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Idhifa
enasidenib
Black Box Warnings .
Differentiation Syndrome
occurred in 14% of patients as early as 1 day and up to 5mo after tx start; can be fatal if untreated; if suspected, initiate corticosteroids and hemodynamic monitoring until symptoms resolved; signs/symptoms include fever, dyspnea, acute respiratory distress, pulmonary infiltrates, pleural or pericardial effusions, rapid weight gain or peripheral edema, lymphadenopathy, bone pain, and hepatic, renal, or multi-organ dysfunction; hospitalize patients with pulmonary and/or renal manifestation for close observation and monitoring; hold tx if severe pulmonary symptoms and/or persistent renal dysfunction
Adult Dosing .
Dosage forms: TAB: 50 mg, 100 mg
Special Note
- [uses, dosing may vary]
- Info: refer to institution protocols and pkg insert prior to prescribing for uses and dosing including toxicity-related dose adjustments
IDH2-positive AML, relapsed or refractory
- [100 mg PO qd for at least 6mo]
- Info: do not cut/crush/chew tab
renal dosing
- [see below]
- CrCl >30: no adjustment; CrCl <30: not defined
- HD/PD: not defined
hepatic dosing
- [see below]
- mild impairment: no adjustment; moderate-severe impairment: not defined
Peds Dosing .
Peds dosing is currently unavailable or not applicable for this drug.
Contraindications / Cautions .
- hypersensitivity to drug or ingredient
- avoid: breastfeeding during tx and for at least 2mo after D/C
- caution: patients of childbearing potential
- caution: male patients of reproductive potential
Drug Interactions .
Overview
enasidenib
IDH2 inhibitor
- CYP1A2 inhibitor, strong
- CYP2C19 inhibitor, weak
- CYP2D6 inhibitor, weak
- BCRP inhibitor
- OATP1B1 inhibitor, moderate
- OATP1B3 inhibitor, moderate
- P-gp inhibitor, weak
- CYP3A4 inducer, weak
Contraindicated
Avoid/Use Alternative
Monitor/Modify Tx
Caution Advised
Adverse Reactions .
Serious Reactions
- differentiation syndrome
- leukocytosis
- tumor lysis syndrome
- QT prolongation
Common Reactions
- nausea
- diarrhea
- vomiting
- appetite decr.
- differentiation syndrome
- leukocytosis
- dysgeusia
- tumor lysis syndrome
- bilirubin elevated
- calcium decr.
- potassium decr.
- phosphate decr.
Safety/Monitoring .
Monitoring Parameters
pregnancy test at baseline; CBC with diff, chemistry profile including Ca, PO4, serum uric acid at baseline, then at least q2wk for at least 3mo
Pregnancy/Lactation .
Pregnancy
Clinical Summary
weigh risk/benefit during pregnancy; risk of spontaneous abortion based on animal data at 0.1x systemic exposure
Individuals of Reproductive Potential
obtain pregnancy test before tx start; avoid pregnancy by using effective contraception during tx and x2mo after D/C in patients of childbearing potential and male patients
Lactation
Clinical Summary
avoid breastfeeding during tx and for at least 2mo after D/C; no human data available to assess risk of infant harm or effects on milk production
Pharmacology .
Metabolism: for enasidenib: liver; CYP450: 1A2, 2B6, 2C8, 2C9, 2C19, 2D6, 3A4 substrate; UGT: 1A1, 1A3, 1A4, 1A9, 2B7, 2B15 substrate
Excretion: for enasidenib: feces 89% (34% unchanged), urine 11% (0.4% unchanged); Half-life: 7.9 days
Subclass: Epigenetic Modifiers, Isocitrate Dehydrogenase (IDH) Inhibitors
Mechanism of Action
for enasidenib: inhibits mutant isocitrate dehydrogenase 2 (IDH2) enzyme, leading to decr. 2-hydroxyglutarate (2-HG) levels and induced myeloid differentiation
Formulary .
No Formulary Selected
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