📄 Detailed Description of Enasinib 50 mg (Enasidenib) – Everest Pharmaceuticals

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Product Name:

• Enasinib® 50 mg Tablet

• Generic name: Enasidenib Mesylate

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💊 Composition

• Each film-coated tablet contains:

  • Enasidenib Mesylate equivalent to 50 mg Enasidenib

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🔬 Pharmacological Class

• IDH2 (isocitrate dehydrogenase 2) inhibitor

• Antineoplastic agent (anticancer drug)

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🩸 Indications and Uses

• Treatment of adult patients with relapsed or refractory acute myeloid leukemia (AML) that has an IDH2 mutation.

• Mutation must be confirmed using an FDA-approved test.

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📈 Mechanism of Action

• Enasidenib selectively inhibits mutant IDH2 enzyme.

• Mutant IDH2 increases 2-hydroxyglutarate (2-HG), which blocks normal blood cell development.

• By lowering 2-HG, Enasidenib promotes differentiation of immature blood cells, reducing leukemia burden.

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🧪 Pharmacokinetics

• Absorption: Oral bioavailability ~57%; peak plasma level ~4 hours after dose.

• Distribution: Protein binding ~94%; widespread distribution.

• Metabolism: Metabolized primarily by enzymes UGT1A1, CYP1A2, CYP2B6, CYP3A4.

• Elimination:

  • Half-life ~137 hours (long duration)

  • Excreted mostly in feces (89%) and some in urine (11%).

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💉 Dosage and Administration

• Recommended dose: 100 mg orally once daily

• Administer with or without food.

• Continue for at least 6 months or until disease progression or unacceptable toxicity.

• If a dose is missed, take it as soon as possible on the same day; skip if a whole day is missed.

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⚠️ Warnings and Precautions

• Differentiation Syndrome:

  • Life-threatening; symptoms: fever, cough, shortness of breath, rapid weight gain, swelling.

  • Treat promptly with corticosteroids.

• Embryo-fetal toxicity:

  • Avoid use in pregnancy; use effective contraception for men and women during and after treatment.

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❗ Adverse Reactions (Side Effects)

• Differentiation syndrome

• Nausea, vomiting, diarrhea

• Jaundice, elevated bilirubin

• Fatigue, loss of appetite

• Electrolyte imbalances (potassium, phosphorus, calcium)

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🔄 Drug Interactions

• Enasidenib inhibits enzymes (CYP1A2, CYP2B6, CYP3A4, UGT1A1) → may increase blood levels of some drugs, including hormonal contraceptives.

• Use caution when combined with sensitive substrates of these enzymes.

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👥 Use in Specific Populations

• Pregnancy & Lactation: Contraindicated; may cause fetal harm.

• Pediatric: Safety and efficacy not established.

• Geriatric: No dose adjustment required.

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📦 Packaging and Storage

• Store at below 30°C, protect from light.

• Keep in child-resistant containers.

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🌐 Manufacturer

• Everest Pharmaceuticals Ltd.

• Country: Bangladesh

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📎 Summary of Category

• Therapeutic Class: Antineoplastic agent

• Pharmacologic Class: IDH2 inhibitor

• Product Type: Oral prescription drug