How it Works

Gilteritinib works by targeting and inhibiting the activity of the FLT3 enzyme (also called kinase), which is involved in the growth and survival of cancer cells. By blocking the action of this enzyme, gilteretinib may help to slow the growth and spread of cancer cells and may lead to cancer cell death (apoptosis). 

It is important to note that gilteretinib is a targeted therapy for FLT3-mutated AML and is not suitable for all patients with AML.

How Gilteritinib is Administered

Gilteritinib is usually given as a pill that is taken orally (by mouth). It is usually taken once a day, at the same time each day, this pill should be swallowed whole without breaking it or crushing it. You must avoid grapefruit produce if ingesting food with the medication, as it may affect the metabolization of Gilteritinib.  

The dosage and duration of treatment will depend on the individual patient and the specific type of AML being treated.

Who Should Take Gilteritinib

Gilteritinib is currently approved for:

• Adult patients with acute myeloid leukemia who have an FLT3 mutation and have relapsed after receiving at least one prior induction treatment. 
• Patients with acute myeloid leukemia who have the FLT3 mutation and have not responded to other treatments.

Who Shouldn’t Take Gilteritinib 

• It should not be used in patients who are allergic to gilteretinib or any of its ingredients.
• Patients diagnosed with Long QT syndrome (LQTS). A rare inherited heart rhythm disorder that can cause potentially life-threatening irregular heartbeats, known as arrhythmias.
• Patients with an electrolyte imbalance like low-potassium or low-magnesium. Electrolyte abnormalities must be corrected before initiating and during administration. 
• Pregnant women.  It is important to inform your healthcare provider if you are pregnant, or planning to become pregnant before starting treatment with gilteretinib.
• Gilteretinib may also pass into breast milk, you should suspend breastfeeding when taking this medication. 

The Most Common Side Effects of Taking Gilteritinib Include the Following: 

• Pain in the muscles or articulations
• Increased liver enzymes
• Fatigue, malaise, fever
• Difficulty Breathing, pneumonia or coughs
• Swelling (edema), rash
• Gastrointestinal symptoms, like, noninfectious diarrhea, constipation, nausea, stomatitis, vomiting,  abdominal pain, decreased appetite
• Headache or dizziness
• Low blood pressure or decreased kidney function
• 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, and 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.
• Pulmonary infiltrates, accumulation of excess fluid in the space surrounding the heart or the chest wall, rapid weight gain, swelling of the extremities, low blood pressure, or kidney dysfunction.

Commonly Used in Acute Myeloid Leukemia With

• Venetoclax (Venclexta)
• FLAG-ida (fludarabine, cytarabine, G-CSF, idarubicin)
• CLIA (cladribine, idarubicin, cytarabine)
• GO (Gemtuzumab Ozogamicin)
• As a single-drug therapy

TAKE A LOOK AT THE AVAILABLE CLINICAL TRIALS FOR AML

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Date last updated: 12/22/22