Revuforj/revumenib

Revuforj/revumenib

[Indications] Revuforj is a menin inhibitor targeting the lysine methyltransferase 2A gene (KMT2A) translocation, specifically designed for the treatment of adult and pediatric patients aged 1 and above with relapsed or refractory acute leukemia. This gene translocation is associated with the aggressive characteristics of acute leukemia, and Revuforj exerts its anticancer effect by specifically inhibiting the interaction between menin and KMT2A.

[Mechanism of Action] Revumenib is a methyltransferase inhibitor that interferes with the activation pathway of leukemia genes by blocking the binding of lysine methyltransferase 2A (KMT2A) wild-type and KMT2A fusion proteins to methyltransferase. The binding of KMT2A fusion proteins to methyltransferase plays a crucial role in KMT2A rearrangement (KMT2Ar) acute leukemia. Non-clinical studies have shown that Revumenib can alter the transcription of multiple genes, including differentiation markers, by inhibiting this interaction. Furthermore, in both in vitro and in vivo experiments, Revumenib exhibits anti-proliferative and anti-tumor activity against leukemia cells carrying KMT2A fusion proteins.

[Drug specification] Tablets, 30 tablets/bottle, available in three specifications: 25mg, 110mg, and 160mg.

[Side Effects] The most common adverse reactions (≥20%) include laboratory abnormalities, such as bleeding, nausea, elevated phosphate levels, musculoskeletal pain, infection, elevated aspartate aminotransferase, febrile neutropenia, elevated alanine aminotransferase, unimpaired elevation of parathyroid hormone, bacterial infection, diarrhea, differentiation syndrome, QT prolongation on electrocardiogram, decreased phosphate levels, elevated triglyceride levels, decreased potassium levels, decreased appetite, constipation, edema, viral infection, fatigue, and elevated alkaline phosphatase.

[Dosage and Administration] • Patients should be selected for Revuforj treatment based on the presence of the KMT2A translocation. • Revuforj should be taken orally twice daily, either with or without food, or with a low-fat meal at approximately the same time each day. • For recommended dosage regimens, dosage adjustments, and administration instructions for Revuforj, please refer to the complete prescribing information.