Difference between revisions of "Belzutifan (Welireg)"
Jump to navigation
Jump to search
Warner-admin (talk | contribs) |
|||
| Line 8: | Line 8: | ||
==History of changes in FDA indication== | ==History of changes in FDA indication== | ||
| − | *8/13/2021: Approved for adult patients with von Hippel-Lindau (VHL) disease who require therapy for associated [[Renal cell carcinoma|renal cell carcinoma (RCC)]], [[CNS hemangioblastoma|central nervous system (CNS) hemangioblastomas]], or [[Pancreatic NET|pancreatic neuroendocrine tumors (pNET)]], not requiring immediate surgery. ''(Based on | + | *8/13/2021: Approved for adult patients with von Hippel-Lindau (VHL) disease who require therapy for associated [[Renal cell carcinoma|renal cell carcinoma (RCC)]], [[CNS hemangioblastoma|central nervous system (CNS) hemangioblastomas]], or [[Pancreatic NET|pancreatic neuroendocrine tumors (pNET)]], not requiring immediate surgery. ''(Based on MK-6482-004)'' |
[[Category:Drugs]] | [[Category:Drugs]] | ||
Revision as of 14:59, 17 June 2022
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
- 8/13/2021: 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)