Stem definition | Drug id | CAS RN |
---|---|---|
angiogenesis inhibitors | 4178 | 443913-73-3 |
Dose | Unit | Route |
---|---|---|
0.30 | g | O |
Property | Value | Reference |
---|---|---|
BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Hosey CM, Chan R, Benet LZ |
S (Water solubility) | 0.01 mg/mL | Bocci G, Oprea TI, Benet LZ |
Date | Agency | Company | Orphan |
---|---|---|---|
Feb. 16, 2012 | EMA | GENZYME EUROPE BV | |
April 6, 2011 | FDA | IPR PHARMS INC |
MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
---|---|---|---|---|---|---|
Electrocardiogram QT prolonged | 150.65 | 34.55 | 55 | 1401 | 59475 | 63428091 |
Reflux gastritis | 86.03 | 34.55 | 16 | 1440 | 1179 | 63486387 |
Hypophosphataemia | 67.10 | 34.55 | 20 | 1436 | 11406 | 63476160 |
Facial paralysis | 63.03 | 34.55 | 20 | 1436 | 14021 | 63473545 |
Lymphocyte count decreased | 61.93 | 34.55 | 24 | 1432 | 30233 | 63457333 |
Ataxia | 61.48 | 34.55 | 20 | 1436 | 15175 | 63472391 |
Blood triglycerides increased | 61.11 | 34.55 | 19 | 1437 | 12469 | 63475097 |
Myoclonus | 60.63 | 34.55 | 20 | 1436 | 15848 | 63471718 |
Hypophagia | 54.20 | 34.55 | 22 | 1434 | 31237 | 63456329 |
Hemiparesis | 53.13 | 34.55 | 20 | 1436 | 23262 | 63464304 |
Ocular hyperaemia | 51.63 | 34.55 | 20 | 1436 | 25124 | 63462442 |
Flatulence | 45.41 | 34.55 | 20 | 1436 | 34682 | 63452884 |
Neutrophil count decreased | 44.65 | 34.55 | 23 | 1433 | 56383 | 63431183 |
Malignant neoplasm progression | 44.34 | 34.55 | 26 | 1430 | 82095 | 63405471 |
Disease progression | 44.06 | 34.55 | 30 | 1426 | 122728 | 63364838 |
Abdominal distension | 37.96 | 34.55 | 24 | 1432 | 86591 | 63400975 |
Metastases to liver | 35.42 | 34.55 | 15 | 1441 | 23624 | 63463942 |
MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
---|---|---|---|---|---|---|
Electrocardiogram QT prolonged | 79.31 | 34.95 | 29 | 591 | 40923 | 34915388 |
Blood calcitonin increased | 49.82 | 34.95 | 6 | 614 | 25 | 34956286 |
Diarrhoea | 43.58 | 34.95 | 43 | 577 | 389869 | 34566442 |
Acne | 37.67 | 34.95 | 12 | 608 | 11054 | 34945257 |
MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
---|---|---|---|---|---|---|
Electrocardiogram QT prolonged | 173.33 | 32.29 | 70 | 1936 | 90316 | 79652066 |
Reflux gastritis | 83.82 | 32.29 | 16 | 1990 | 1233 | 79741149 |
Myoclonus | 54.79 | 32.29 | 22 | 1984 | 27638 | 79714744 |
Hypophosphataemia | 54.34 | 32.29 | 20 | 1986 | 19893 | 79722489 |
Blood calcitonin increased | 53.38 | 32.29 | 7 | 1999 | 43 | 79742339 |
Facial paralysis | 53.23 | 32.29 | 20 | 1986 | 21052 | 79721330 |
Diarrhoea | 52.47 | 32.29 | 85 | 1921 | 880404 | 78861978 |
Ataxia | 49.88 | 32.29 | 20 | 1986 | 25019 | 79717363 |
Blood triglycerides increased | 49.65 | 32.29 | 19 | 1987 | 21021 | 79721361 |
Lymphocyte count decreased | 49.43 | 32.29 | 24 | 1982 | 47265 | 79695117 |
Ocular hyperaemia | 47.58 | 32.29 | 20 | 1986 | 28186 | 79714196 |
Flatulence | 45.60 | 32.29 | 22 | 1984 | 42702 | 79699680 |
Malignant neoplasm progression | 45.44 | 32.29 | 33 | 1973 | 135957 | 79606425 |
Acne | 44.93 | 32.29 | 19 | 1987 | 27171 | 79715211 |
Hypophagia | 44.35 | 32.29 | 22 | 1984 | 45345 | 79697037 |
Hemiparesis | 44.14 | 32.29 | 20 | 1986 | 33713 | 79708669 |
Hypertension | 43.05 | 32.29 | 47 | 1959 | 330945 | 79411437 |
Metastases to liver | 40.92 | 32.29 | 18 | 1988 | 28296 | 79714086 |
Metastases to bone | 40.13 | 32.29 | 17 | 1989 | 24410 | 79717972 |
None
Source | Code | Description |
---|---|---|
ATC | L01EX04 | ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS PROTEIN KINASE INHIBITORS Other protein kinase inhibitors |
FDA MoA | N0000175076 | Protein Kinase Inhibitors |
FDA EPC | N0000175605 | Kinase Inhibitor |
FDA MoA | N0000185503 | P-Glycoprotein Inhibitors |
FDA MoA | N0000187061 | Organic Cation Transporter 2 Inhibitors |
CHEBI has role | CHEBI:35610 | antineoplastic agents |
CHEBI has role | CHEBI:38637 | tyrosine kinase inhibitors |
Disease | Relation | SNOMED_ID | DOID |
---|---|---|---|
Medullary thyroid carcinoma | indication | 255032005 | DOID:3973 |
Carcinoma of thyroid | indication | 448216007 | |
Hypocalcemia | contraindication | 5291005 | |
Torsades de pointes | contraindication | 31722008 | |
Hypertensive disorder | contraindication | 38341003 | DOID:10763 |
Hypothyroidism | contraindication | 40930008 | DOID:1459 |
Hypokalemia | contraindication | 43339004 | |
Heart failure | contraindication | 84114007 | DOID:6000 |
Prolonged QT interval | contraindication | 111975006 | |
Hypomagnesemia | contraindication | 190855004 | |
Impaired renal function disorder | contraindication | 197663003 | |
Interstitial lung disease | contraindication | 233703007 | DOID:3082 |
Cerebral ischemia | contraindication | 287731003 | |
Pregnancy, function | contraindication | 289908002 | |
Severe diarrhea | contraindication | 409587002 | |
Breastfeeding (mother) | contraindication | 413712001 | |
Congenital long QT syndrome | contraindication | 442917000 | |
Posterior reversible encephalopathy syndrome | contraindication | 450886002 | |
Significant Bleeding | contraindication |
None
None
Dissociation level | Dissociation constant | Type (acidic/basic) |
---|---|---|
pKa1 | 9.58 | Basic |
pKa2 | 5.88 | Basic |
None
None
Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
---|---|---|---|---|---|---|---|---|---|
Proto-oncogene tyrosine-protein kinase receptor Ret | Kinase | INHIBITOR | Kd | 7.85 | CHEMBL | CHEMBL | |||
Epidermal growth factor receptor | Kinase | INHIBITOR | Kd | 8.32 | CHEMBL | CHEMBL | |||
Vascular endothelial growth factor receptor 2 | Kinase | INHIBITOR | Kd | 6.33 | CHEMBL | CHEMBL | |||
Tyrosine-protein kinase ABL1 | Kinase | Kd | 8.05 | CHEMBL | |||||
Mast/stem cell growth factor receptor Kit | Kinase | Kd | 7.47 | CHEMBL | |||||
Breakpoint cluster region protein | Kinase | Kd | 6.06 | CHEMBL | |||||
Proto-oncogene tyrosine-protein kinase Src | Kinase | INHIBITOR | Kd | 7.15 | CHEMBL | ||||
Tyrosine-protein kinase Lck | Kinase | Kd | 7.77 | CHEMBL | |||||
Tyrosine-protein kinase Yes | Kinase | Kd | 6.92 | CHEMBL | |||||
Tyrosine-protein kinase Fyn | Kinase | Kd | 6.44 | CHEMBL | |||||
Ephrin type-A receptor 2 | Kinase | INHIBITOR | Kd | 5.96 | CHEMBL | ||||
Receptor-type tyrosine-protein kinase FLT3 | Kinase | Kd | 6.72 | CHEMBL | |||||
Vascular endothelial growth factor receptor 1 | Kinase | INHIBITOR | Kd | 6.59 | CHEMBL | ||||
Vascular endothelial growth factor receptor 3 | Kinase | INHIBITOR | Kd | 6.52 | CHEMBL | ||||
Macrophage colony-stimulating factor 1 receptor | Kinase | Kd | 5.92 | CHEMBL | |||||
Platelet-derived growth factor receptor alpha | Kinase | Kd | 6.64 | CHEMBL | |||||
Receptor tyrosine-protein kinase erbB-2 | Kinase | INHIBITOR | Kd | 5.59 | CHEMBL | ||||
Phosphorylase b kinase gamma catalytic chain, liver/testis isoform | Kinase | Kd | 5.10 | CHEMBL | |||||
Fibroblast growth factor receptor 3 | Kinase | Kd | 6.62 | CHEMBL | |||||
Tyrosine-protein kinase HCK | Kinase | Kd | 6.44 | CHEMBL | |||||
Receptor tyrosine-protein kinase erbB-4 | Kinase | INHIBITOR | Kd | 6.32 | CHEMBL | ||||
Rho-associated protein kinase 2 | Kinase | Kd | 5.44 | CHEMBL | |||||
Tyrosine-protein kinase CSK | Kinase | Kd | 5.60 | CHEMBL | |||||
Angiopoietin-1 receptor | Kinase | INHIBITOR | Kd | 6 | CHEMBL | ||||
Ephrin type-A receptor 8 | Kinase | INHIBITOR | Kd | 7.04 | CHEMBL | ||||
Hepatocyte growth factor receptor | Kinase | Kd | 5.39 | CHEMBL | |||||
Tyrosine-protein kinase Lyn | Kinase | Kd | 6.96 | CHEMBL | |||||
5'-AMP-activated protein kinase catalytic subunit alpha-1 | Kinase | Kd | 5.52 | CHEMBL | |||||
Fibroblast growth factor receptor 1 | Kinase | Kd | 6.25 | CHEMBL | |||||
Phosphorylase b kinase gamma catalytic chain, skeletal muscle/heart isoform | Kinase | Kd | 5.96 | CHEMBL | |||||
Serine/threonine-protein kinase 10 | Kinase | Kd | 7.09 | CHEMBL | |||||
Serine/threonine-protein kinase PLK4 | Kinase | Kd | 6.21 | CHEMBL | |||||
Aurora kinase C | Kinase | Kd | 5.82 | CHEMBL | |||||
Abelson tyrosine-protein kinase 2 | Kinase | Kd | 7.16 | CHEMBL | |||||
Ephrin type-A receptor 5 | Kinase | INHIBITOR | Kd | 6.62 | CHEMBL | ||||
Ephrin type-A receptor 4 | Kinase | INHIBITOR | Kd | 5.80 | CHEMBL | ||||
Fibroblast growth factor receptor 2 | Kinase | Kd | 5.96 | CHEMBL | |||||
Ephrin type-A receptor 6 | Kinase | INHIBITOR | Kd | 7.30 | CHEMBL | ||||
TRAF2 and NCK-interacting protein kinase | Kinase | Kd | 5.64 | CHEMBL | |||||
Casein kinase I isoform epsilon | Kinase | Kd | 5.82 | CHEMBL | |||||
Tyrosine-protein kinase Fgr | Kinase | Kd | 6.57 | CHEMBL | |||||
ALK tyrosine kinase receptor | Kinase | Kd | 5.68 | CHEMBL | |||||
Ephrin type-A receptor 3 | Kinase | INHIBITOR | Kd | 5.74 | CHEMBL | ||||
Tyrosine-protein kinase FRK | Kinase | Kd | 6.77 | CHEMBL | |||||
Mitogen-activated protein kinase kinase kinase kinase 5 | Kinase | Kd | 6.35 | CHEMBL | |||||
Mitogen-activated protein kinase kinase kinase 4 | Kinase | Kd | 5.52 | CHEMBL | |||||
Cyclin-G-associated kinase | Kinase | Kd | 7.07 | CHEMBL | |||||
Receptor-interacting serine/threonine-protein kinase 2 | Kinase | Kd | 8.34 | CHEMBL | |||||
Ephrin type-B receptor 1 | Kinase | INHIBITOR | Kd | 6.54 | CHEMBL | ||||
Ephrin type-A receptor 7 | Kinase | INHIBITOR | Kd | 5.62 | CHEMBL | ||||
STE20-like serine/threonine-protein kinase | Kinase | Kd | 7.02 | CHEMBL | |||||
MAP kinase-interacting serine/threonine-protein kinase 2 | Kinase | Kd | 5.77 | CHEMBL | |||||
Epithelial discoidin domain-containing receptor 1 | Kinase | Kd | 7.96 | CHEMBL | |||||
Ephrin type-B receptor 4 | Kinase | INHIBITOR | Kd | 6.28 | CHEMBL | ||||
Serine/threonine-protein kinase receptor R3 | Kinase | Kd | 6.33 | CHEMBL | |||||
Activin receptor type-1 | Kinase | Kd | 6.82 | CHEMBL | |||||
Dual specificity mitogen-activated protein kinase kinase 1 | Kinase | Kd | 5.74 | CHEMBL | |||||
Dual specificity mitogen-activated protein kinase kinase 2 | Kinase | Kd | 5.96 | CHEMBL | |||||
Protein-tyrosine kinase 6 | Kinase | INHIBITOR | Kd | 7.48 | CHEMBL | ||||
Tyrosine-protein kinase BTK | Kinase | Kd | 5.77 | CHEMBL | |||||
Tyrosine-protein kinase receptor UFO | Kinase | Kd | 6.60 | CHEMBL | |||||
Tyrosine-protein kinase receptor TYRO3 | Kinase | Kd | 7.03 | CHEMBL | |||||
Ephrin type-B receptor 2 | Kinase | INHIBITOR | Kd | 6.36 | CHEMBL | ||||
Cyclin-dependent kinase 7 | Kinase | Kd | 5.39 | CHEMBL | |||||
Ribosomal protein S6 kinase beta-1 | Kinase | Kd | 5.80 | CHEMBL | |||||
Ribosomal protein S6 kinase alpha-6 | Kinase | Kd | 6.62 | CHEMBL | |||||
Mitogen-activated protein kinase kinase kinase MLT | Kinase | Kd | 5.29 | CHEMBL | |||||
Tyrosine-protein kinase receptor Tie-1 | Kinase | Kd | 5.82 | CHEMBL | |||||
Tyrosine-protein kinase TXK | Kinase | Kd | 5.43 | CHEMBL | |||||
MAP kinase-interacting serine/threonine-protein kinase 1 | Kinase | Kd | 6.44 | CHEMBL | |||||
Serine/threonine-protein kinase SIK2 | Kinase | Kd | 6.37 | CHEMBL | |||||
Serine/threonine-protein kinase 33 | Kinase | Kd | 5.85 | CHEMBL | |||||
Serine/threonine-protein kinase TNNI3K | Kinase | Kd | 5.55 | CHEMBL | |||||
Discoidin domain-containing receptor 2 | Kinase | Kd | 6.49 | CHEMBL | |||||
Chaperone activity of bc1 complex-like, mitochondrial | Kinase | Kd | 5.35 | CHEMBL | |||||
Serine/threonine-protein kinase MRCK gamma | Kinase | Kd | 5.66 | CHEMBL | |||||
Leukocyte tyrosine kinase receptor | Kinase | Kd | 6.26 | CHEMBL | |||||
Mitogen-activated protein kinase kinase kinase kinase 1 | Kinase | Kd | 5.26 | CHEMBL | |||||
Mitogen-activated protein kinase kinase kinase kinase 3 | Kinase | Kd | 5.82 | CHEMBL | |||||
Tyrosine-protein kinase Blk | Kinase | Kd | 7.18 | CHEMBL | |||||
Mitogen-activated protein kinase kinase kinase kinase 4 | Kinase | Kd | 5.85 | CHEMBL | |||||
Tyrosine-protein kinase Mer | Kinase | Kd | 5.85 | CHEMBL | |||||
Serine/threonine-protein kinase MRCK alpha | Kinase | Kd | 5.59 | CHEMBL | |||||
Serine/threonine-protein kinase MRCK beta | Kinase | Kd | 5.60 | CHEMBL | |||||
Citron Rho-interacting kinase | Kinase | Kd | 5.74 | CHEMBL | |||||
AarF domain-containing protein kinase 4 | Kinase | Kd | 5.77 | CHEMBL | |||||
Serine/threonine-protein kinase SIK1 | Kinase | Kd | 5.72 | CHEMBL | |||||
Tyrosine-protein kinase Srms | Kinase | Kd | 5.72 | CHEMBL | |||||
Dual specificity testis-specific protein kinase 1 | Kinase | Kd | 5.43 | CHEMBL | |||||
Ephrin type-A receptor 1 | Kinase | INHIBITOR | Kd | 6.64 | CHEMBL | ||||
Mitogen-activated protein kinase 6 | Kinase | Kd | 5.82 | CHEMBL | |||||
Fibroblast growth factor receptor 4 | Kinase | Kd | 5.64 | CHEMBL | |||||
Ribosomal protein S6 kinase alpha-1 | Kinase | Kd | 6.40 | CHEMBL | |||||
Mitogen-activated protein kinase kinase kinase kinase 2 | Kinase | Kd | 5.80 | CHEMBL | |||||
Misshapen-like kinase 1 | Kinase | Kd | 5.47 | CHEMBL | |||||
Interleukin-1 receptor-associated kinase 4 | Kinase | Kd | 7.12 | CHEMBL | |||||
Ephrin type-B receptor 6 | Kinase | INHIBITOR | Kd | 7.12 | CHEMBL | ||||
Hormonally up-regulated neu tumor-associated kinase | Kinase | Kd | 5.39 | CHEMBL | |||||
Interleukin-1 receptor-associated kinase 1 | Kinase | Kd | 5.92 | CHEMBL | |||||
Serine/threonine-protein kinase ULK3 | Kinase | Kd | 5.19 | CHEMBL | |||||
Mitogen-activated protein kinase kinase kinase 19 | Kinase | Kd | 6.01 | CHEMBL | |||||
Receptor-interacting serine/threonine-protein kinase 4 | Kinase | Kd | 6.21 | CHEMBL | |||||
Serine/threonine-protein kinase 35 | Kinase | Kd | 7.25 | CHEMBL | |||||
Receptor tyrosine-protein kinase erbB-3 | Kinase | INHIBITOR | Kd | 6.80 | CHEMBL | ||||
Serine/threonine-protein kinase SIK3 | Kinase | Kd | 5.41 | CHEMBL | |||||
Bone morphogenetic protein receptor type-1B | Kinase | Kd | 6.62 | CHEMBL | |||||
Serine/threonine-protein kinase 32A | Kinase | Kd | 5.30 | CHEMBL | |||||
Macrophage-stimulating protein receptor | Kinase | IC50 | 5.47 | CHEMBL | |||||
Dual specificity mitogen-activated protein kinase kinase 5 | Kinase | Kd | 7.31 | CHEMBL | |||||
ATP-binding cassette sub-family G member 2 | Transporter | IC50 | 6.70 | CHEMBL | |||||
Platelet-derived growth factor receptor beta | Kinase | Kd | 7.06 | CHEMBL | |||||
Tubulin alpha-1A chain | Structural | Kd | 6.32 | CHEMBL |
ID | Source |
---|---|
4030726 | VUID |
N0000182736 | NUI |
D06407 | KEGG_DRUG |
4030726 | VANDF |
C1121849 | UMLSCUI |
CHEBI:49960 | CHEBI |
ZD6 | PDB_CHEM_ID |
CHEMBL24828 | ChEMBL_ID |
DB05294 | DRUGBANK_ID |
C452423 | MESH_SUPPLEMENTAL_RECORD_UI |
5717 | IUPHAR_LIGAND_ID |
8365 | INN_ID |
YO460OQ37K | UNII |
3081361 | PUBCHEM_CID |
1098413 | RXNORM |
181099 | MMSL |
189346 | MMSL |
27846 | MMSL |
d07761 | MMSL |
013703 | NDDF |
418260004 | SNOMEDCT_US |
418520004 | SNOMEDCT_US |
Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
---|---|---|---|---|---|---|---|---|
CAPRELSA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 58468-7820 | TABLET, FILM COATED | 100 mg | ORAL | NDA | 32 sections |
CAPRELSA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 58468-7820 | TABLET, FILM COATED | 100 mg | ORAL | NDA | 32 sections |
CAPRELSA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 58468-7820 | TABLET, FILM COATED | 100 mg | ORAL | NDA | 32 sections |
CAPRELSA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 58468-7840 | TABLET, FILM COATED | 300 mg | ORAL | NDA | 32 sections |
CAPRELSA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 58468-7840 | TABLET, FILM COATED | 300 mg | ORAL | NDA | 32 sections |
CAPRELSA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 58468-7840 | TABLET, FILM COATED | 300 mg | ORAL | NDA | 32 sections |
CAPRELSA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 58468-7860 | TABLET, FILM COATED | 300 mg | ORAL | UNAPPROVED DRUG FOR USE IN DRUG SHORTAGE | 4 sections |