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 1111.91 60.19 295 1432 27066 2329292
Malignant neoplasm progression 832.26 60.19 200 1527 11928 2344430
Decreased appetite 629.86 60.19 193 1534 28698 2327660
Proteinuria 541.90 60.19 109 1618 2741 2353617
Diarrhoea 400.84 60.19 184 1543 83380 2272978
Palmar-plantar erythrodysaesthesia syndrome 389.54 60.19 89 1638 4112 2352246
Hepatic encephalopathy 284.12 60.19 58 1669 1549 2354809
Fatigue 279.25 60.19 145 1582 84728 2271630
Platelet count decreased 248.47 60.19 83 1644 15730 2340628
Vomiting 211.02 60.19 114 1613 71488 2284870
Nausea 195.26 60.19 127 1600 112062 2244296
Stomatitis 176.47 60.19 57 1670 9653 2346705
Malaise 159.02 60.19 87 1640 55498 2300860
Blood pressure increased 156.00 60.19 60 1667 16926 2339432
Hypothyroidism 113.82 60.19 34 1693 4423 2351935
Cholecystitis 112.22 60.19 29 1698 2211 2354147
Dehydration 107.94 60.19 50 1677 22245 2334113
Tumour haemorrhage 106.69 60.19 20 1707 334 2356024
Ascites 101.95 60.19 33 1694 5587 2350771
Weight decreased 99.39 60.19 51 1676 28320 2328038
Pyrexia 88.09 60.19 59 1668 53649 2302709
Pneumothorax 87.58 60.19 24 1703 2288 2354070
Abdominal pain 87.48 60.19 50 1677 34324 2322034
Arterial haemorrhage 84.32 60.19 15 1712 184 2356174
Asthenia 82.84 60.19 54 1673 46872 2309486
Oral pain 74.22 60.19 23 1704 3374 2352984
Tracheal fistula 74.15 60.19 10 1717 12 2356346
Epistaxis 70.23 60.19 29 1698 9750 2346608
Pneumonia 68.60 60.19 49 1678 49247 2307111
Hepatic function abnormal 68.41 60.19 25 1702 6067 2350291
Fistula 61.59 60.19 17 1710 1662 2354696
Headache 61.07 60.19 56 1671 80123 2276235

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 1056.84 56.10 343 2381 23528 1720529
Malignant neoplasm progression 885.95 56.10 266 2458 13892 1730165
Diarrhoea 784.71 56.10 343 2381 53509 1690548
Hypertension 730.54 56.10 248 2476 19200 1724857
Hepatic encephalopathy 626.74 56.10 140 2584 2152 1741905
Proteinuria 586.12 56.10 138 2586 2706 1741351
Fatigue 530.36 56.10 258 2466 50523 1693534
Palmar-plantar erythrodysaesthesia syndrome 404.52 56.10 107 2617 3400 1740657
Malaise 299.31 56.10 148 2576 29417 1714640
Blood pressure increased 293.83 56.10 109 2615 10644 1733413
Hypothyroidism 238.00 56.10 66 2658 2494 1741563
Dehydration 219.39 56.10 102 2622 17556 1726501
Nausea 196.99 56.10 137 2587 51059 1692998
Weight decreased 189.11 56.10 100 2624 22653 1721404
Dysphonia 182.87 56.10 58 2666 3497 1740560
Pyrexia 168.53 56.10 120 2604 46280 1697777
Vomiting 150.35 56.10 104 2620 38211 1705846
Stomatitis 147.95 56.10 55 2669 5349 1738708
Platelet count decreased 138.08 56.10 73 2651 16450 1727607
Tumour haemorrhage 134.08 56.10 31 2693 548 1743509
Ascites 128.21 56.10 50 2674 5536 1738521
Epistaxis 125.06 56.10 55 2669 8251 1735806
Ammonia increased 122.11 56.10 31 2693 823 1743234
Hepatic failure 122.05 56.10 49 2675 5854 1738203
Asthenia 112.59 56.10 84 2640 34586 1709471
Oesophageal varices haemorrhage 108.15 56.10 26 2698 547 1743510
Cholecystitis 98.92 56.10 30 2694 1550 1742507
Pneumonia 97.38 56.10 87 2637 46095 1697962
Hepatic function abnormal 97.32 56.10 44 2680 7030 1737027
Renal cancer 96.08 56.10 27 2697 1064 1742993
Blood thyroid stimulating hormone increased 95.32 56.10 24 2700 615 1743442
Liver carcinoma ruptured 93.02 56.10 16 2708 51 1744006
Pneumothorax 90.57 56.10 32 2692 2680 1741377
Death 89.67 56.10 112 2612 87331 1656726
Abdominal pain 85.49 56.10 59 2665 21431 1722626
Oral pain 84.60 56.10 26 2698 1404 1742653
Blood bilirubin increased 74.06 56.10 35 2689 6175 1737882
Constipation 71.20 56.10 46 2678 14954 1729103
C-reactive protein increased 66.60 56.10 32 2692 5853 1738204
Dyspnoea 65.15 56.10 74 2650 51985 1692072
Aspartate aminotransferase increased 63.72 56.10 38 2686 10718 1733339
Cholangitis 63.52 56.10 20 2704 1169 1742888
Rash 60.64 56.10 62 2662 38631 1705426

Pharmacologic Action:

SourceCodeDescription
ATC L01XE29 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
OTHER ANTINEOPLASTIC AGENTS
Protein kinase inhibitors
CHEBI has role CHEBI:71031 orphan drug
CHEBI has role CHEBI:35610 antineoplastic agent
MeSH PA D000970 Antineoplastic Agents
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D047428 Protein Kinase Inhibitors
FDA EPC N0000175605 Kinase Inhibitor
FDA MoA N0000020000 Receptor Tyrosine Kinase Inhibitors

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)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 10MG BASE LENVIMA EISAI INC N206947 Feb. 13, 2015 RX CAPSULE ORAL 9006256 July 27, 2027 METHOD FOR TREATING THYROID CARCINOMA INCLUDING DIFFERENTIATED THYROID CANCER
EQ 4MG BASE LENVIMA EISAI INC N206947 Feb. 13, 2015 RX CAPSULE ORAL 9006256 July 27, 2027 METHOD FOR TREATING THYROID CARCINOMA INCLUDING DIFFERENTIATED THYROID CANCER

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 Feb. 13, 2020 NEW CHEMICAL ENTITY
EQ 4MG BASE LENVIMA EISAI INC N206947 Feb. 13, 2015 RX CAPSULE ORAL Feb. 13, 2020 NEW CHEMICAL ENTITY
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
C2986924 UMLSCUI
3J78384F61 UNII
857890-39-2 SECONDARY_CAS_RN
714109005 SNOMEDCT_US
1603296 RXNORM
015899 NDDF
4034239 VANDF
d08346 MMSL
714108002 SNOMEDCT_US
9823820 PUBCHEM_CID
CHEBI:85994 CHEBI
9361 INN_ID
LEV PDB_CHEM_ID
DB09078 DRUGBANK_ID
CHEMBL1289601 ChEMBL_ID
CHEMBL2105704 ChEMBL_ID
7426 IUPHAR_LIGAND_ID
C531958 MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Lenvima HUMAN PRESCRIPTION DRUG LABEL 1 62856-704 CAPSULE 4 mg ORAL NDA 18 sections
Lenvima HUMAN PRESCRIPTION DRUG LABEL 1 62856-708 CAPSULE 4 mg ORAL NDA 18 sections
Lenvima HUMAN PRESCRIPTION DRUG LABEL 1 62856-710 CAPSULE 10 mg ORAL NDA 18 sections
Lenvima HUMAN PRESCRIPTION DRUG LABEL 1 62856-712 CAPSULE 4 mg ORAL NDA 18 sections
Lenvima HUMAN PRESCRIPTION DRUG LABEL 2 62856-714 KIT 10 mg None NDA 18 sections
Lenvima HUMAN PRESCRIPTION DRUG LABEL 2 62856-714 KIT 4 mg None NDA 18 sections
Lenvima HUMAN PRESCRIPTION DRUG LABEL 2 62856-718 KIT 4 mg None NDA 18 sections
Lenvima HUMAN PRESCRIPTION DRUG LABEL 2 62856-718 KIT 10 mg None NDA 18 sections
Lenvima HUMAN PRESCRIPTION DRUG LABEL 1 62856-720 CAPSULE 10 mg ORAL NDA 18 sections
Lenvima HUMAN PRESCRIPTION DRUG LABEL 2 62856-724 KIT 10 mg None NDA 18 sections
Lenvima HUMAN PRESCRIPTION DRUG LABEL 2 62856-724 KIT 4 mg None NDA 18 sections