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ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ANTINEOPLASTIC AGENTS › OTHER ANTINEOPLASTIC AGENTS › Other antineoplastic agents
revumenib
L01XX87
Forms & Strengths
- Oral tablets: 110 mg
- Oral tablets: 160 mg
Adult Dosing
- Relapsed or refractory acute leukemia with KMT2A translocation: 160 mg orally twice daily with or without food until disease progression or unacceptable toxicity
- Administer with strong or moderate CYP3A4 inhibitors with caution, reduce dose as clinically indicated per prescribing guidelines
Pediatric Dosing
- Pediatric patients 1 year and older with relapsed or refractory KMT2A-rearranged acute leukemia: 160 mg/m² orally twice daily (dose adjusted by body surface area)
- Safety and efficacy in pediatric patients under 1 year have not been established
Indications
- Treatment of relapsed or refractory acute leukemia with a lysine methyltransferase 2A (KMT2A) gene translocation in adult and pediatric patients 1 year and older
Mechanism of Action
- Selective, small-molecule inhibitor of the menin-KMT2A protein-protein interaction
- Blocks the interaction between menin and KMT2A fusion proteins, downregulating downstream leukemogenic target genes (such as HOXA9 and MEIS1) and inducing differentiation and apoptosis in KMT2A-rearranged leukemia cells
Contraindications
- Hypersensitivity to revumenib or any of its excipients
Adverse Reactions
- Differentiation syndrome
- QTc interval prolongation
- Hemorrhage
- Nausea and vomiting
- Increased musculoskeletal pain
- Decreased appetite
- Edema
- Fatigue
- Constipation
- Diarrhea
Drug Interactions
- Strong and moderate CYP3A4 inhibitors: May increase revumenib plasma concentrations and toxicity risk
- Strong and moderate CYP3A4 inducers: May decrease revumenib efficacy
- QTc-prolonging drugs: Coadministration may increase the risk of ventricular arrhythmias
Curated Content: Needs Vetting Before Put to Clinical Use