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 |
Date | Agency | Company | Orphan |
---|---|---|---|
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 | 133.34 | 35.93 | 50 | 1254 | 51836 | 50551984 |
Reflux gastritis | 75.85 | 35.93 | 14 | 1290 | 879 | 50602941 |
Hypophosphataemia | 61.88 | 35.93 | 18 | 1286 | 8396 | 50595424 |
Lymphocyte count decreased | 55.41 | 35.93 | 22 | 1282 | 26285 | 50577535 |
Facial paralysis | 54.56 | 35.93 | 18 | 1286 | 12697 | 50591123 |
Ataxia | 53.13 | 35.93 | 18 | 1286 | 13768 | 50590052 |
Blood triglycerides increased | 52.52 | 35.93 | 17 | 1287 | 11295 | 50592525 |
Myoclonus | 52.28 | 35.93 | 18 | 1286 | 14452 | 50589368 |
Hemiparesis | 46.55 | 35.93 | 18 | 1286 | 20030 | 50583790 |
Ocular hyperaemia | 46.34 | 35.93 | 18 | 1286 | 20274 | 50583546 |
Hypophagia | 44.18 | 35.93 | 19 | 1285 | 27709 | 50576111 |
Disease progression | 42.70 | 35.93 | 28 | 1276 | 95838 | 50507982 |
Malignant neoplasm progression | 40.72 | 35.93 | 24 | 1280 | 68100 | 50535720 |
Neutrophil count decreased | 40.69 | 35.93 | 21 | 1283 | 46005 | 50557815 |
Flatulence | 39.86 | 35.93 | 18 | 1286 | 29440 | 50574380 |
Metastases to liver | 36.09 | 35.93 | 15 | 1289 | 20089 | 50583731 |
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 | 83.80 | 35.42 | 29 | 481 | 36108 | 29537909 |
Blood calcitonin increased | 52.33 | 35.42 | 6 | 504 | 15 | 29574002 |
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 | 160.41 | 32.33 | 65 | 1666 | 79383 | 64417618 |
Reflux gastritis | 73.68 | 32.33 | 14 | 1717 | 986 | 64496015 |
Blood calcitonin increased | 54.32 | 32.33 | 7 | 1724 | 34 | 64496967 |
Hypophosphataemia | 51.23 | 32.33 | 18 | 1713 | 14702 | 64482299 |
Myoclonus | 48.58 | 32.33 | 20 | 1711 | 25098 | 64471903 |
Facial paralysis | 46.78 | 32.33 | 18 | 1713 | 18948 | 64478053 |
Lymphocyte count decreased | 45.28 | 32.33 | 22 | 1709 | 40677 | 64456324 |
Malignant neoplasm progression | 44.35 | 32.33 | 31 | 1700 | 112840 | 64384161 |
Ataxia | 44.12 | 32.33 | 18 | 1713 | 22066 | 64474935 |
Ocular hyperaemia | 43.75 | 32.33 | 18 | 1713 | 22546 | 64474455 |
Blood triglycerides increased | 43.32 | 32.33 | 17 | 1714 | 18849 | 64478152 |
Metastases to liver | 42.72 | 32.33 | 18 | 1713 | 23923 | 64473078 |
Metastases to bone | 42.00 | 32.33 | 17 | 1714 | 20418 | 64476583 |
Hemiparesis | 38.92 | 32.33 | 18 | 1713 | 29809 | 64467192 |
Flatulence | 38.83 | 32.33 | 19 | 1712 | 35647 | 64461354 |
Hypophagia | 36.95 | 32.33 | 19 | 1712 | 39568 | 64457433 |
Diarrhoea | 34.86 | 32.33 | 66 | 1665 | 722638 | 63774363 |
Blood cholesterol increased | 32.77 | 32.33 | 19 | 1712 | 50047 | 64446954 |
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 |
---|---|---|---|
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 |
Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
---|---|---|---|---|---|---|---|---|---|---|
100MG | CAPRELSA | GENZYME CORP | N022405 | April 6, 2011 | RX | TABLET | ORAL | 8642608 | Feb. 6, 2022 | FOR USE IN PATIENTS HAVING SYMPTOMATIC OR PROGRESSIVE MEDULLARY THYROID CANCER, WITH UNRESECTABLE LOCALLY ADVANCED OR METASTATIC DISEASE |
300MG | CAPRELSA | GENZYME CORP | N022405 | April 6, 2011 | RX | TABLET | ORAL | 8642608 | Feb. 6, 2022 | FOR USE IN PATIENTS HAVING SYMPTOMATIC OR PROGRESSIVE MEDULLARY THYROID CANCER, WITH UNRESECTABLE LOCALLY ADVANCED OR METASTATIC DISEASE |
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 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 | |||||
Tyrosine-protein kinase Yes | Kinase | Kd | 6.92 | CHEMBL | |||||
Dual specificity mitogen-activated protein kinase kinase 5 | Kinase | Kd | 7.31 | CHEMBL | |||||
Macrophage-stimulating protein receptor | Kinase | IC50 | 5.47 | 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 | 58468-7840 | 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 |