Difference between revisions of "Belzutifan (Welireg)"
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*[[CNS hemangioblastoma]] | *[[CNS hemangioblastoma]] | ||
*[[Pancreatic NET]] | *[[Pancreatic NET]] | ||
| − | *[[Renal_cell_carcinoma,_VHL-associated|VHL-associated RCC]] | + | *[[Renal cell carcinoma]] |
| + | **[[Renal_cell_carcinoma,_VHL-associated|VHL-associated RCC]] | ||
==History of changes in FDA indication== | ==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|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)'' |
| + | *2023-12-14: Approved for patients with advanced [[Renal cell carcinoma|renal cell carcinoma (RCC)]] following a programmed death receptor-1 (PD-1) or programmed death-ligand 1 (PD-L1) inhibitor and a vascular endothelial growth factor tyrosine kinase inhibitor (VEGF-TKI). ''(Based on LITESPARK-005)'' | ||
| + | |||
| + | ==Also known as== | ||
| + | *'''Code names:''' MK-6482, PT-2977 | ||
| + | *'''Brand name:''' Welireg | ||
[[Category:Drugs]] | [[Category:Drugs]] | ||
Latest revision as of 02:20, 15 December 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)
- 2023-12-14: Approved for patients with advanced renal cell carcinoma (RCC) following a programmed death receptor-1 (PD-1) or programmed death-ligand 1 (PD-L1) inhibitor and a vascular endothelial growth factor tyrosine kinase inhibitor (VEGF-TKI). (Based on LITESPARK-005)
Also known as
- Code names: MK-6482, PT-2977
- Brand name: Welireg