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belzutifan + lenvatinib + pembrolizumab
- Development stage
- Phase 3
- Lead developer
- Merck
- Modality
- Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
- Administration
- Oral, Intravenous
01
Overview
A novel **three-drug cancer therapy** composed of the small molecule HIF-2α inhibitor **belzutifan**, the VEGF receptor tyrosine kinase inhibitor **lenvatinib**, and the monoclonal antibody checkpoint inhibitor **pembrolizumab**. The regimen combines targeted therapy with immunotherapy: belzutifan blocks hypoxia-inducible factor 2α, reducing tumor adaptation to low oxygen; lenvatinib inhibits VEGF-mediated angiogenesis; pembrolizumab blocks PD-1, enhancing antitumor immune response. It is under study as a first-line treatment for advanced clear cell renal cell carcinoma (ccRCC) and other solid tumors including hepatocellular carcinoma, colorectal cancer, pancreatic ductal adenocarcinoma, biliary tract cancer, endometrial cancer, and esophageal squamous cell carcinoma[1][2][4][5].
- Brand names
- Keytruda (pembrolizumab)Welireg (belzutifan)Lenvima (lenvatinib)
- Other names
- belzutifan + lenvatinib + pembrolizumabpembrolizumab + lenvatinib + belzutifan
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)PDCD1 (Programmed cell death protein 1 receptor)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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