less toxicity. Amisometradine produces diuresis by a mechanism similar to that of the xanthines. Amisometradine causes inhibition of reabsorption of sodium by the proximal tubules. Amisometradine was used to for treatment of mild edema in patients with congestive heart failure. Amisometradine was voluntarly withdrawn from market. 1956 YEAR INTRODUCED
Click to view aminometradine Aminometradine is a pyrimidinedione-based diuretic. Aminometradine appears to inhibit the reabsorption of sodium ions by the renal tubules and is a relatively weak diuretic. It was used to for treatment of congestive heart failure. It was withdrawn from the market due to its unsatisfactory results and replaced by amisometradine. 1954 YEAR INTRODUCED
Click to view pimeclone Pimeclone is a respiratory stimulant. It is no longer available.
Click to view flurbiprofen Prostaglandin G/H synthase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P23219, gene: PTGS1, swissprot: PGH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10377455) Prostaglandin G/H synthase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P35354, gene: PTGS2, swissprot: PGH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10091674) Aldo-keto reductase family 1 member C3 (Organism: Homo sapiens, class: Enzyme, accessions: P42330, gene: AKR1C3, swissprot: AK1C3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22877157) Aldo-keto reductase family 1 member C2 (Organism: Homo sapiens, class: Enzyme, accessions: P52895, gene: AKR1C2, swissprot: AK1C2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22877157) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/018766s020lbl.pdf) UDP-glucuronosyltransferase 2B7 (Organism: Homo sapiens, class: Enzyme, accessions: P16662, gene: UGT2B7, swissprot: UD2B7_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/018766s020lbl.pdf) Multidrug resistance-associated protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P33527, gene: ABCC1, swissprot: MRP1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12835412) Multidrug resistance-associated protein 4 (Organism: Homo sapiens, class: Transporter, accessions: O15439, gene: ABCC4, swissprot: MRP4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12835412) Solute carrier family 22 member 6 (Organism: Homo sapiens, class: Transporter, accessions: Q4U2R8, gene: SLC22A6, swissprot: S22A6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10991954) UDP-glucuronosyltransferase 1-1 (Organism: Homo sapiens, class: Enzyme, accessions: P22309, gene: UGT1A1, swissprot: UD11_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15843492) UDP-glucuronosyltransferase 1-3 (Organism: Homo sapiens, class: Enzyme, accessions: P35503, gene: UGT1A3, swissprot: UD13_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15843492) UDP-glucuronosyltransferase 1-4 (Organism: Homo sapiens, class: Enzyme, accessions: P22310, gene: UGT1A4, swissprot: UD14_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15843492) UDP-glucuronosyltransferase 1-6 (Organism: Homo sapiens, class: Enzyme, accessions: P19224, gene: UGT1A6, swissprot: UD16_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15843492) UDP-glucuronosyltransferase 1-8 (Organism: Homo sapiens, class: Enzyme, accessions: Q9HAW9, gene: UGT1A8, swissprot: UD18_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15843492) UDP-glucuronosyltransferase 2B4 (Organism: Homo sapiens, class: Enzyme, accessions: P06133, gene: UGT2B4, swissprot: UD2B4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15843492) UDP-glucuronosyltransferase 1-9 (Organism: Homo sapiens, class: Enzyme, accessions: O60656, gene: UGT1A9, swissprot: UD19_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15843492) UDP-glucuronosyltransferase 1-10 (Organism: Homo sapiens, class: Enzyme, accessions: Q9HAW8, gene: UGT1A10, swissprot: UD110_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15843492) Flurbiprofen is a derivative of propionic acid, and a phenylalkanoic acid derivative of non-steroidal antiinflammatory drugs (NSAIDs) with analgesic, antiinflammatory and antipyretic effects. Flurbiprofen non-selectively binds to and inhibits cyclooxygenase (COX). This results in a reduction of arachidonic acid conversion into prostaglandins that are involved in the regulation of pain, inflammation and fever. This NSAID also inhibits carbonic anhydrase, thereby reducing the production of hydrogen and bicarbonate ions. Upon ocular administration, flurbiprofen may reduce bicarbonate ion concentrations leading to a decrease in the production of aqueous humor, thereby lowering intraocular pressure. Esflurbiprofen (S-enantiomer of flurbiprofen) was approved by PMDA on Sep 28, 2015. Flurbiprofen is used for the treatment of intraoperative miosis, rheumatoid arthritis, osteorarthritis and anklosing spondylitis. Esflurbiprofen is indicated for the treatment of osteoarthritis pain and inflammation. Nonsteroidal Anti-inflammatory Compounds (Code: N0000175721) Nonsteroidal Anti-inflammatory Drug (Code: N0000175722) Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) antipyretic (Code: CHEBI:35493) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) non-narcotic analgesic (Code: CHEBI:35481) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Central Nervous System Agents (Code: D002491) Cyclooxygenase Inhibitors (Code: D016861) Enzyme Inhibitors (Code: D004791) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1986-12-31 FDA FLP
FLR
Click to view gluconic acid Gluconic Acid is the carboxylic acid formed by the oxidation of the first carbon of glucose with antiseptic and chelating properties. Gluconic acid, found abundantly in plant, honey and wine, can be prepared by fungal fermentation process commercially. This agent and its derivatives can used in formulation of pharmaceuticals, cosmetics and food products as additive or buffer salts. Aqueous gluconic acid solution contains cyclic ester glucono delta lactone structure, which chelates metal ions and forms very stable complexes. In alkaline solution, this agent exhibits strong chelating activities towards anions, i.e. calcium, iron, aluminium, copper, and other heavy metals. 1975-08-13 FDA GCO
Click to view bismuth camphocarbonate
Click to view creatinolfosfate Creatinolphosphate is an anti-ischemic and an antiarrhythmic agent. It is used for the treatment of conditions involving a hypoxic damage of the heart muscle. 1968 Italian Medicines Agency (AIFA)
Click to view levodopa D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9633680) D(1A) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21728, gene: DRD1, swissprot: DRD1_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9633680) Carbonic anhydrase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P00915, gene: CA1, swissprot: CAH1_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/16730978) Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/16730978) Carbonic anhydrase 13 (Organism: Mus musculus, class: Enzyme, accessions: Q9D6N1, gene: Ca13, swissprot: CAH13_MOUSE) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/16730978) Carbonic anhydrase 7 (Organism: Homo sapiens, class: Enzyme, accessions: P43166, gene: CA7, swissprot: CAH7_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/17540561) Carbonic anhydrase 14 (Organism: Homo sapiens, class: Enzyme, accessions: Q9ULX7, gene: CA14, swissprot: CAH14_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/17540561) Carbonic anhydrase 5A, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P35218, gene: CA5A, swissprot: CAH5A_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/17174092) Carbonic anhydrase 5B, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: Q9Y2D0, gene: CA5B, swissprot: CAH5B_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/17174092) Carbonic anhydrase 6 (Organism: Homo sapiens, class: Enzyme, accessions: P23280, gene: CA6, swissprot: CAH6_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/17499996) Carbonic anhydrase 9 (Organism: Homo sapiens, class: Enzyme, accessions: Q16790, gene: CA9, swissprot: CAH9_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/18294854) Carbonic anhydrase 12 (Organism: Homo sapiens, class: Enzyme, accessions: O43570, gene: CA12, swissprot: CAH12_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/18294854) Carbonic anhydrase 3 (Organism: Homo sapiens, class: Enzyme, accessions: P07451, gene: CA3, swissprot: CAH3_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/18627905) Carbonic anhydrase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P22748, gene: CA4, swissprot: CAH4_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/18627905) Carbonic anhydrase 15 (Organism: Mus musculus, class: Enzyme, accessions: Q99N23, gene: Ca15, swissprot: CAH15_MOUSE) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/19464888) Carbonic anhydrase (Organism: Methanosarcina thermophila, class: Unclassified, accessions: P40881, gene: None, swissprot: CAH_METTE) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/20061162) Carbonic anhydrase (Organism: Candida albicans (strain SC5314 / ATCC MYA-2876), class: Unclassified, accessions: Q5AJ71, gene: NCE103, swissprot: CAN_CANAL) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/20061162) The naturally occurring form of dihydroxyphenylalanine and the immediate precursor of dopamine. Unlike dopamine itself, it can be taken orally and crosses the blood-brain barrier. It is rapidly taken up by dopaminergic neurons and converted to dopamine. It is used for the treatment of parkinsonian disorders and is usually given with agents that inhibit its conversion to dopamine outside of the central nervous system. antidyskinesia agent (Code: CHEBI:66956) dopaminergic agent (Code: CHEBI:48560) antiparkinson drug (Code: CHEBI:48407) prodrug (Code: CHEBI:50266) Aromatic Amino Acid Decarboxylation Inhibitor (Code: N0000175754) DOPA Decarboxylase Inhibitors (Code: N0000175755) Aromatic Amino Acid (Code: N0000193220) Amino Acids, Aromatic (Code: N0000011248) Anti-Dyskinesia Agents (Code: D018726) Antiparkinson Agents (Code: D000978) Central Nervous System Agents (Code: