Stem definition | Drug id | CAS RN |
---|---|---|
tyrosine kinase inhibitors | 4225 | 319460-85-0 |
None
Property | Value | Reference |
---|---|---|
BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Hosey CM, Chan R, Benet LZ |
CL (Clearance) | 5 mL/min/kg | Lombardo F, Berellini G, Obach RS |
fu (Fraction unbound in plasma) | 0.00 % | Lombardo F, Berellini G, Obach RS |
t_half (Half-life) | 4.30 hours | Lombardo F, Berellini G, Obach RS |
Date | Agency | Company | Orphan |
---|---|---|---|
Jan. 27, 2012 | FDA | PFIZER |
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 |
---|---|---|---|---|---|---|
Disease progression | 342.66 | 27.02 | 168 | 4235 | 91132 | 46590527 |
Neoplasm progression | 282.99 | 27.02 | 103 | 4300 | 26580 | 46655079 |
Renal cancer | 248.25 | 27.02 | 58 | 4345 | 3110 | 46678549 |
Diarrhoea | 214.04 | 27.02 | 261 | 4142 | 559341 | 46122318 |
Metastatic renal cell carcinoma | 173.63 | 27.02 | 35 | 4368 | 928 | 46680731 |
Death | 167.10 | 27.02 | 180 | 4223 | 335368 | 46346291 |
Hypertension | 143.29 | 27.02 | 130 | 4273 | 196226 | 46485433 |
Renal cell carcinoma | 119.06 | 27.02 | 33 | 4370 | 3505 | 46678154 |
Palmar-plantar erythrodysaesthesia syndrome | 105.24 | 27.02 | 47 | 4356 | 20404 | 46661255 |
Decreased appetite | 101.25 | 27.02 | 107 | 4296 | 193729 | 46487930 |
Dysphonia | 93.10 | 27.02 | 53 | 4350 | 38361 | 46643298 |
Hypothyroidism | 77.97 | 27.02 | 44 | 4359 | 31294 | 46650365 |
Stomatitis | 71.83 | 27.02 | 56 | 4347 | 68241 | 46613418 |
Blood pressure increased | 67.89 | 27.02 | 71 | 4332 | 126595 | 46555064 |
Fatigue | 46.71 | 27.02 | 144 | 4259 | 608553 | 46073106 |
Posterior reversible encephalopathy syndrome | 39.64 | 27.02 | 22 | 4381 | 15119 | 46666540 |
Dehydration | 38.27 | 27.02 | 60 | 4343 | 159480 | 46522179 |
Weight decreased | 38.27 | 27.02 | 70 | 4333 | 210779 | 46470880 |
Renal cancer metastatic | 35.83 | 27.02 | 8 | 4395 | 348 | 46681311 |
Oligodipsia | 32.56 | 27.02 | 5 | 4398 | 24 | 46681635 |
Oral pain | 31.96 | 27.02 | 23 | 4380 | 24774 | 46656885 |
Proteinuria | 27.60 | 27.02 | 18 | 4385 | 16535 | 46665124 |
Drug ineffective | 27.46 | 27.02 | 15 | 4388 | 677823 | 46003836 |
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 |
---|---|---|---|---|---|---|
Disease progression | 1060.18 | 20.46 | 538 | 10637 | 79336 | 29861967 |
Renal cancer | 650.37 | 20.46 | 173 | 11002 | 3867 | 29937436 |
Neoplasm progression | 630.76 | 20.46 | 241 | 10934 | 17782 | 29923521 |
Dysphonia | 530.73 | 20.46 | 216 | 10959 | 18816 | 29922487 |
Diarrhoea | 413.16 | 20.46 | 559 | 10616 | 333544 | 29607759 |
Metastatic renal cell carcinoma | 378.57 | 20.46 | 102 | 11073 | 2390 | 29938913 |
Renal cell carcinoma | 345.30 | 20.46 | 115 | 11060 | 5651 | 29935652 |
Death | 335.00 | 20.46 | 525 | 10650 | 356758 | 29584545 |
Hypertension | 305.99 | 20.46 | 295 | 10880 | 121059 | 29820244 |
Palmar-plantar erythrodysaesthesia syndrome | 230.63 | 20.46 | 112 | 11063 | 14758 | 29926545 |
Fatigue | 181.89 | 20.46 | 380 | 10795 | 320293 | 29621010 |
Decreased appetite | 142.62 | 20.46 | 223 | 10952 | 149687 | 29791616 |
Blood pressure increased | 122.02 | 20.46 | 142 | 11033 | 71786 | 29869517 |
Hypothyroidism | 102.77 | 20.46 | 66 | 11109 | 14897 | 29926406 |
Neoplasm malignant | 96.95 | 20.46 | 68 | 11107 | 17746 | 29923557 |
Aphonia | 93.09 | 20.46 | 37 | 11138 | 3007 | 29938296 |
Stomatitis | 92.23 | 20.46 | 90 | 11085 | 37189 | 29904114 |
Drug ineffective | 76.36 | 20.46 | 17 | 11158 | 340370 | 29600933 |
Renal cancer metastatic | 71.42 | 20.46 | 20 | 11155 | 541 | 29940762 |
Oral pain | 60.66 | 20.46 | 40 | 11135 | 9429 | 29931874 |
Second primary malignancy | 53.68 | 20.46 | 32 | 11143 | 6324 | 29934979 |
Weight decreased | 51.71 | 20.46 | 148 | 11027 | 150773 | 29790530 |
Proteinuria | 51.59 | 20.46 | 45 | 11130 | 16100 | 29925203 |
Glossodynia | 48.12 | 20.46 | 24 | 11151 | 3337 | 29937966 |
Malignant urinary tract neoplasm | 47.83 | 20.46 | 8 | 11167 | 12 | 29941291 |
Toxicity to various agents | 43.55 | 20.46 | 7 | 11168 | 177176 | 29764127 |
Neutropenia | 31.74 | 20.46 | 5 | 11170 | 128535 | 29812768 |
Blood thyroid stimulating hormone increased | 31.16 | 20.46 | 17 | 11158 | 2839 | 29938464 |
Thyroid disorder | 29.18 | 20.46 | 16 | 11159 | 2698 | 29938605 |
Therapy interrupted | 28.68 | 20.46 | 19 | 11156 | 4510 | 29936793 |
Nausea | 28.10 | 20.46 | 198 | 10977 | 296759 | 29644544 |
Oral discomfort | 24.57 | 20.46 | 14 | 11161 | 2542 | 29938761 |
Febrile neutropenia | 24.49 | 20.46 | 5 | 11170 | 106688 | 29834615 |
Blister | 24.17 | 20.46 | 34 | 11141 | 20649 | 29920654 |
Posterior reversible encephalopathy syndrome | 23.35 | 20.46 | 22 | 11153 | 8685 | 29932618 |
Constipation | 22.89 | 20.46 | 93 | 11082 | 112813 | 29828490 |
Pain in extremity | 22.52 | 20.46 | 91 | 11084 | 110130 | 29831173 |
Renal cell carcinoma stage IV | 22.07 | 20.46 | 5 | 11170 | 55 | 29941248 |
Dry skin | 22.04 | 20.46 | 34 | 11141 | 22420 | 29918883 |
Nephrotic syndrome | 21.60 | 20.46 | 19 | 11156 | 6866 | 29934437 |
Drug interaction | 21.21 | 20.46 | 26 | 11149 | 199542 | 29741761 |
Dysgeusia | 20.85 | 20.46 | 35 | 11140 | 24766 | 29916537 |
Clear cell renal cell carcinoma | 20.64 | 20.46 | 9 | 11166 | 922 | 29940381 |
Dehydration | 20.64 | 20.46 | 96 | 11079 | 123443 | 29817860 |
Source | Code | Description |
---|---|---|
ATC | L01EK01 | ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS PROTEIN KINASE INHIBITORS Vascular endothelial growth factor receptor (VEGFR) tyrosine kinase inhibitors |
FDA MoA | N0000020000 | Receptor Tyrosine Kinase Inhibitors |
FDA EPC | N0000175605 | Kinase Inhibitor |
MeSH PA | D000970 | Antineoplastic Agents |
MeSH PA | D004791 | Enzyme Inhibitors |
MeSH PA | D047428 | Protein Kinase Inhibitors |
CHEBI has role | CHEBI:35610 | cytostatic |
CHEBI has role | CHEBI:38637 | tyrosine kinase inhibitors |
CHEBI has role | CHEBI:65207 | vegfr inhibitors |
Disease | Relation | SNOMED_ID | DOID |
---|---|---|---|
Renal cell carcinoma | indication | 702391001 | DOID:4450 |
Dissociation level | Dissociation constant | Type (acidic/basic) |
---|---|---|
pKa1 | 11.57 | acidic |
pKa2 | 12.18 | acidic |
pKa3 | 4.85 | Basic |
pKa4 | 1.98 | Basic |
None
None
Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
---|---|---|---|---|---|---|---|---|---|
Vascular endothelial growth factor receptor 3 | Kinase | INHIBITOR | Kd | 6.77 | CHEMBL | CHEMBL | |||
Vascular endothelial growth factor receptor 1 | Kinase | INHIBITOR | Kd | 8.24 | CHEMBL | CHEMBL | |||
Vascular endothelial growth factor receptor 2 | Kinase | INHIBITOR | Kd | 8.23 | CHEMBL | CHEMBL | |||
Receptor-type tyrosine-protein kinase FLT3 | Kinase | Kd | 7.51 | CHEMBL | |||||
Cyclin-dependent kinase-like 2 | Kinase | Kd | 6.28 | CHEMBL | |||||
Epidermal growth factor receptor | Kinase | Kd | 5.64 | CHEMBL | |||||
Fibroblast growth factor receptor 3 | Kinase | Kd | 6.68 | CHEMBL | |||||
SRSF protein kinase 1 | Kinase | Kd | 5.74 | CHEMBL | |||||
Platelet-derived growth factor receptor alpha | Kinase | Kd | 9.29 | CHEMBL | |||||
Serine/threonine-protein kinase RIO3 | Kinase | Kd | 6 | CHEMBL | |||||
Hepatocyte growth factor receptor | Kinase | Kd | 6.09 | CHEMBL | |||||
Receptor-interacting serine/threonine-protein kinase 2 | Kinase | Kd | 5 | CHEMBL | |||||
Tyrosine-protein kinase JAK2 | Kinase | Kd | 5.48 | CHEMBL | |||||
Cyclin-G-associated kinase | Kinase | Kd | 5.57 | CHEMBL | |||||
Aurora kinase A | Kinase | Kd | 7.14 | CHEMBL | |||||
Dual specificity mitogen-activated protein kinase kinase 5 | Kinase | Kd | 6.85 | CHEMBL | |||||
Tyrosine-protein kinase ITK/TSK | Kinase | Kd | 5.92 | CHEMBL | |||||
Mitogen-activated protein kinase kinase kinase MLT | Kinase | Kd | 5.59 | CHEMBL | |||||
Interferon-induced, double-stranded RNA-activated protein kinase | Kinase | Kd | 5.13 | CHEMBL | |||||
Mitogen-activated protein kinase kinase kinase kinase 1 | Kinase | Kd | 6.48 | CHEMBL | |||||
Tyrosine-protein kinase Fgr | Kinase | Kd | 5.74 | CHEMBL | |||||
Dual specificity protein kinase TTK | Kinase | Kd | 5.41 | CHEMBL | |||||
Serine/threonine-protein kinase 10 | Kinase | Kd | 5.92 | CHEMBL | |||||
Serine/threonine-protein kinase 16 | Kinase | Kd | 6.43 | CHEMBL | |||||
Serine/threonine-protein kinase PLK4 | Kinase | Ki | 8.38 | CHEMBL | |||||
AP2-associated protein kinase 1 | Kinase | Kd | 5.92 | CHEMBL | |||||
Tyrosine-protein kinase JAK3 | Kinase | Kd | 5.51 | CHEMBL | |||||
Casein kinase II subunit alpha' | Kinase | Kd | 5.55 | CHEMBL | |||||
Tyrosine-protein kinase Yes | Kinase | Kd | 5.57 | CHEMBL | |||||
Serine/threonine-protein kinase N2 | Kinase | Kd | 5.57 | CHEMBL | |||||
Tyrosine-protein kinase CSK | Kinase | Kd | 5.96 | CHEMBL | |||||
Aurora kinase C | Kinase | Kd | 8.89 | CHEMBL | |||||
High affinity nerve growth factor receptor | Kinase | Kd | 5.74 | CHEMBL | |||||
Platelet-derived growth factor receptor beta | Kinase | Kd | 9.24 | CHEMBL | |||||
Fibroblast growth factor receptor 1 | Kinase | Kd | 6.42 | CHEMBL | |||||
Fibroblast growth factor receptor 2 | Kinase | Kd | 6.96 | CHEMBL | |||||
Myosin-IIIa | Kinase | Kd | 5.72 | CHEMBL | |||||
Ankyrin repeat and protein kinase domain-containing protein 1 | Kinase | Kd | 5.44 | CHEMBL | |||||
Mitogen-activated protein kinase kinase kinase 4 | Kinase | Kd | 5.25 | CHEMBL | |||||
Mitogen-activated protein kinase kinase kinase kinase 5 | Kinase | Kd | 6.26 | CHEMBL | |||||
Misshapen-like kinase 1 | Kinase | Kd | 6.25 | CHEMBL | |||||
Leucine-rich repeat serine/threonine-protein kinase 2 | Kinase | Kd | 6.04 | CHEMBL | |||||
Mast/stem cell growth factor receptor Kit | Kinase | Kd | 9.31 | CHEMBL | |||||
BMP-2-inducible protein kinase | Kinase | Kd | 6 | CHEMBL | |||||
TRAF2 and NCK-interacting protein kinase | Kinase | Kd | 6.74 | CHEMBL | |||||
Calcium/calmodulin-dependent protein kinase kinase 2 | Kinase | Kd | 5.82 | CHEMBL | |||||
Aurora kinase B | Kinase | Kd | 7.96 | CHEMBL | |||||
STE20-like serine/threonine-protein kinase | Kinase | Kd | 6 | CHEMBL | |||||
Bone morphogenetic protein receptor type-1B | Kinase | Kd | 5.54 | CHEMBL | |||||
Non-receptor tyrosine-protein kinase TYK2 | Kinase | Kd | 5.44 | CHEMBL | |||||
Interleukin-1 receptor-associated kinase 1 | Kinase | Kd | 5.51 | CHEMBL | |||||
Serine/threonine-protein kinase 4 | Kinase | Kd | 5.85 | CHEMBL | |||||
Calcium/calmodulin-dependent protein kinase kinase 1 | Kinase | Kd | 5.85 | CHEMBL | |||||
Serine/threonine-protein kinase 3 | Kinase | Kd | 5.66 | CHEMBL | |||||
Serine/threonine-protein kinase ULK2 | Kinase | Kd | 5 | CHEMBL | |||||
Activated CDC42 kinase 1 | Kinase | Kd | 5.22 | CHEMBL | |||||
Cyclin-dependent kinase 16 | Kinase | Kd | 5.28 | CHEMBL | |||||
Mitogen-activated protein kinase kinase kinase kinase 3 | Kinase | Kd | 5.92 | CHEMBL | |||||
Dual specificity testis-specific protein kinase 1 | Kinase | Kd | 5.37 | CHEMBL | |||||
Serine/threonine-protein kinase MRCK beta | Kinase | Kd | 5.32 | CHEMBL | |||||
G protein-coupled receptor kinase 4 | Kinase | Kd | 5.64 | CHEMBL | |||||
Serine/threonine-protein kinase ULK3 | Kinase | Kd | 6.17 | CHEMBL | |||||
Abelson tyrosine-protein kinase 2 | Kinase | Kd | 7.15 | CHEMBL | |||||
Activin receptor type-2B | Kinase | Kd | 5.28 | CHEMBL | |||||
Tyrosine-protein kinase Blk | Kinase | Kd | 5.51 | CHEMBL | |||||
Angiopoietin-1 receptor | Kinase | Kd | 6.51 | CHEMBL | |||||
Proto-oncogene tyrosine-protein kinase ROS | Kinase | Kd | 5.49 | CHEMBL | |||||
Ephrin type-B receptor 6 | Kinase | Kd | 6.44 | CHEMBL | |||||
Mitogen-activated protein kinase 8 | Kinase | Kd | 5.41 | CHEMBL | |||||
Macrophage colony-stimulating factor 1 receptor | Kinase | Kd | 7.68 | CHEMBL | |||||
Hormonally up-regulated neu tumor-associated kinase | Kinase | Kd | 5.82 | CHEMBL | |||||
Discoidin domain-containing receptor 2 | Kinase | Kd | 5.28 | CHEMBL | |||||
Tyrosine-protein kinase receptor Tie-1 | Kinase | Kd | 7.01 | CHEMBL | |||||
Serine/threonine-protein kinase PAK 4 | Kinase | Kd | 5.35 | CHEMBL | |||||
Proto-oncogene tyrosine-protein kinase receptor Ret | Kinase | Kd | 7 | CHEMBL | |||||
Epithelial discoidin domain-containing receptor 1 | Kinase | Kd | 6.47 | CHEMBL | |||||
Mitogen-activated protein kinase kinase kinase kinase 4 | Kinase | Kd | 6.46 | CHEMBL | |||||
Tyrosine-protein kinase Lck | Kinase | Kd | 5.57 | CHEMBL | |||||
Myosin light chain kinase 2, skeletal/cardiac muscle | Kinase | Kd | 5.89 | CHEMBL | |||||
Mitogen-activated protein kinase kinase kinase 9 | Kinase | Kd | 5.52 | CHEMBL | |||||
Mitogen-activated protein kinase kinase kinase 19 | Kinase | Kd | 6.57 | CHEMBL | |||||
Tyrosine-protein kinase receptor UFO | Kinase | Kd | 6.38 | CHEMBL | |||||
NUAK family SNF1-like kinase 2 | Kinase | Kd | 5.89 | CHEMBL | |||||
Dual specificity mitogen-activated protein kinase kinase 2 | Kinase | Kd | 5.59 | CHEMBL | |||||
SRSF protein kinase 3 | Kinase | Kd | 5.64 | CHEMBL | |||||
Tyrosine-protein kinase TXK | Kinase | Kd | 5.62 | CHEMBL | |||||
Mitogen-activated protein kinase kinase kinase 12 | Kinase | Kd | 5.77 | CHEMBL | |||||
Myosin light chain kinase 3 | Kinase | Kd | 5.77 | CHEMBL | |||||
Receptor-interacting serine/threonine-protein kinase 1 | Kinase | Kd | 5.60 | CHEMBL | |||||
Mitogen-activated protein kinase kinase kinase 3 | Kinase | Kd | 5.55 | CHEMBL | |||||
Serine/threonine-protein kinase RIO1 | Kinase | Kd | 5.92 | CHEMBL | |||||
Receptor-interacting serine/threonine-protein kinase 4 | Kinase | Kd | 5.85 | CHEMBL | |||||
Serine/threonine-protein kinase SIK1 | Kinase | Kd | 5.68 | CHEMBL | |||||
Mitogen-activated protein kinase kinase kinase kinase 2 | Kinase | Kd | 5.89 | CHEMBL | |||||
Tyrosine-protein kinase Mer | Kinase | Kd | 5.49 | CHEMBL | |||||
Mitogen-activated protein kinase 10 | Kinase | Kd | 5.96 | CHEMBL | |||||
Non-receptor tyrosine-protein kinase TNK1 | Kinase | Kd | 6.80 | CHEMBL | |||||
Dual specificity mitogen-activated protein kinase kinase 1 | Kinase | Kd | 5.57 | CHEMBL | |||||
Tyrosine-protein kinase ABL1 | Kinase | Kd | 8.82 | CHEMBL |
ID | Source |
---|---|
C9LVQ0YUXG | UNII |
4031332 | VUID |
N0000184323 | NUI |
D03218 | KEGG_DRUG |
4031332 | VANDF |
C1328149 | UMLSCUI |
CHEBI:66910 | CHEBI |
AXI | PDB_CHEM_ID |
CHEMBL1289926 | ChEMBL_ID |
6450551 | PUBCHEM_CID |
DB06626 | DRUGBANK_ID |
D000077784 | MESH_DESCRIPTOR_UI |
8720 | INN_ID |
5659 | IUPHAR_LIGAND_ID |
1242999 | RXNORM |
187097 | MMSL |
28294 | MMSL |
d07823 | MMSL |
014143 | NDDF |
427882000 | SNOMEDCT_US |
429507005 | SNOMEDCT_US |
Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
---|---|---|---|---|---|---|---|---|
INLYTA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0069-0145 | TABLET, FILM COATED | 1 mg | ORAL | NDA | 32 sections |
INLYTA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0069-0151 | TABLET, FILM COATED | 5 mg | ORAL | NDA | 32 sections |
INLYTA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 63539-026 | TABLET, FILM COATED | 1 mg | ORAL | NDA | 29 sections |
INLYTA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 63539-044 | TABLET, FILM COATED | 5 mg | ORAL | NDA | 29 sections |