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belzutifan + lenvatinib
- Development stage
- Phase 3
- Lead developer
- Merck
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Belzutifan + lenvatinib is a combination of two oral small molecule drugs: **belzutifan**, a hypoxia-inducible factor 2 alpha (HIF-2α) inhibitor, and **lenvatinib**, a receptor tyrosine kinase inhibitor that targets multiple kinases involved in tumor angiogenesis, proliferation, and cancer progression. This combination is being investigated for the treatment of advanced clear cell renal cell carcinoma (ccRCC), particularly in patients whose disease has progressed following treatment with PD-1/L1 inhibitors and VEGF tyrosine kinase inhibitors. Belzutifan inhibits HIF-2α, impairing cellular hypoxia response and blocking downstream genes involved in growth and angiogenesis. Lenvatinib inhibits VEGF receptors (VEGFR1-3), FGFR1-4, PDGFRα, KIT, and RET, disrupting angiogenic and proliferative signaling. Clinical trials have demonstrated promising antitumor activity and manageable safety with this combination in ccRCC patients[1][3][5].
- Other names
- belzutifan + lenvatinib
02
Targets
FGFR1 (Fibroblast growth factor receptor 1)FGFR2 (Keratinocyte growth factor receptor)FGFR3 (Fibroblast growth factor receptor 3)FGFR4 (Fibroblast growth factor receptor 4)EPAS1 (Hypoxia-inducible factor 2-alpha)KIT (c-KIT proto-oncogene receptor tyrosine kinase)PDGFRA (Platelet-derived growth factor receptor alpha)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)
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