Belzutifan

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.

Also known as BELZUTIFAN, HIF-2alpha Inhibitor PT2977, MK 6482, MK-6482, MK6482, PT 2977, PT-2977, PT2977, Welireg — per NCIT

Also identified as

• ATC L01XX74 per RXNORM
• NCIT NCIT:C135627 per NCIT
• SCTID 41129411000001102 per RXNORM
• UNII 7K28NB895L per RXNORM

Indications