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)