Belzutifan

**Semantic type:** Pharmacologic Substance

**Definition:** An orally active, small molecule inhibitor of hypoxia inducible factor (HIF)-2alpha (HIF-2a), with potential antineoplastic activity. Upon oral administration, belzutifan binds to and blocks the function of HIF-2alpha, thereby preventing HIF-2alpha heterodimerization and its subsequent binding to DNA. This results in decreased transcription and expression of HIF-2alpha downstream target genes, many of which regulate hypoxic signaling. This inhibits cell growth and survival of HIF-2alpha-expressing tumor cells. HIF-2alpha, the alpha subunit for the heterodimeric transcription factor HIF-2, is overexpressed in many cancers and promotes tumorigenesis.

**Synonyms:** - BELZUTIFAN - HIF-2alpha Inhibitor PT2977 - MK 6482 - MK-6482 - MK6482 - PT 2977 - PT-2977 - PT2977 - Welireg