belzutifan + metformin

Belzutifan + metformin is an investigational combination of two orally administered small molecules: belzutifan, a hypoxia-inducible factor 2 alpha (HIF-2α) inhibitor, and metformin, an antihyperglycemic agent that reduces hepatic glucose production and increases insulin sensitivity. The combination is currently being studied for potential drug–drug interactions, specifically to determine how belzutifan affects the pharmacokinetics of metformin in healthy adults. - Belzutifan selectively inhibits HIF-2α, thereby blocking its dimerization with HIF-1β, suppressing transcription of genes involved in tumor proliferation and angiogenesis. It is FDA-approved for von Hippel-Lindau (VHL) disease-associated cancers and advanced renal cell carcinoma. - Metformin acts primarily by inhibiting mitochondrial respiratory chain complex I, decreasing hepatic gluconeogenesis, and improving peripheral insulin sensitivity. It is FDA-approved for type 2 diabetes mellitus but is also being investigated for oncology indications. This combination currently has no established therapeutic indication; its primary study focus is pharmacokinetic interaction.

Other names

belzutifan + metforminMK-6482 + metforminWelireg + metformin