Enasidenib

What is Enasidenib?

• Enasidenib (Idhifa) is an isocitrate dehydrogenase-2 inhibitor used to treat relapsed or refractory acute myeloid leukemia in people with specific mutations of the isocitrate dehydrogenase 2 (IDH2) gene.

What are the uses of this medicine?

• This medicine is used to treat people with acute myeloid leukemia (AML) with an isocitrate dehydrogenase-2 (IDH2) mutation whose disease has come back or has not improved after previous treatment(s).

How does this medicine work?

• Enasidenib (en" a sid' e nib) is a small molecule inhibitor of isocitrate dehydrogenase-2 (IDH2), an enzyme rearranged and mutated in some forms of leukemia and lymphoma.
• The mutated IDH2 causes epigenetic alterations that result in a block in myeloid cell differentiation.
• Enasidenib has been found to inhibit mutated IDH2 and in several clinical trials was found to induce objective responses in a high proportion of patients with refractory AML who harbored mutant IDH2.

Who Should Not Use this medicine ?

• This medicine have no usage limitations.

What drug interactions can this medicine cause?

• Coadministration of Idhifa increases the exposure of OATP1B1, OATP1B3, and BCRP substrates, which may increase the incidence and severity of adverse reactions of these substrates. Decrease the dosage of OATP1B1, OATP1B3, and BCRP substrate(s) as recommended in the respective prescribing information, and as clinically indicated.
• Coadministration of Idhifa increases the exposure of P-gp substrates, which may increase the incidence and severity of adverse reactions of these substrates. Decrease the dosage of these substrates as recommended in its prescribing information when coadministered with Idhifa, and as clinically indicated.

Is this medicine FDA approved?

• It was approved for use in the United States in 2017.

How should this medicine be used?

• Select patients for the treatment of AML with Idhifa based on the presence of IDH2 mutations in the blood or bone marrow.

Recommended Dosage:

• The recommended dosage of Idhifa is 100 mg taken orally once daily with or without food until disease progression or unacceptable toxicity. For patients without disease progression or unacceptable toxicity, treat for a minimum of 6 months to allow time for clinical response.

Administration

• Take Idhifa exactly as your healthcare provider tells you to.
• Take Idhifa 1 time a day at the same time each day.
• Swallow Idhifa tablets whole. Do not chew or split the tablet.
• Swallow Idhifa with 8 ounces (one cup) of water.
• Idhifa can be taken with or without food.
• If you miss a dose of Idhifa or vomit after taking a dose of Idhifa, take the dose of Idhifa as soon as possible on the same day. Then take your next dose the next day at your regularly scheduled time. Do not take 2 doses at the same time to make up for the missed dose.
• Your healthcare provider should do blood tests to check your blood counts before you start Idhifa treatment and at a minimum of every 2 weeks for at least the first 3 months during treatment to check for side effects.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Tablets: 50 mg or 100 mg

This medicine is available in fallowing brand namesː

• Idhifa

What side effects can this medication cause?

The most common side effects of this medicine include:

• nausea
• vomiting
• diarrhea
• jaundice
• decreased appetite

Idhifa may cause serious side effects, including:

• Differentiation Syndrome

What special precautions should I follow?

• Patients treated with Idhifa experienced differentiation syndrome, which may be life-threatening or fatal if not treated. If differentiation syndrome is suspected, initiate oral or intravenous corticosteroids (e.g., dexamethasone 10 mg every 12 hours). Symptoms of differentiation syndrome may recur with premature discontinuation of corticosteroid treatment. If severe pulmonary symptoms requiring intubation or ventilator support, and/or renal dysfunction persist for more than 48 hours after initiation of corticosteroids, interrupt Idhifa until signs and symptoms are no longer severe. Hospitalization for close observation and monitoring of patients with pulmonary and/or renal manifestation is recommended.
• Idhifa can cause fetal harm. Advise patients of the potential risk to a fetus and use effective contraception.

What to do in case of emergency/overdose?

• In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

• Overdose related information is also available online at poisonhelp.org/help.
• In the event that the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services. In the United States, call 911.

Can this medicine be used in pregnancy?

• Idhifa can cause fetal harm when administered to a pregnant woman.
• There are no available data on Idhifa use in pregnant women to inform a drug-associated risk of major birth defects and miscarriage.

Can this medicine be used in children?

• Safety and effectiveness in pediatric patients have not been established.

What are the active and inactive ingredients in this medicine?

• Active ingredient: enasidenib
• Inactive ingredients: colloidal silicon dioxide, hydroxypropyl cellulose, hypromellose acetate succinate, iron oxide yellow, magnesium stearate, microcrystalline cellulose, polyethylene glycol, polyvinyl alcohol, sodium lauryl sulfate, sodium starch glycolate, talc, and titanium dioxide

Manufactured for and marketed by: Celgene Corporation, Summit, NJ 07901

Who manufactures and distributes this medicine?

• Manufactured for and marketed by:

Celgene Corporation Summit, NJ

• Licensed from:

Agios Pharmaceuticals Cambridge, MA

What should I know about storage and disposal of this medication?

• Store at 20°C-25°C (68°F-77°F); excursions permitted between 15°C-30°C (59°F-86°F).
• Keep the bottle tightly closed.
• Store in the original bottle (with a desiccant canister) to protect from moisture.

• Dailymed label info on Enasidenib
• FDA Enasidenib