Revuforj (revumenib) is a novel menin inhibitor that received approval from the U.S. Food and Drug Administration (FDA) in 2024 for the treatment of relapsed or refractory acute leukemia (in adults and pediatric patients aged ≥1 year) harboring KMT2A gene translocation.
How to Use Revuforj (Revumenib)
Pre-Treatment Preparation
Patient Screening: Confirmation of KMT2A translocation via bone marrow cell testing is required. Additionally, the white blood cell (WBC) count must be reduced to <25 Gi/L prior to treatment initiation.
Dosage Form Selection: Three tablet strengths are available: 25 mg (pink), 110 mg (beige), and 160 mg (purple). The appropriate combination should be selected based on the patient’s body weight and the use of CYP3A4 inhibitors.
Administration Regimen
Patients ≥40 kg: 270 mg orally twice daily (when not co-administered with strong CYP3A4 inhibitors) or 160 mg twice daily (when co-administered with strong CYP3A4 inhibitors).
Patients <40 kg: Dosage is calculated based on body surface area (BSA), at either 160 mg/m² or 95 mg/m².
Administration Method: Swallow the tablets whole either on an empty stomach or after a low-fat meal (≤400 calories, with fat accounting for ≤25% of total calories). If swallowing is not possible, crush the tablets and mix with water, then administer the mixture within 2 hours.
Treatment Course: Continue treatment until disease progression or the occurrence of intolerable toxicity. For patients with no disease progression, treatment should last for at least 6 months.
Management of Missed Doses
If a dose is missed, administer the missed dose as soon as possible on the same day, ensuring a minimum interval of ≥12 hours before the next scheduled dose.
Do not administer a double dose within a 12-hour period.
Dose Adjustments for Revuforj (Revumenib)
Adjustments Due to Adverse Reactions
Differentiation Syndrome (DS): If symptoms such as fever or dyspnea occur, promptly administer intravenous glucocorticoids (e.g., dexamethasone) and suspend Revuforj treatment. Resume the original dose once symptoms improve to ≤ Grade 1.
QT Interval Prolongation: Discontinue administration if QTc > 480 ms; resume treatment after correcting hypokalemia/hypomagnesemia. Permanent discontinuation is required if QTc > 500 ms or if arrhythmic symptoms are present.
Other ≥ Grade 3 Toxicities:
For the first occurrence: Suspend treatment until toxicity resolves to ≤ Grade 1, then resume at the original dose.
For recurrent occurrences: Reduce the dose (e.g., for patients ≥40 kg, reduce from 270 mg to 160 mg).
Adjustments Due to Drug Interactions
Strong CYP3A4 Inhibitors (e.g., posaconazole): Reduce the Revuforj dose by approximately 40%.
Strong/Moderate CYP3A4 Inducers (e.g., rifampicin): Co-administration is prohibited.
QT-Prolonging Drugs (e.g., fluoroquinolones): Avoid co-administration if possible; if necessary, enhance electrocardiogram (ECG) monitoring.
Revuforj (Revumenib) Use in Special Populations
Patients with Hepatic/Renal Impairment
No dose adjustment is required for mild to moderate impairment. Limited data are available for severe impairment, so caution is advised.
No clear dosage recommendations are available for patients undergoing dialysis.
Pediatric Patients
Efficacy has been demonstrated in pediatric patients aged ≥1 year, with dosing based on BSA.
No data are available for infants aged <1 year, so use is contraindicated in this population. Monitor bone development (animal studies have shown a risk of growth plate closure).
Pregnant and Lactating Patients
Pregnancy: Revuforj has embryo-fetal toxicity. Confirm a negative pregnancy test before initiating treatment. Effective contraception is required during treatment and for 4 months after discontinuing the drug.
Lactation: Breastfeeding is prohibited during treatment and for 1 week after the last dose of Revuforj.
