Medical Information

Enasidenib is an IDH2 inhibitor suitable for adult patients with relapsed/refractory acute myeloid leukemia (AML) carrying IDH2 mutations. It should be noted that there are limitations such as liver dysfunction and embryotoxicity, and there is a risk of interaction with drugs such as CYP3A4 substrates and P-glycoprotein inhibitors.

1. Applicable population

(1) Genetic testing confirms the presence of IDH2 mutations (R140 or R172) in adult patients with relapsed/refractory AML.

(2) Not applicable to newly diagnosed AML or IDH2 wild-type patients, safety in children has not been established.

2. Restrictive conditions

(1) Liver function impairment: Moderate to severe impairment (Child Pugh B/C) should be reduced or discontinued, and transaminases should be monitored during treatment.

(2) Pregnancy risk: May cause fetal malformation, confirm pregnancy status before treatment, and take effective contraceptive measures during medication.

(3) Breastfeeding period: Medication may be secreted into breast milk. Breastfeeding is prohibited during treatment and for 2 weeks after discontinuation of medication.

3. Drug interactions

(1) Strong CYP3A4 inducers (such as rifampicin): may reduce the blood concentration of amlodipine and should be avoided in combination.

(2) CYP3A4 substrates (such as midazolam): Ensidipine may increase its exposure and adverse reactions need to be monitored.

(3) P-glycoprotein inhibitors (such as amiodarone): may increase the absorption of amlodipine, it is recommended to adjust the dosage.

4. Special precautions

(1) Differentiation syndrome: Close monitoring of symptoms such as dyspnea/fever is necessary, and medication should be suspended and corticosteroids should be given when it occurs.

(2) Hyperbilirubinemia: Approximately 81% of patients experience it, and usually does not require dose adjustment, but regular monitoring of liver function is necessary.