belzutifan

Belzutifan is an oral small molecule inhibitor of hypoxia-inducible factor 2 alpha (HIF-2α), a transcription factor involved in cellular adaptation to hypoxia. By inhibiting HIF-2α, belzutifan blocks its interaction with HIF-1β, reducing the expression of genes that promote tumor growth and angiogenesis. It is primarily indicated for adults with von Hippel-Lindau (VHL) disease who require therapy for associated renal cell carcinoma (RCC), central nervous system hemangioblastomas, or pancreatic neuroendocrine tumors not requiring immediate surgery. Belzutifan is also approved for certain types of advanced RCC following prior treatment with PD-1/PD-L1 and VEGF inhibitors. Developed by Merck & Co., it was first approved in the United States in August 2021 as the first-in-class HIF-2α inhibitor[4][5][6][8].

Brand names

Welireg

Other names

belzutifan