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pembrolizumab + belzutifan + lenvatinib
- Development stage
- Unknown
- Lead developer
- Merck
- Modality
- Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
- Administration
- Intravenous, Oral
01
Overview
This is a combination therapy of three agents: pembrolizumab (a humanized monoclonal antibody against PD-1), belzutifan (a small molecule inhibitor of hypoxia-inducible factor 2-alpha, HIF-2α), and lenvatinib (a small molecule multi-kinase inhibitor targeting primarily vascular endothelial growth factor receptors VEGFR1-3, among others). The triplet regimen is under investigation as a first-line treatment for advanced or metastatic clear cell renal cell carcinoma (ccRCC) and other solid tumors, aiming to provide synergistic antitumor effects by engaging immune checkpoint inhibition, anti-angiogenesis, and tumor hypoxia modulation pathways. This combination is being tested in large phase 3 clinical trials for ccRCC and earlier-phase studies in other solid tumors. Merck (MSD) leads the development of both pembrolizumab and belzutifan; lenvatinib is developed by Eisai, often in collaboration with Merck[1][2][4][5][7][9].
- Brand names
- Keytruda (pembrolizumab)Welireg (belzutifan)Lenvima (lenvatinib)
- Other names
- pembrolizumab + belzutifan + lenvatinib
02
Targets
EPAS1 (Hypoxia-inducible factor 2-alpha)FGFR4 (Fibroblast growth factor receptor 4)PDCD1 (Programmed cell death protein 1 receptor)PDGFRA (Platelet-derived growth factor receptor alpha)KIT (c-KIT proto-oncogene receptor tyrosine kinase)VEGFR2 (Vascular endothelial growth factor receptor 2)FGFR3 (Fibroblast growth factor receptor 3)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR3 (Vascular endothelial growth factor receptor 3)FGFR2 (Keratinocyte growth factor receptor)FGFR1 (Fibroblast growth factor receptor 1)RET (Rearranged during transfection receptor tyrosine kinase)
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