Stem definition | Drug id | CAS RN |
---|---|---|
tyrosine kinase inhibitors | 4942 | 417716-92-8 |
None
None
Date | Agency | Company | Orphan |
---|---|---|---|
May 28, 2015 | EMA | Eisai Europe Ltd | |
Feb. 13, 2015 | FDA | EISAI 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 |
---|---|---|---|---|---|---|
Hypertension | 658.70 | 27.44 | 399 | 7013 | 195957 | 46482693 |
Malignant neoplasm progression | 593.79 | 27.44 | 260 | 7152 | 64666 | 46613984 |
Proteinuria | 424.47 | 27.44 | 141 | 7271 | 16412 | 46662238 |
Decreased appetite | 344.47 | 27.44 | 267 | 7145 | 193569 | 46485081 |
Palmar-plantar erythrodysaesthesia syndrome | 277.99 | 27.44 | 109 | 7303 | 20342 | 46658308 |
Hepatic encephalopathy | 214.95 | 27.44 | 75 | 7337 | 10082 | 46668568 |
Diarrhoea | 145.92 | 27.44 | 291 | 7121 | 559311 | 46119339 |
Blood pressure increased | 94.17 | 27.44 | 108 | 7304 | 126558 | 46552092 |
Platelet count decreased | 93.05 | 27.44 | 96 | 7316 | 99928 | 46578722 |
Stomatitis | 89.05 | 27.44 | 79 | 7333 | 68218 | 46610432 |
Cholecystitis | 85.39 | 27.44 | 43 | 7369 | 14423 | 46664227 |
Hypothyroidism | 84.72 | 27.44 | 56 | 7356 | 31282 | 46647368 |
Tumour haemorrhage | 79.11 | 27.44 | 22 | 7390 | 1393 | 46677257 |
Tracheal fistula | 69.04 | 27.44 | 11 | 7401 | 37 | 46678613 |
Drug ineffective | 65.66 | 27.44 | 14 | 7398 | 677824 | 46000826 |
Fatigue | 64.66 | 27.44 | 227 | 7185 | 608470 | 46070180 |
Arterial haemorrhage | 49.44 | 27.44 | 16 | 7396 | 1702 | 46676948 |
Pneumothorax | 46.59 | 27.44 | 29 | 7383 | 14600 | 46664050 |
Oral pain | 43.30 | 27.44 | 34 | 7378 | 24763 | 46653887 |
Blood thyroid stimulating hormone increased | 42.28 | 27.44 | 20 | 7392 | 5849 | 46672801 |
Fistula | 42.02 | 27.44 | 22 | 7390 | 7988 | 46670662 |
Ascites | 39.25 | 27.44 | 38 | 7374 | 36546 | 46642104 |
Vomiting | 38.82 | 27.44 | 158 | 7254 | 452636 | 46226014 |
Dehydration | 37.54 | 27.44 | 80 | 7332 | 159460 | 46519190 |
Epistaxis | 35.06 | 27.44 | 47 | 7365 | 64258 | 46614392 |
Nephrotic syndrome | 33.11 | 27.44 | 16 | 7396 | 4905 | 46673745 |
Tracheal haemorrhage | 32.23 | 27.44 | 7 | 7405 | 156 | 46678494 |
Dysphonia | 30.57 | 27.44 | 34 | 7378 | 38380 | 46640270 |
Protein urine present | 29.53 | 27.44 | 15 | 7397 | 5116 | 46673534 |
Malaise | 29.44 | 27.44 | 117 | 7295 | 331115 | 46347535 |
Ammonia increased | 28.75 | 27.44 | 14 | 7398 | 4363 | 46674287 |
Drug hypersensitivity | 28.12 | 27.44 | 3 | 7409 | 243822 | 46434828 |
Cerebral haemorrhage | 27.70 | 27.44 | 28 | 7384 | 28343 | 46650307 |
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 |
---|---|---|---|---|---|---|
Decreased appetite | 671.71 | 24.02 | 504 | 10608 | 149406 | 29791960 |
Malignant neoplasm progression | 635.89 | 24.02 | 371 | 10741 | 71916 | 29869450 |
Hepatic encephalopathy | 601.02 | 24.02 | 218 | 10894 | 13974 | 29927392 |
Proteinuria | 433.06 | 24.02 | 178 | 10934 | 15967 | 29925399 |
Hypertension | 394.36 | 24.02 | 339 | 10773 | 121015 | 29820351 |
Palmar-plantar erythrodysaesthesia syndrome | 392.16 | 24.02 | 162 | 10950 | 14708 | 29926658 |
Diarrhoea | 336.45 | 24.02 | 506 | 10606 | 333597 | 29607769 |
Hypothyroidism | 200.89 | 24.02 | 102 | 11010 | 14861 | 29926505 |
Fatigue | 174.00 | 24.02 | 372 | 10740 | 320301 | 29621065 |
Tumour haemorrhage | 157.86 | 24.02 | 52 | 11060 | 2476 | 29938890 |
Blood pressure increased | 141.60 | 24.02 | 153 | 10959 | 71775 | 29869591 |
Dysphonia | 131.34 | 24.02 | 84 | 11028 | 18948 | 29922418 |
Liver carcinoma ruptured | 111.46 | 24.02 | 22 | 11090 | 116 | 29941250 |
Malaise | 102.01 | 24.02 | 204 | 10908 | 166758 | 29774608 |
Oesophageal varices haemorrhage | 93.21 | 24.02 | 37 | 11075 | 3014 | 29938352 |
Ascites | 91.69 | 24.02 | 88 | 11024 | 35833 | 29905533 |
Hepatic failure | 89.93 | 24.02 | 85 | 11027 | 33958 | 29907408 |
Ammonia increased | 81.47 | 24.02 | 37 | 11075 | 4204 | 29937162 |
Stomatitis | 74.44 | 24.02 | 80 | 11032 | 37199 | 29904167 |
Cholecystitis | 70.34 | 24.02 | 44 | 11068 | 9535 | 29931831 |
Drug ineffective | 69.94 | 24.02 | 20 | 11092 | 340367 | 29600999 |
Dehydration | 67.13 | 24.02 | 144 | 10968 | 123395 | 29817971 |
Renal cancer | 64.45 | 24.02 | 31 | 11081 | 4009 | 29937357 |
Blood thyroid stimulating hormone increased | 61.52 | 24.02 | 27 | 11085 | 2829 | 29938537 |
Oral pain | 58.45 | 24.02 | 39 | 11073 | 9430 | 29931936 |
Epistaxis | 56.40 | 24.02 | 83 | 11029 | 52898 | 29888468 |
Pneumothorax | 55.77 | 24.02 | 47 | 11065 | 16146 | 29925220 |
Blood bilirubin increased | 55.21 | 24.02 | 68 | 11044 | 36568 | 29904798 |
Cholangitis | 52.70 | 24.02 | 34 | 11078 | 7768 | 29933598 |
Tumour rupture | 50.98 | 24.02 | 12 | 11100 | 159 | 29941207 |
Weight decreased | 49.33 | 24.02 | 145 | 10967 | 150776 | 29790590 |
Hepatic function abnormal | 46.50 | 24.02 | 67 | 11045 | 41878 | 29899488 |
Hyperammonaemia | 42.15 | 24.02 | 26 | 11086 | 5494 | 29935872 |
Condition aggravated | 37.05 | 24.02 | 4 | 11108 | 137862 | 29803504 |
Toxicity to various agents | 37.04 | 24.02 | 10 | 11102 | 177173 | 29764193 |
Vomiting | 36.79 | 24.02 | 170 | 10942 | 219648 | 29721718 |
Tracheal fistula | 36.42 | 24.02 | 8 | 11104 | 76 | 29941290 |
Portal vein thrombosis | 36.20 | 24.02 | 20 | 11092 | 3444 | 29937922 |
Drug interaction | 35.25 | 24.02 | 15 | 11097 | 199553 | 29741813 |
Rhythm idioventricular | 31.17 | 24.02 | 9 | 11103 | 274 | 29941092 |
Protein urine present | 30.27 | 24.02 | 20 | 11092 | 4755 | 29936611 |
Platelet count decreased | 29.08 | 24.02 | 96 | 11016 | 106033 | 29835333 |
Off label use | 28.89 | 24.02 | 30 | 11082 | 249260 | 29692106 |
Cholecystitis acute | 28.32 | 24.02 | 20 | 11092 | 5297 | 29936069 |
Gastrointestinal perforation | 27.52 | 24.02 | 17 | 11095 | 3599 | 29937767 |
Tracheo-oesophageal fistula | 27.44 | 24.02 | 9 | 11103 | 422 | 29940944 |
Nausea | 27.42 | 24.02 | 196 | 10916 | 296761 | 29644605 |
Haemobilia | 26.39 | 24.02 | 8 | 11104 | 289 | 29941077 |
Taste disorder | 25.56 | 24.02 | 16 | 11096 | 3467 | 29937899 |
Source | Code | Description |
---|---|---|
ATC | L01EX08 | ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS PROTEIN KINASE INHIBITORS Other protein 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:62434 | alk inhibitor |
CHEBI has role | CHEBI:63457 | fibroblast growth factor receptor antagonists |
CHEBI has role | CHEBI:65207 | vegfr inhibitors |
CHEBI has role | CHEBI:71031 | orphan drugs |
Disease | Relation | SNOMED_ID | DOID |
---|---|---|---|
Follicular thyroid carcinoma | indication | 255028004 | DOID:3962 |
Papillary thyroid carcinoma | indication | 255029007 | DOID:3969 |
Renal cell carcinoma | indication | 702391001 | DOID:4450 |
Dissociation level | Dissociation constant | Type (acidic/basic) |
---|---|---|
pKa1 | 12.09 | acidic |
pKa2 | 12.74 | acidic |
pKa3 | 13.02 | acidic |
pKa4 | 4.67 | Basic |
None
Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
---|---|---|---|---|---|---|---|---|---|
EQ 10MG BASE | LENVIMA | EISAI INC | N206947 | Feb. 13, 2015 | RX | CAPSULE | ORAL | Aug. 15, 2021 | FIRST-LINE TREATMENT OF PATIENTS WITH UNRESECTABLE HEPATOCELLULAR CARCINOMA (HCC) |
EQ 4MG BASE | LENVIMA | EISAI INC | N206947 | Feb. 13, 2015 | RX | CAPSULE | ORAL | Aug. 15, 2021 | FIRST-LINE TREATMENT OF PATIENTS WITH UNRESECTABLE HEPATOCELLULAR CARCINOMA (HCC) |
EQ 10MG BASE | LENVIMA | EISAI INC | N206947 | Feb. 13, 2015 | RX | CAPSULE | ORAL | Feb. 13, 2022 | TREATMENT OF PATIENTS WITH LOCALLY RECURRENT OR METASTATIC, PROGRESSIVE, RADIOACTIVE IODINE REFRACTORY DIFFERENTIATED THYROID CANCER |
EQ 4MG BASE | LENVIMA | EISAI INC | N206947 | Feb. 13, 2015 | RX | CAPSULE | ORAL | Feb. 13, 2022 | TREATMENT OF PATIENTS WITH LOCALLY RECURRENT OR METASTATIC, PROGRESSIVE, RADIOACTIVE IODINE REFRACTORY DIFFERENTIATED THYROID CANCER |
EQ 10MG BASE | LENVIMA | EISAI INC | N206947 | Feb. 13, 2015 | RX | CAPSULE | ORAL | Sept. 17, 2022 | TREATMENT OF ADVANCED ENDOMETRIAL CARCINOMA THAT IS NOT MICROSATELLITE INSTABILITY-HIGH OR MISMATCH REPAIR DEFICIENT, WHO HAVE DISEASE PROGRESSION FOLLOWING PRIOR SYSTEMIC THERAPY AND ARE NOT CANDIDATES FOR CURATIVE SURGERY OR RADIATION |
EQ 4MG BASE | LENVIMA | EISAI INC | N206947 | Feb. 13, 2015 | RX | CAPSULE | ORAL | Sept. 17, 2022 | TREATMENT OF ADVANCED ENDOMETRIAL CARCINOMA THAT IS NOT MICROSATELLITE INSTABILITY-HIGH OR MISMATCH REPAIR DEFICIENT, WHO HAVE DISEASE PROGRESSION FOLLOWING PRIOR SYSTEMIC THERAPY AND ARE NOT CANDIDATES FOR CURATIVE SURGERY OR RADIATION |
EQ 10MG BASE | LENVIMA | EISAI INC | N206947 | Feb. 13, 2015 | RX | CAPSULE | ORAL | Aug. 15, 2025 | INDICATED FOR THE FIRST-LINE TREATMENT OF PATIENTS WITH UNRESECTABLE HEPATOCELLULAR CARCINOMA (HCC) |
EQ 4MG BASE | LENVIMA | EISAI INC | N206947 | Feb. 13, 2015 | RX | CAPSULE | ORAL | Aug. 15, 2025 | INDICATED FOR THE FIRST-LINE TREATMENT OF PATIENTS WITH UNRESECTABLE HEPATOCELLULAR CARCINOMA (HCC) |
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 | Ki | 8.82 | CHEMBL | DRUG LABEL | |||
Vascular endothelial growth factor receptor 2 | Kinase | INHIBITOR | IC50 | 8.40 | SCIENTIFIC LITERATURE | DRUG LABEL | |||
Vascular endothelial growth factor receptor 3 | Kinase | INHIBITOR | IC50 | 8.28 | SCIENTIFIC LITERATURE | DRUG LABEL | |||
Fibroblast growth factor receptor 1 | Kinase | INHIBITOR | IC50 | 7.34 | SCIENTIFIC LITERATURE | DRUG LABEL | |||
Platelet-derived growth factor receptor alpha | Kinase | INHIBITOR | IC50 | 7.29 | SCIENTIFIC LITERATURE | DRUG LABEL | |||
Mast/stem cell growth factor receptor Kit | Kinase | INHIBITOR | IC50 | 7 | SCIENTIFIC LITERATURE | DRUG LABEL | |||
Vascular endothelial growth factor receptor 1 | Kinase | INHIBITOR | IC50 | 7.66 | SCIENTIFIC LITERATURE | DRUG LABEL | |||
Platelet-derived growth factor receptor beta | Kinase | INHIBITOR | IC50 | 7.41 | SCIENTIFIC LITERATURE | ||||
Epidermal growth factor receptor | Kinase | INHIBITOR | IC50 | 5.19 | SCIENTIFIC LITERATURE |
ID | Source |
---|---|
D09919 | KEGG_DRUG |
4034239 | VUID |
N0000191429 | NUI |
857890-39-2 | SECONDARY_CAS_RN |
4034239 | VANDF |
C2606791 | UMLSCUI |
CHEBI:85994 | CHEBI |
LEV | PDB_CHEM_ID |
CHEMBL1289601 | ChEMBL_ID |
CHEMBL2105704 | ChEMBL_ID |
DB09078 | DRUGBANK_ID |
C531958 | MESH_SUPPLEMENTAL_RECORD_UI |
9823820 | PUBCHEM_CID |
7426 | IUPHAR_LIGAND_ID |
9361 | INN_ID |
EE083865G2 | UNII |
1603296 | RXNORM |
232716 | MMSL |
294829 | MMSL |
294831 | MMSL |
30895 | MMSL |
d08346 | MMSL |
015899 | NDDF |
015900 | NDDF |
714108002 | SNOMEDCT_US |
714109005 | SNOMEDCT_US |
735068004 | SNOMEDCT_US |
Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
---|---|---|---|---|---|---|---|---|
Lenvima | HUMAN PRESCRIPTION DRUG LABEL | 1 | 62856-704 | CAPSULE | 4 mg | ORAL | NDA | 29 sections |
Lenvima | HUMAN PRESCRIPTION DRUG LABEL | 1 | 62856-708 | CAPSULE | 4 mg | ORAL | NDA | 29 sections |
Lenvima | HUMAN PRESCRIPTION DRUG LABEL | 1 | 62856-710 | CAPSULE | 10 mg | ORAL | NDA | 29 sections |
Lenvima | HUMAN PRESCRIPTION DRUG LABEL | 1 | 62856-712 | CAPSULE | 4 mg | ORAL | NDA | 29 sections |
Lenvima | HUMAN PRESCRIPTION DRUG LABEL | 1 | 62856-720 | CAPSULE | 10 mg | ORAL | NDA | 29 sections |