Lenvatinib

EGFR Inhibitor

DB09078

Approved Indication

Lenvatinib is indicated for the treatment of patients with locally recurrent or metastatic, progressive, radioactive iodine-refractory differentiated thyroid cancer.

8 Targets

0 Resistance Mutations

4 References

3WZD Structure Loaded

3D Structure PDB: 3WZD

Switch structure: RCSB ↗

Protein Targets

FGFR1 P11362 ✓ FGFR2 P21802 ✓ FGFR3 P22607 ✓ FGFR4 P22455 ✓ FLT1 P17948 ✓ FLT4 P35916 ✓ KDR P35968 ✓ 1 PDB KIT P10721 ✓

Mechanism of Action

Lenvatinib is 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). Lenvatinib also inhibits other RTKs that have been implicated in pathogenic angiogenesis, tumor growth, and cancer progression in addition to their normal cellular functions, including fibroblast growth factor (FGF) receptors FGFR1, 2, 3, and 4; the platelet derived growth factor receptor alpha (PDGFRα), KIT, and RET.

Details

DrugBank ID DB09078 ↗

Approval Date 2015-02-13

Molecular Weight 426.86 g/mol

Drug Class EGFR Inhibitor

ATC Codes L01XE29

Synonyms Lenvatinib Mesylate

PubChem CID: 9823820 ↗

ChEMBL CHEMBL1289601 ↗

SMILES

COC1=C(C=C2C(OC3=CC(Cl)=C(NC(O)=NC4CC4)C=C3)=CC=NC2=C1)C(O)=N

ADMET Profile

Computing properties…

Drug References (DrugBank)

PMID:17943726 PMID:21781317 PMID:25707627 PMID:25795101