| Identification | Back Directory | [Name]
Benzonitrile, 3-[[(1S,2S,3R)-2,3-difluoro-2,3-dihydro-1-hydroxy-7-(methylsulfonyl)-1H-inden-4-yl]oxy]-5-fluoro- | [CAS]
1672668-24-4 | [Synonyms]
PT2977
MK-6482
Belzutifan
PT2977 (MK-6482)
Belzutifan (MK-6482)
Belzutifan (PT2977, MK-6482)
Benzonitrile, 3-[[(1S,2S,3R)-2,3-difluoro-2,3-dihydro-1-hydroxy-7-(methylsulfonyl)-1H-inden-4-yl]oxy]-5-fluoro- | [Molecular Formula]
C17H12F3NO4S | [MDL Number]
MFCD32197212 | [MOL File]
1672668-24-4.mol | [Molecular Weight]
383.34 |
| Chemical Properties | Back Directory | [Boiling point ]
505.8±50.0 °C(Predicted) | [density ]
1.56±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C, stored under nitrogen | [solubility ]
DMSO: 50 mg/mL (130.43 mM) | [form ]
Solid | [pka]
11.66±0.60(Predicted) | [color ]
White to light yellow |
| Hazard Information | Back Directory | [Description]
Belzutifan is an orally active, small molecule inhibitor of hypoxia inducible factor (HIF)-2alpha (HIF-2a), with potential antineoplastic activity. The HIF-2α protein was a key player in the growth of certain cancers. 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.
| [Uses]
Belzutifan is a prescription medicine used to treat adults with von Hippel-Lindau (VHL) disease who need treatment for a type of kidney cancer called renal cell carcinoma (RCC), tumors in the brain and spinal cord called central nervous system hemangioblastomas, or a type of pancreatic cancer called pancreatic neuroendocrine tumors, that do not need surgery right away. | [Indications]
Belzutifan is indicated for the treatment of 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), who do not require immediate surgery. | [Mechanism of action]
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. | [Pharmacokinetics]
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. HIF-2alpha, the alpha subunit for the heterodimeric transcription factor HIF-2, is overexpressed in many cancers and promotes tumorigenesis. | [Side effects]
Side effects ofBelzutifan that was reported:
allergic reactions(skin rash,itchingorhives; swelling of the face, lips, or tongue)
blurred vision OR changes in vision
high blood sugar (increased hunger, thirst or urination; unusually weak or tired, blurry vision)
infection (fever, chills,cough,sore throat,pain;or trouble passing urine)
low calcium levels(fast heartbeat; muscle cramps or;pain;;pain, tingling, or numbness in the hands or feet; seizures)
low red blood cell counts (feeling faint; lightheaded, falls; unusually weak or tired)
trouble breathing
trouble passing urine or change in the amount of urine |
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