Drugs Information:
Belzutifan
Basic Information
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| ID | DDInter2000 | |
| Drug Type | small molecule | |
| Molecular Formula | C17H12F3NO4S | |
| Molecular Weight | 383.340 | |
| CAS Number | 1672668-24-4 | |
| Description | Belzutifan is an inhibitor of hypoxia-inducible factor 2α (HIF-2α) used in the treatment of von Hippel-Lindau (VHL) disease-associated cancers.[L35995] The HIF-2α protein was first identified in the 1990s by researchers at UT Southwestern Medical Center as a key player in the growth of certain cancers.[L36105] Initially considered to be undruggable, a binding pocket was eventually discovered in the HIF-2α molecule which allowed for compounds to bind and inhibit these proteins. This discovery led to the initial development of belzutifan (at the time called PT2977), which was further developed by a spin-off company named Peloton Pharmaceuticals (which itself was eventually acquired by Merck in 2019).[L36105] Belzutifan inhibits the complexation of HIF-2α with another transcription factor, HIF-1β, a necessary step in its activation - by preventing the formation of this complex, belzutifan can slow or stop the growth of VHL-associated tumors. Belzutifan received FDA approval for the treatment of select VHL-associated cancers on August 13, 2021.[L36000] | |
| ATC Classification | L01XX74 | |
| IUPAC Name | 3-{[(1S,2S,3R)-2,3-difluoro-1-hydroxy-7-methanesulfonyl-2,3-dihydro-1H-inden-4-yl]oxy}-5-fluorobenzonitrile | |
| InChI | LOMMPXLFBTZENJ-ZACQAIPSSA-N | |
| Canonical SMILES | CS(=O)(=O)C1=CC=C(OC2=CC(=CC(F)=C2)C#N)C2=C1[C@H](O)[C@H](F)[C@@H]2F | |
| Useful Links | DrugBank ChemSpider BindingDB Wikipedia ChEMBL ZINC | |
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Belzutifan
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