Drug intelligence / Profile preview

belzutifan + cabozantinib

Development stage
Unknown
Lead developer
Merck
Modality
Small Molecules
Administration
Oral
01

Overview

Belzutifan + cabozantinib is an oral combination therapy of two small molecule drugs: **belzutifan**, a selective inhibitor of hypoxia-inducible factor 2 alpha (HIF-2α), and **cabozantinib**, a multi-targeted tyrosine kinase inhibitor that blocks vascular endothelial growth factor receptor (VEGFR), c-MET, AXL and multiple other receptor tyrosine kinases. This combination is designed to exert synergistic antitumor effects by simultaneously inhibiting hypoxia-driven signaling (via HIF-2α) and multiple pro-angiogenic and oncogenic kinetics (via MET, AXL, VEGFR, etc.). It is being investigated primarily for the treatment of advanced or metastatic clear cell renal cell carcinoma (ccRCC), and has shown promising response rates and disease control in phase 2 trials, both in treatment-naive and previously treated patients. The regimen is under clinical development, with support from Merck Sharp & Dohme and the National Cancer Institute[1][3][5][6][7].

Brand names
Cabometyx (cabozantinib)belzutifan + cabozantinib
Other names
belzutifan plus cabozantinibHIF-2α inhibitor and TKI combination
02

Targets

AXL (AXL receptor tyrosine kinase)MET (Mesenchymal-epithelial transition factor receptor)EPAS1 (Hypoxia-inducible factor 2-alpha)KIT (c-KIT proto-oncogene receptor tyrosine kinase)TEK (Tie2)VEGFR2 (Vascular endothelial growth factor receptor 2)RET (Rearranged during transfection receptor tyrosine kinase)FLT3 (Fms related receptor tyrosine kinase 3)

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