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ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ANTINEOPLASTIC AGENTS › OTHER ANTINEOPLASTIC AGENTS › Other antineoplastic agents
belzutifan
L01XX74
Adult Dosing
- Von Hippel-Lindau (VHL) disease-associated manifestations: 120 mg orally once daily until disease progression or unacceptable toxicity
Pediatric Dosing
- Safety and effectiveness in pediatric patients have not been established
Indications
- Treatment of adults with Von Hippel-Lindau (VHL) disease who require therapy for associated renal cell carcinoma, central nervous system hemangioblastomas, or pancreatic neuroendocrine tumors, not requiring immediate surgery
Mechanism of Action
- Hypoxia-inducible factor 2 alpha (HIF-2a) inhibitor that binds to HIF-2a and blocks its interaction with HIF-1b, reducing transcription and expression of HIF-2a target genes
Contraindications
- Hypersensitivity to belzutifan or any of its components
- Pregnancy
Adverse Reactions
- Anemia
- Fatigue
- Headache
- Dizziness
- Nausea
- Dyspnea
- Hypoxia
Drug Interactions
- Strong CYP2C19 inducers: Avoid coadministration or manage increased toxicity risk
- Strong CYP3A4 inducers: Avoid coadministration or manage decreased belzutifan exposure
- Uridine diphosphate-glucuronosyltransferase (UGT) 2B17 or CYP2C19 substrates: May alter plasma concentrations
Curated Content: Needs Vetting Before Put to Clinical Use