Revumenib
NA
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Drug Status
Government Approvals
US(FDA)
WHO Essential Medicine
NO
Known Teratogen
No
Pharmaceutical Class
NA
Controlled Drug Substance
No
Revumenib
Summary
Revumenib is used to treat a type of blood cancer known as acute leukemia that has returned or has not responded to previous treatments. It is specifically used when the leukemia has a genetic change known as a KMT2A translocation. It can be used in adults and children aged 1 year and older.
Revumenib works by blocking the interaction of certain proteins in the body called KMT2A fusion proteins with a protein called menin. This interaction is involved in the development of leukemia. By blocking it, Revumenib alters the way genes are read by the cells, encouraging the leukemia cells to mature and stop growing.
Revumenib is taken orally, twice daily. The dose depends on your weight and whether you are taking certain other medicines. For those weighing 40 kg or more, the dose is 270 mg without certain other medicines, and 160 mg with them. For those under 40 kg, the dose is calculated based on body surface area.
Common side effects of Revumenib include nausea, diarrhea, fatigue, and decreased appetite. More serious side effects can include a condition called differentiation syndrome, heart rhythm changes, and a decrease in white blood cells that fight infection.
Revumenib can cause serious side effects, including differentiation syndrome and changes in heart rhythm. It can also harm an unborn baby, so effective contraception is necessary for both males and females of reproductive potential. Caution is advised in patients with heart conditions or electrolyte imbalances.
Indications and Purpose
How does Revumenib work?
Revumenib is a menin inhibitor that blocks the interaction of KMT2A fusion proteins with menin. This interaction is involved in the development of KMT2A-rearranged acute leukemias. By inhibiting this interaction, Revumenib alters gene transcription, promoting cell differentiation and reducing the proliferation of leukemia cells.
Is Revumenib effective?
Revumenib's effectiveness was evaluated in a clinical trial involving patients with relapsed or refractory acute leukemia with a KMT2A translocation. The trial showed a complete remission (CR) or CR with partial hematologic recovery (CRh) in 21% of patients. The median duration of CR+CRh was 6.4 months. These results demonstrate Revumenib's potential to induce remission in this patient population.
What is Revumenib?
Revumenib is used to treat relapsed or refractory acute leukemia with a KMT2A translocation in patients 1 year and older. It works by inhibiting the interaction of KMT2A fusion proteins with menin, which is involved in leukemia development. This inhibition alters gene transcription, promoting differentiation and reducing leukemia cell proliferation.
Directions for Use
For how long do I take Revumenib?
Revumenib is typically used until disease progression or unacceptable toxicity occurs. For patients without disease progression or unacceptable toxicity, treatment should continue for a minimum of 6 months to allow time for a clinical response.
How do I take Revumenib?
Revumenib should be taken twice daily, either fasted or with a low-fat meal. It is important to take the medication at the same time each day, approximately 12 hours apart. Swallow the tablets whole with water, and do not cut or chew them. If you miss a dose, take it as soon as possible, ensuring there is at least 12 hours before the next dose.
How long does it take for Revumenib to start working?
The median time to achieve complete remission (CR) or CR with partial hematologic recovery (CRh) with Revumenib is approximately 1.9 months. However, the time it takes for the medication to start working can vary depending on individual patient factors and the severity of the condition.
How should I store Revumenib?
Store Revumenib tablets at room temperature, between 68°F to 77°F (20°C to 25°C). Keep the tablets in their original container with a desiccant and child-resistant closure until you are ready to take them. Ensure the medication is kept out of reach of children to prevent accidental ingestion.
What is the usual dose of Revumenib?
The usual daily dose of Revumenib for adults and children 1 year and older is based on weight and the use of strong CYP3A4 inhibitors. For those weighing 40 kg or more, the dose is 270 mg orally twice daily without strong CYP3A4 inhibitors, and 160 mg orally twice daily with them. For those under 40 kg, the dose is 160 mg/m2 orally twice daily without strong CYP3A4 inhibitors, and 95 mg/m2 orally twice daily with them.
Warnings and Precautions
Can I take Revumenib with other prescription drugs?
Revumenib is primarily metabolized by CYP3A4, so strong CYP3A4 inhibitors can increase its systemic exposure, potentially leading to increased side effects. Conversely, strong or moderate CYP3A4 inducers may decrease its effectiveness. Additionally, drugs that prolong the QTc interval should be avoided as they can increase the risk of QTc prolongation when used with Revumenib.
Can Revumenib be taken safely while breastfeeding?
There is no data on the presence of Revumenib in human milk or its effects on the breastfed child. Due to the potential for serious adverse reactions in a breastfed child, women are advised not to breastfeed during treatment with Revumenib and for 1 week after the last dose.
Can Revumenib be taken safely while pregnant?
Revumenib can cause fetal harm based on animal studies, and there is no available data from human studies. Pregnant women should be advised of the potential risk to the fetus. Females of reproductive potential should use effective contraception during treatment and for 4 months after the last dose. Males with female partners of reproductive potential should also use effective contraception during this period.
Is Revumenib safe for the elderly?
In elderly patients, the incidence of QTc prolongation and edema is higher. Therefore, it is important to monitor these patients closely for these side effects. Regular ECGs and electrolyte monitoring are recommended to manage any potential risks. Elderly patients should also be informed about the signs of differentiation syndrome and advised to report any symptoms immediately.
Who should avoid taking Revumenib?
Revumenib can cause differentiation syndrome, which may be life-threatening. Symptoms include fever, dyspnea, and rapid weight gain. QTc interval prolongation is another risk, requiring regular ECG monitoring. Revumenib can also harm a fetus, so effective contraception is necessary for both males and females of reproductive potential. There are no specific contraindications, but caution is advised in patients with heart conditions or electrolyte imbalances.
