Drug intelligence / Profile preview

lenvatinib + everolimus

Development stage
Phase 3
Lead developer
Eisai
Modality
Small Molecules
Administration
Oral
01

Overview

**Lenvatinib + everolimus** is an oral, two-drug targeted anticancer regimen administered as separate products. Lenvatinib is a multitarget receptor tyrosine kinase inhibitor that blocks VEGFR1-3, FGFR1-4, PDGFRα, KIT, and RET, while everolimus is an allosteric mTORC1 inhibitor that acts through FKBP12 binding. The regimen combines antiangiogenic and antiproliferative mTOR-pathway inhibition and is FDA-approved for adults with advanced renal cell carcinoma following one prior antiangiogenic therapy, at lenvatinib 18 mg plus everolimus 5 mg orally once daily. ([fda.gov](https://www.fda.gov/drugs/resources-information-approved-drugs/lenvatinib-combination-everolimus))

Other names
everolimus + lenvatinibLEN + EVElen/evelenvatinib + everolimuslenvatinib and everolimus
02

Targets

FKBP1AKIT (c-KIT proto-oncogene receptor tyrosine kinase)PDGFRA (Platelet-derived growth factor receptor alpha)PDGFRB (Platelet-derived growth factor receptor beta)RET (Rearranged during transfection receptor tyrosine kinase)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR2 (Vascular endothelial growth factor receptor 2)VEGFR4 (Vascular endothelial growth factor Receptor-3)Mechanistic target of rapamycin complex 1FGFR1 (Fibroblast growth factor receptor 1)FGFR2 (Keratinocyte growth factor receptor)FGFR3 (Fibroblast growth factor receptor 3)FGFR4 (Fibroblast growth factor receptor 4)

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