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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) .
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
View more information in the IUPHAR Pharmacology Education Project: lenvatinib
|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 . 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 . Inhibits vascular endothelial growth factor (VEGF)-stimulated neo-angiogenesis and may therefore reduce the vascularisation which underpins and supports tumour development and growth.|
|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.|
For extended ADME data see the following:
Electronic Medicines Compendium (eMC)
European Medicines Agency (EMA)