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Synonyms: compound 2 [PMID: 31282155] | MK-6482 | MK6482 | PT2977 | Welireg®
belzutifan is an approved drug (FDA (2021))
Compound class: Synthetic organic
Comment: Belzutifan (previously PT2977 and MK-6482) binds to and inhibits HIF-2α function, and has been developed as a novel cancer therapeutic . HIF-2α is a transcription factor component that is established as an oncogneic driver of ccRCC, via loss of its interaction with the tumour suppressor von Hippel-Lindau (VHL), which results in disrupted proteasomal degradation and thereby accumulation of HIF-2α. Elevated HIF-2α promotes increased expression of hypoxia-responsive genes which regulate processes including angiogenesis, proliferation, migration, and immune evasion.
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
1. Choueiri TK, Bauer TM, Papadopoulos KP, Plimack ER, Merchan JR, McDermott DF, Michaelson MD, Appleman LJ, Thamake S, Perini RF et al.. (2021)
Inhibition of hypoxia-inducible factor-2α in renal cell carcinoma with belzutifan: a phase 1 trial and biomarker analysis.
Nat Med, 27 (5): 802-805. [PMID:33888901]
2. Hasanov E, Jonasch E. (2021)
MK-6482 as a potential treatment for von Hippel-Lindau disease-associated clear cell renal cell carcinoma.
Expert Opin Investig Drugs, 30 (5): 495-504. [PMID:33945366]
3. Xu R, Wang K, Rizzi JP, Huang H, Grina JA, Schlachter ST, Wang B, Wehn PM, Yang H, Dixon DD et al.. (2019)
3-[(1S,2S,3R)-2,3-Difluoro-1-hydroxy-7-methylsulfonylindan-4-yl]oxy-5-fluorobenzonitrile (PT2977), a Hypoxia-Inducible Factor 2α (HIF-2α) Inhibitor for the Treatment of Clear Cell Renal Cell Carcinoma.
J Med Chem, 62 (15): 6876-6893. [PMID:31282155]
The HIF2α Inhibitor Belzutifan Shows Signs of Efficacy in Kidney Cancer.
Cancer Discov, 11 (6): 1319. [PMID:33931436]