lenvatinib Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
tyrosine kinase inhibitors 4942 417716-92-8

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • E-7080
  • E 7080
  • lenvatinib
  • lenvima
  • ER-203492-00
  • E7080
  • lenvatinib mesylate
  • lenvatinib mesilate
a receptor tyrosine kinase (RTK) inhibitor that inhibits the kinase activities of vascular endothelial growth factor (VEGF) receptors VEGFR1 (FLT1), VEGFR2 (KDR), and VEGFR3 (FLT4)
  • Molecular weight: 426.86
  • Formula: C21H19ClN4O4
  • CLOGP: 3.35
  • LIPINSKI: 0
  • HAC: 8
  • HDO: 3
  • TPSA: 115.57
  • ALOGS: -4.84
  • ROTB: 6

  • Status: ONP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
May 28, 2015 EMA Eisai Europe Ltd
Feb. 13, 2015 FDA EISAI INC

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients 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

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients 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

Pharmacologic Action:

SourceCodeDescription
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

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Follicular thyroid carcinoma indication 255028004 DOID:3962
Papillary thyroid carcinoma indication 255029007 DOID:3969
Renal cell carcinoma indication 702391001 DOID:4450

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 12.09 acidic
pKa2 12.74 acidic
pKa3 13.02 acidic
pKa4 4.67 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
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)

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA 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

External reference:

IDSource
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

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
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