Enasidenib

Enasidenib is a prescription medication used for the treatment of relapsed/refractory acute myeloid leukemia with an isocitrate dehydrogenase-2 mutation as detected by an FDA-approved test.

• Enasidenib is available under the following different brand names: Idhifa.

Common side effects of Enasidenib include:

• nausea
• vomiting
• diarrhea
• elevated bilirubin
• decreased appetite
• changes in taste
• tumor lysis syndrome
• differentiation syndrome
• noninfectious leukocytosis

Serious side effects of Enasidenib include:

• hives
• difficulty breathing
• swelling of the face, lips, tongue, or throat
• fever
• cough
• bone pain
• rapid weight gain
• swelling in the arms, legs, underarms, groin, or neck
• dark urine
• clay-colored stools
• yellowing of the skin or eyes (jaundice)
• severe or ongoing vomiting or diarrhea
• tiredness
• weakness
• muscle cramps
• nausea
• vomiting
• diarrhea
• fast or slow heart rate
• tingling in the hands and feet or around the mouth

Rare side effects of Enasidenib include:

• none

Seek medical care or call 911 at once if you have the following serious side effects:

• Severe headache, confusion, slurred speech, arm or leg weakness, trouble walking, coordination loss, unsteady, very stiff muscles, high fever, profuse sweating, or tremors
• Serious eye symptoms such as sudden vision loss, blurred vision, tunnel vision, eye pain or swelling, or seeing halos around lights
• Serious heart symptoms include fast, irregular, or pounding heartbeats, fluttering in the chest; shortness of breath, sudden dizziness, lightheadedness, or passing out

This is not a complete list of side effects and other serious side effects or health problems that may occur because of the use of this drug. Call your doctor for medical advice about serious side effects or adverse reactions. You may report side effects or health problems to FDA at 1-800-FDA-1088.

Adult dosage

Tablet

• 50 mg
• 100 mg

Acute myeloid leukemia

Adult dosage

• 100 mg orally once a day until disease progression or unacceptable toxicity
• Treat patients without disease progression or unacceptable toxicity for more than 6 months to allow time for clinical response.

Dosage Considerations – Should be Given as Follows:

• See “Dosages”

If your medical doctor is using this medicine to treat your pain, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, health care provider, or pharmacist first.

• Enasidenib has severe interactions with no other drugs.
• Enasidenib has serious interactions with no other drugs.
• Enasidenib has moderate interactions with no other drugs.
• Enasidenib has minor interactions with the following drugs:
  • dienogest/estradiol valerate
  • drospirenone
  • ethinylestradiol
  • levonorgestrel oral
  • levonorgestrel oral/ethinylestradiol/ferrous bisglycinate

This information does not contain all possible interactions or adverse effects. Visit the RxList Drug Interaction Checker for any drug interactions. Therefore, before using this product, tell your doctor or pharmacist about all the products you use. Keep a list of all your medications with you and share this information with your doctor and pharmacist. Check with your healthcare professional or doctor for additional medical advice, health questions, or concerns.

Contraindications

• none

Effects of drug abuse

• none

Short-Term Effects

• See “What Are Side Effects Associated with Using Enasidenib?”

Long-Term Effects

• See “What Are Side Effects Associated with Using Enasidenib?”

Cautions

• Differentiation syndrome reported, which can be fatal if not treated
• Based on animal embryofetal toxicity studies, Enasidenib can cause embryofetal harm when administered to pregnant women
• Drug interaction overview
  • OATP1B1, OATP1B3, and BCRP substrates
    • Enasidenib is an OATP1B1, OATP1B3, and BCRP inhibitor
    • Coadministration with OATP1B1, OATP1B3, and BCRP substrates will increase the effects and toxicities of these substrates
    • Decrease the dose of OATP1B1, OATP1B3, and BCRP substrate(s) as recommended in the respective prescribing information, and as clinically indicated
  • P-glycoprotein (P-gp) substrates
    • Enasidenib is a P-gp inhibitor
    • Coadministration with P-gp substrates will increase the effects and toxicities of these substrates
    • For a sensitive P-gp substrate that may lead to serious adverse reactions, decrease the dose, or modify the dosing frequency of such a P-gp substrate and monitor for adverse reactions as recommended in the respective prescribing information

Pregnancy and Lactation

• Based on animal embryofetal toxicity studies, fetal harm may occur when administered to pregnant women
• No data on use in pregnant women is available to inform a drug-associated risk for major birth defects and miscarriage
• Infertility
  • Based on findings in animals, fertility may be impaired in women and men of reproductive potential
  • Unknown whether the drug’s effects on fertility are reversible
• Contraception
  • Women of reproductive potential
    • Avoid getting pregnant while receiving Enasidenib
    • Use effective contraception during treatment with Enasidenib and for at least 2 months after the last dose
    • Coadministration of Enasidenib may increase or decrease the concentrations of combined hormonal contraceptives; the clinical significance is unknown at this time
  • Men with women partners of reproductive potential
    • Use effective contraception during treatment with Enasidenib and for at least 2 months after the last dose
• Lactation
  • There are no data on the presence of Enasidenib or its metabolites in human milk, its effects on breastfed infants, or on milk production
  • Advise women not to breastfeed during treatment with Enasidenib and for at least 2 months after the last dose