How it Works

Enasidenib targets a specific enzyme called IDH2 that is often mutated in AML. By inhibiting this enzyme, the growth and spread of cancer cells is prevented. Enasidenib has also been shown to block several other enzymes involved in the normal differentiation and growth of cells in the myeloid lineage. This can help to slow down the production of abnormal cells and may help to improve the effectiveness of other treatments.

How it’s Administered

• Oral pill: The pills are usually taken once a day, and the patient should take them at the same time each day. It is important to swallow the pills whole and not crush or chew them, and avoid eating grapefruit products, because they can interfere with the way the drug is metabolized in the body.

Who Should Take Enasidenib 

• Is indicated for the treatment of adult patients with relapsed or refractory (R/R) acute myeloid leukemia (AML) with an isocitrate dehydrogenase-2 (IDH2) mutation

Who Shouldn’t Take Enasidenib 

• Pregnant women. It is important to inform your healthcare provider if you are pregnant, or planning to become pregnant before starting treatment, as it may cause harm to the fetus.
• Breastfeeding women should suspend breastfeeding if they start taking this medication. 
• Patients with a high amount of bilirubin in the blood 
• High levels of white blood cells 
• People who are allergic to the medication or any of its components.

The Most Common Side Effects of Taking Enasidenib Include:

• Gastrointestinal issues like nausea, vomiting, diarrhea, decreased appetite, bilirubin level in the blood, and electrolyte imbalance. 
• Rash on the skin.
• Fatigue, headache
• Low white blood cell count, increasing the risk of infections
• Differentiation syndrome is a very serious side effect that is preventable with proper monitoring and immediate treatment. This syndrome is a reaction between the drug and leukemia, which produces fever, difficulty breathing, weight gain, lung and heart problems. It is generally treated with high-dose steroids. In most cases, treatment will continue. The syndrome usually occurs during the first month of treatment, with some cases reported following the first dose.

Commonly Used in Acute Myeloid Leukemia With

• Enasidenib is currently FDA-approved for AML only as a single drug therapy.

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Date last updated 12/22/22