Difference between revisions of "Belzutifan (Welireg)"
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==Also known as== | ==Also known as== | ||
| − | *'''Code names:''' | + | *'''Code names:''' MK-6482, PT-2977 |
*'''Brand name:''' Welireg | *'''Brand name:''' Welireg | ||
Revision as of 01:27, 28 July 2023
Mechanism of action
From the NCI Drug Dictionary: 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.
Diseases for which it is used
History of changes in FDA indication
- 2021-08-13: Approved for adult patients with von Hippel-Lindau (VHL) disease who require therapy for associated renal cell carcinoma (RCC), central nervous system (CNS) hemangioblastomas, or pancreatic neuroendocrine tumors (pNET), not requiring immediate surgery. (Based on MK-6482-004)
Also known as
- Code names: MK-6482, PT-2977
- Brand name: Welireg