How it is administered

Enasidenib is taken by mouth as a tablet. It is available in 50 mg and 100 mg strengths. The usual recommended dose is 100 mg taken once daily, with or without food. Tablets should be swallowed whole with water and should not be chewed, split, or crushed.

How it works

Enasidenib is a targeted therapy that works by inhibiting a specific enzyme called isocitrate dehydrogenase 2 (IDH2). In some patients with acute myeloid leukemia (AML), mutations in the IDH2 gene cause the enzyme to function abnormally. This abnormal enzyme produces a substance called 2-hydroxyglutarate (2-HG), which interferes with the normal development of blood cells and contributes to the growth of cancerous cells.

By blocking the mutant IDH2 enzyme, enasidenib reduces the levels of 2-HG in the blood. This helps restore the normal process of blood cell development and can lead to a reduction in leukemia cells and an increase in healthy, mature blood cells. Enasidenib is specifically designed for patients whose AML cells have the IDH2 mutation, and its effectiveness depends on the presence of this mutation.

Who Should take it

Enasidenib is indicated for adult patients with relapsed or refractory acute myeloid leukemia (AML) who have an IDH2 mutation. This means it is used when the leukemia has returned after previous treatment or has not responded to other treatments, and only if the IDH2 mutation is detected by an FDA-approved test.

It is important for patients to undergo genetic testing to confirm the presence of the IDH2 mutation before starting enasidenib. Your healthcare provider will determine if this medication is appropriate for you based on your specific diagnosis and previous treatments.

Who should not take it

There are no absolute contraindications listed for enasidenib. However, it should be used with caution in certain populations:

• Pregnant women should not take enasidenib, as it can cause harm to an unborn baby. Women of reproductive potential should use effective contraception during treatment and for at least 2 months after the last dose.
• Breastfeeding is not recommended during treatment and for 2 months after the last dose.

Patients should inform their healthcare provider about all other medications and health conditions before starting enasidenib. Your doctor will assess if enasidenib is safe for you.

Commonly used with

Enasidenib is primarily used as a single agent for the treatment of relapsed or refractory AML with IDH2 mutation. However, supportive medications may be used alongside enasidenib to manage side effects or complications. For example, corticosteroids are often used to treat differentiation syndrome, and hydroxyurea may be used to control high white blood cell counts.

Patients may also receive medications to prevent or treat infections, manage nausea, or address other symptoms related to AML or its treatment.

Commonly tested with

Enasidenib has been tested in combination with supportive care medications such as corticosteroids (for differentiation syndrome) and hydroxyurea (for leukocytosis). It has also been studied in patients who have previously received other chemotherapy agents for AML.

Before starting enasidenib, patients are tested for the IDH2 mutation using an FDA-approved test, as the medication is only effective in those with this specific mutation.