• Relapsed or refractory acute myeloid leukemia (AML) with an isocitrate dehydrogenase-2 (IDH2) mutation.

Contraindicated in:

• OB: Pregnancy (may cause fetal harm)
• Lactation: Lactation.

Use Cautiously in:

• Rep: Women of reproductive potential and men with female partners of reproductive potential
• Pedi: Safety and effectiveness not established in children.

F and E: hypocalcemia, hypokalemia, hypophosphatemia.

GI: ↓appetite, ↑bilirubin, diarrhea, nausea, vomiting.

GU: ↓fertility.

Hemat: differentiation syndrome, leukocytosis.

Neuro: dysgeusia.

Misc: tumor lysis syndrome.

Drug-Drug:

• May ↑ levels and risk of toxicity of OATP1B1 substrates, OATP1B3 substrates, and BCRP substrates, including rosuvastatin; ↓ dose of OAT1B1 substrates, OAT1B3 substrates, and BCRP substrates.
• May ↑ levels and risk of toxicity of P-glycoprotein substrates, including digoxin; ↓ dose of P-glycoprotein substrates with narrow therapeutic indices.

• Tablets: 50 mg; 100 mg;

• PO (Adults): 100 mg once daily for 6 mo; continue until disease progression or unacceptable toxicity.

Idhifa

• Inhibits the IDH2 enzyme, especially the mutant variants, R140Q, R172S, and R172K. Inhibiting these mutant enzymes results in decreased 2-hydroxyglutarate levels with subsequent induction of myeloid differentiation. Overall effect in patients with AML is a reduction in blast cells and an increased proportion of mature myeloid cells.

• Promotion of complete remission and reduction in need for transfusions.

Therapeutic Classification: antineoplastics

Pharmacologic Classification:

Absorption: 57% absorbed following oral administration.

Distribution: 55.8 L.

Protein Binding: 98.5%.

Metabolism/Excretion: Metabolized by numerous CYP450 isoenzymes (CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, and CYP3A4) to an active metabolite (AGI-16903). Also metabolized by multiple UDP-glucuronosyltransferase (UGTs). AGI–16903 is also metabolized by multiple CYP450 isoenzymes and UGTs. 89% eliminated in feces (34% as unchanged drug); 11% eliminated in urine (<1% as unchanged drug).

Half-life: 7.9 days.

(blood levels)

• Instruct patient to take enasidenib as directed at same time each day. If dose is missed, not taken at usual time, or vomited, take dose as soon as possible on same day. Then return to routine schedule. Advise patient to read Medication Guide before starting therapy and with each Rx refill in case of changes.
• Advise patient to notify health care professional if signs and symptoms of differentiation syndrome (fever, cough or difficulty breathing, bone pain, rapid weight gain, swelling of their arms or legs) occur. May occur as early as 1 day through 5 mo of therapy.
• Inform patient of risk of tumor lysis syndrome and advise of need to maintain fluid intake and frequent blood chemistry monitoring.
• Advise patient to notify health care professional if signs and symptoms of GI adverse reactions (diarrhea, nausea, vomiting, decreased appetite, changes in sense of taste) or elevated bilirubin (changes to color of skin or whites of eyes) occur.
• Rep: May cause fetal harm. Advise females of reproductive potential and male patients with female partners of reproductive potential to use effective contraception during and for at least 2 mo after last dose of enasidenib. Advise female patient not to breastfeed during therapy and for at least 2 mo after last dose. Inform patients that enasidenib may impair fertility in male and female patients.
• Encourage patient to follow up with lab tests to monitor for side effects.

en-a-SID-a-nib

NDC Code^*

• 59572- Celgene Corporation
  • 59572-705- Idhifa
    • 59572-705-30- 30 TABLET, FILM COATED in 1 BOTTLE (59572-705-30)

• 59572- Celgene Corporation
  • 59572-710- Idhifa
    • 59572-710-30- 30 TABLET, FILM COATED in 1 BOTTLE (59572-710-30)