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ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ANTINEOPLASTIC AGENTS › OTHER ANTINEOPLASTIC AGENTS › Other antineoplastic agents
tazemetostat
L01XX72
Adult Dosing
- 800 mg orally twice daily with or without food
- Continue treatment until disease progression or unacceptable toxicity
Pediatric Dosing
- Safety and efficacy not established in pediatric patients < 16 years
- Epithelioid sarcoma (age >= 16 years): 800 mg orally twice daily
Indications
- Epithelioid sarcoma that is metastatic or locally advanced not eligible for curative resection
- Relapsed or refractory follicular lymphoma with an EZH2 mutation
- Relapsed or refractory follicular lymphoma with no satisfactory alternative treatment options
Mechanism of Action
- Inhibitor of the EZH2 (Enhancer of zeste homolog 2) histone methyltransferase
- Inhibits EZH2 and mutant forms (Y641N, Y641F, Y641S, Y641H, A682G, A677V), leading to decreased H3K27 methylation and transcriptional repression of genes involved in cellular proliferation
Contraindications
- Severe hypersensitivity to tazemetostat or any of its components
Adverse Reactions
- Fatigue
- Nausea
- Musculoskeletal pain
- Vomiting
- Decreased appetite
- Abdominal pain
- Constipation
- Anemia
- Thrombocytopenia
Drug Interactions
- Strong CYP3A inhibitors: Avoid coadministration; if unavoidable, reduce tazemetostat dose to 400 mg twice daily
- Strong CYP3A inducers: Avoid coadministration as it decreases tazemetostat exposure and efficacy
- Moderate CYP3A inducers: Avoid coadministration
- CYP3A substrates: Coadministration with sensitive CYP3A substrates may decrease their efficacy due to enzyme induction
Curated Content: Needs Vetting Before Put to Clinical Use