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Drug intelligence / Profile preview
MK-3795 + cabozantinib
- Development stage
- Phase 1
- Lead developer
- Merck
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
MK-3795 + cabozantinib is an investigational combination therapy for cancer, specifically studied in advanced clear cell renal cell carcinoma (ccRCC). MK-3795, previously known as PT2385, is a first-generation small molecule inhibitor of hypoxia-inducible factor-2α (HIF-2α), a transcription factor implicated in the pathogenesis of ccRCC due to frequent loss-of-function mutations in the VHL gene. By inhibiting HIF-2α, MK-3795 disrupts expression of genes promoting tumor growth and angiogenesis. Cabozantinib is an approved multikinase inhibitor targeting receptors involved in tumor growth and angiogenesis, including MET, VEGFR, and AXL. The combination seeks to simultaneously target both the hypoxic response and angiogenic signaling in ccRCC to enhance antitumor efficacy.
- Other names
- belzutifan precursor + cabozantinib
02
Targets
AXL (AXL receptor tyrosine kinase)VEGFR-1 (Vascular endothelial growth factor receptor 1)EPAS1 (Hypoxia-inducible factor 2-alpha)KIT (c-KIT proto-oncogene receptor tyrosine kinase)MET (Mesenchymal-epithelial transition factor receptor)RET (Rearranged during transfection receptor tyrosine kinase)ROS1 (Proto-oncogene tyrosine-protein kinase ROS)TEK (Angiopoietin-1 receptor)NTRK2 (Tropomyosin-related kinase receptor type B)VEGFR2 (Vascular endothelial growth factor receptor 2)
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