Belzutifan

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Belzutifan
Belzutifan.png
Clinical data
Pronunciationbell-ZOO-ti-fan
Trade namesWelireg
Other namesMK-6482, PT2977
License data
Routes of
administration		By mouth
Drug classAntineoplastic
ATC code
Legal status
Legal status
Identifiers
  • 3-{[(1S,2S,3R)-2,3-Difluoro-1-hydroxy-7-(methylsulfonyl)-2,3-dihydro-1H-inden-4-yl]oxy}-5-fluorobenzonitrile
CAS Number
  • 1672668-24-4 checkY[KEGG]
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
PDB ligand
Chemical and physical data
FormulaC17H12F3NO4S
Molar mass383.34 g·mol−1
3D model (JSmol)
  • CS(=O)(=O)C1=CC=C(OC2C=C(F)C=C(C=2)C#N)C2[C@@H](F)[C@@H](F)[C@@H](O)C1=2
  • InChI=1S/C17H12F3NO4S/c1-26(23,24)12-3-2-11(13-14(12)17(22)16(20)15(13)19)25-10-5-8(7-21)4-9(18)6-10/h2-6,15-17,22H,1H3/t15-,16-,17+/m1/s1
  • Key:LOMMPXLFBTZENJ-ZACQAIPSSA-N

Belzutifan, sold under the brand name Welireg, is a medication used for the treatment of von Hippel–Lindau disease-associated renal cell carcinoma.[1][2][3][4][5][6] It is taken by mouth.[1]

The most common side effects include decreased hemoglobin, anemia, fatigue, increased creatinine, headache, dizziness, increased glucose, and nausea.[2]

Belzutifan is an hypoxia-inducible factor-2 alpha (HIF-2α) inhibitor.[1][2][7]

Belzutifan is the first drug to be awarded an "innovation passport" from the UK Medicines and Healthcare products Regulatory Agency (MHRA).[8][4] Belzutifan was approved for medical use in the United States in August 2021.[2][9] Belzutifan is the first hypoxia-inducible factor-2 alpha inhibitor therapy approved in the U.S.[9]

Medical uses[]

Belzutifan is indicated for treatment of adults 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.[2] Belzutifan was also found to be efficacious in an adolescent who had Pacak–Zhuang syndrome with polycythemia and paragangliomas.[10]

References[]

  1. ^ a b c d "Welireg- belzutifan tablet, film coated". DailyMed. Retrieved 12 September 2021.
  2. ^ a b c d e f "FDA approves belzutifan for cancers associated with von Hippel-Lindau". U.S. Food and Drug Administration (FDA). 13 August 2021. Retrieved 13 August 2021. Public Domain This article incorporates text from this source, which is in the public domain.
  3. ^ "Belzutifan". SPS - Specialist Pharmacy Service. 18 March 2021. Retrieved 25 April 2021.
  4. ^ a b "MHRA awards first 'innovation passport' under new pathway". RAPS (Press release). Retrieved 25 April 2021.
  5. ^ "Merck Receives Priority Review From FDA for New Drug Application for HIF-2α Inhibitor Belzutifan (MK-6482)" (Press release). Merck. 16 March 2016. Retrieved 25 April 2021 – via Business Wire.
  6. ^ "FDA Grants Priority Review to Belzutifan for von Hippel-Lindau Disease–Associated RCC". Cancer Network. Retrieved 26 April 2021.
  7. ^ {{cite journal |vauthors=Choueiri TK, Bauer TM, Papadopoulos KP, Plimack ER, Merchan JR, McDermott DF, Michaelson MD, Appleman LJ, Thamake S, Perini RF, Zojwalla NJ, Jonasch E | display-authors=6 |title=Inhibition of hypoxia-inducible factor-2α in renal cell carcinoma with belzutifan: a phase 1 trial and biomarker analysis |journal=Nat Med |volume= |issue= |pages= |date=April 2021 |pmid=33888901 |doi=10.1038/s41591-021-01324-7 }
  8. ^ "First Innovation Passport awarded to help support development and access to cutting-edge medicines". Medicines and Healthcare products Regulatory Agency (MHRA) (Press release). 26 February 2021. Retrieved 14 August 2021.
  9. ^ a b "FDA Approves Merck's Hypoxia-Inducible Factor-2 Alpha (HIF-2α) Inhibitor Welireg (belzutifan) for the Treatment of Patients With Certain Types of Von Hippel-Lindau (VHL) Disease-Associated Tumors" (Press release). Merck. 13 August 2021. Retrieved 13 August 2021 – via Business Wire.
  10. ^ Kamihara, Junne; Hamilton, Kayla V.; Pollard, Jessica A.; Clinton, Catherine M.; Madden, Jill A.; Lin, Jasmine; Imamovic, Alma; Wall, Catherine B.; Wassner, Ari J.; Weil, Brent R.; Heeney, Matthew M. (25 November 2021). "Belzutifan, a Potent HIF2α Inhibitor, in the Pacak–Zhuang Syndrome". New England Journal of Medicine. 385 (22): 2059–2065. doi:10.1056/NEJMoa2110051. ISSN 0028-4793.

External links[]

  • "Belzutifan". Drug Information Portal. U.S. National Library of Medicine.
  • Clinical trial number NCT04195750 for "A Study of Belzutifan (MK-6482) Versus Everolimus in Participants With Advanced Renal Cell Carcinoma (MK-6482-005)" at ClinicalTrials.gov
  • Clinical trial number NCT03401788 for "A Phase 2 Study of Belzutifan (PT2977, MK-6482) for the Treatment of Von Hippel Lindau (VHL) Disease-Associated Renal Cell Carcinoma (RCC) (MK-6482-004)" at ClinicalTrials.gov


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