Difference between revisions of "Belzutifan (Welireg)"
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(Created page with "==Mechanism of action== From the [https://www.cancer.gov/publications/dictionaries/cancer-drug/def/belzutifan NCI Drug Dictionary]: An orally active, small molecule inhibitor...") |
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*[[CNS hemangioblastoma]] | *[[CNS hemangioblastoma]] | ||
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==History of changes in FDA indication== | ==History of changes in FDA indication== | ||
Revision as of 16:21, 16 August 2021
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 Study 004)