GtoPdb Ligand ID: 7426

Synonyms: E 7080 | ER-203492-00 | Kisplyx® | Lenvima®
lenvatinib is an approved drug (FDA & EMA (2015))
Compound class: Synthetic organic
Comment: Lenvatinib is a potent inhibitor of VEGFR-2 (KDR) and VEGFR-3 (FLT4) [2].
IUPHAR Pharmacology Education Project (PEP) logo

View more information in the IUPHAR Pharmacology Education Project: lenvatinib

2D Structure
Click here for structure editor
Physico-chemical Properties
Hydrogen bond acceptors 6
Hydrogen bond donors 3
Rotatable bonds 8
Topological polar surface area 115.57
Molecular weight 426.11
XLogP 2.47
No. Lipinski's rules broken 0
Canonical SMILES COc1cc2nccc(c2cc1C(=O)N)Oc1ccc(c(c1)Cl)NC(=O)NC1CC1
Isomeric SMILES COc1cc2nccc(c2cc1C(=O)N)Oc1ccc(c(c1)Cl)NC(=O)NC1CC1
InChI InChI=1S/C21H19ClN4O4/c1-29-19-10-17-13(9-14(19)20(23)27)18(6-7-24-17)30-12-4-5-16(15(22)8-12)26-21(28)25-11-2-3-11/h4-11H,2-3H2,1H3,(H2,23,27)(H2,25,26,28)
No information available.
Summary of Clinical Use
Lenvatinib's first approval (in 2015) was for use in treating patients with progressive, differentiated thyroid cancer.
Marketed formulations contain lenvatinib mesylate (PubChem CID 11237762).
In May 2016, the US FDA expanded approval to include treatment (in combination with everolimus) of advanced renal cell carcinoma following one prior anti-angiogenic therapy. FDA approval was further expanded in August 2018 to include use as a first-line treatment for unresectable hepatocellular carcinoma (HCC), based on results from trial NCT01761266 [1]. These results showed that lenvatinib was non-inferior to sorafenib in these patients. In Europe lenvatinib was granted EMA orphan designation as an HCC therapy in 2015.
Visit ClinicalTrials.gov to view currently registered drug trials assessing lenvatinib's effectiveness in treating additional types of cancer.
Mechanism Of Action and Pharmacodynamic Effects
Lenvatinib is an inhibitor of all three VEGFR tyrosine kinases [2]. Inhibits vascular endothelial growth factor (VEGF)-stimulated neo-angiogenesis and may therefore reduce the vascularisation which underpins and supports tumour development and growth.
Clinical Trials
Clinical Trial ID Title Type Source Comment References
NCT01761266 A Multicenter, Open-Label, Phase 3 Trial to Compare the Efficacy and Safety of Lenvatinib (E7080) Versus Sorafenib in First-line Treatment of Participants With Unresectable Hepatocellular Carcinoma Phase 3 Interventional Eisai Inc.
External links