Enasidenib
Indications
Enasidenib is used for:
Acute Myeloid Leukemia
Adult Dose
Acute Myeloid Leukemia
Indicated for relapsed/refractory acute myeloid leukemia (AML) with an isocitrate dehydrogenase-2 (IDH2) mutation as detected by an FDA-approved test
100 mg PO qDay with or without food until disease progression or unacceptable toxicity
Child Dose
Renal Dose
Administration
Take once at the same time each day; may be taken with or without food
Contra Indications
Precautions
Differentiation syndrome reported, which can be fatal if not treated
Based on animal embryofetal toxicity studies, can cause embryofetal harm when administered to pregnant women
Pregnancy-Lactation
Pregnancy
Based on animal embryofetal toxicity studies, can cause fetal harm when administered to pregnant women
There are no available data on use in pregnant women to inform a drug-associated risk of major birth defects and miscarriage
Contraception
Females
Females of reproductive potential should avoid becoming pregnant while receiving enasidenib
Advise women to use effective contraception during treatment with enasidenib and for at least 1 month after the last dose
Coadministration of enasidenib may increase or decrease the concentrations of combined hormonal contraceptives; the clinical significance of this potential drug interaction is unknown at this time
Males
Advise males with female partners of reproductive potential to use effective contraception during treatment with enasidenib and for at least 1 month after the last dose
Lactation
There are no data on the presence of enasidenib or its metabolites in human milk, the effects on the breastfed infant, or the effects on milk production
Because many drugs are excreted in human milk and because of the potential for adverse reactions in breastfed infants, advise women not to breastfeed during treatment with enasidenib and for at least 1 month after the last dose
Interactions
Side Effects
Side effects of Enasidenib :
>10%
Total bilirubin increased, all grades (81%)
Calcium decreased, all grades (74%)
Nausea, all grades (50%)
Diarrhea, all grades (43%)
Potassium decreased, all grades (41%)
Vomiting, all grades (34%)
Decreased appetite, all grades (34%)
Phosphorus decreased, all grades (27%)
Total bilirubin increased, grade ≥3 (15%)
Potassium decreased, grade ≥3 (15%)
Differentiation syndrome, all grades (14%)
Noninfectious leukocytosis, all grades (12%)
Dysgeusia, all grades (12%)
1-10%
Pulmonary edema (≤10%)
Acute respiratory distress syndrome (≤10%)
Diarrhea, grade ≥3 (8%)
Calcium decreased, grade ≥3 (8%)
Phosphorus decreased, grade ≥3 (8%)
Differentiation syndrome, grade ≥3 (7%)
Noninfectious leukocytosis, grade ≥3 (6%)
Tumor lysis syndrome, grade ≥3 (6%)
Nausea, grade ≥3 (5%)
Vomiting, grade ≥3 (4%)
Decreased appetite, grade ≥3 (4%)
Mode of Action
Oral, reversible, selective isocitrate dehydrogenase-2 enzyme (IDH2) inhibitor; inhibits mutant IDH2 enzyme, which decreases 2-hydroxyglutarate (2-HG) levels and induces myeloid differentiation in vitro
Enasidenib may have clinical activity in IDH2-mutant AML through the reduction of 2-HG levels and the induction of blast differentiation