Difference between revisions of "Belzutifan (Welireg)"

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==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 MK-6482-004)''
 
*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)''
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==Also known as==
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*'''Code names:''' MK6482, PT2977
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*'''Brand name:''' Welireg
  
 
[[Category:Drugs]]
 
[[Category:Drugs]]

Revision as of 12:31, 4 December 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

Also known as

  • Code names: MK6482, PT2977
  • Brand name: Welireg