Gilteritinib

What is Gilteritinib?

• Gilteritinib (Xospata) is a kinase inhibitor used as an antineoplastic agent in the treatment of acute myeloid leukemia with FLT3 mutations.

Gilteritinib

What are the uses of this medicine?

Gilteritinib (Xospata) is used to treat adults with acute myeloid leukemia (AML) who have a FMS-like tyrosine kinase 3 (FLT3) mutation:

• when the disease has come back, or
• has not improved after previous treatment(s).

How does this medicine work?

• Gilteritinib (gil" te ri' ti nib) is a potent small molecule inhibitor of FLT3 (FMS-like tyrosine kinase 3), a tyrosine kinase receptor that is mutated in to up one-third of patients with acute myeloid leukemia (AML).
• The mutated FLT3 activates an intracellular signaling cascade of RAS-MEK-PI3K-AKT-STAT-5, promoting unregulated cell growth and proliferation. Gilteritinib has been found to inhibit mutated FLT3 and in several clinical trials was found to induce objective responses in a proportion of patients with refractory AML with detectable FLT3 mutations.

Who Should Not Use this medicine ?

This medicine cannot be used in patients who:

• are allergic to gilteritinib or any of the ingredients in Xospata.

What drug interactions can this medicine cause?

Tell your doctor and pharmacist what prescription and nonprescription medications, vitamins, and nutritional supplements you are taking or plan to take. Be sure to mention any of the following:

• certain antifungals such as fluconazole (Diflucan), itraconazole (Onmel, Sporanox), and ketoconazole
• clarithromycin (Biaxin, in PrevPac)
• escitalopram (Lexapro)
• fluoxetine (Prozac)
• certain medications for human immunodeficiency virus (HIV) or acquired immunodeficiency syndrome (AIDS) such as efavirenz (Sustiva, in Atripla), indinavir (Crixivan), nelfinavir (Viracept), nevirapine (Viramune), ritonavir (Norvir, in Kaletra), and saquinavir (Invirase)
• certain medications for seizures such as carbamazepine (Carbatrol, Epitol, Tegretol, others), phenobarbital, and phenytoin (Dilantin, Phenytek)
• nefazodone
• pioglitazone (Actos)
• rifabutin (Mycobutin)
• rifampin (Rifadin, Rimactane, in Rifamate, in Rifater)
• sertraline (Zoloft)

Is this medicine FDA approved?

• Gilteritinib received accelerated approval for this indication in the United States in 2018.

How should this medicine be used?

• Select patients for the treatment of AML with Xospata based on the presence of FLT3 mutations in the blood or bone marrow.

Recommended dosage:

• The recommended starting dose of Xospata is 120 mg orally once daily with or without food.

Administration:

• Take Xospata 1 time a day at about the same time each day.
• Swallow Xospata tablets whole.
• Do not break, crush, or chew the tablet.
• Xospata can be taken with or without food.
• If you miss a dose of Xospata, or did not take it at the usual time, take your dose as soon as possible and at least 12 hours before your next dose.
• Return to your normal schedule the following day.
• Do not take 2 doses of Xospata within 12 hours.

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

This medicine is available in fallowing doasage form:

• As Tablets: 40 mg

This medicine is available in fallowing brand namesː

• Xospata

What side effects can this medication cause?

The most common side effects of this medicine include:

• changes in liver function tests
• joint or muscle pain
• tiredness
• fever
• pain or sores in mouth or throat
• swelling of arms or legs
• rash
• diarrhea
• shortness of breath
• nausea
• cough
• constipation
• eye problems
• headache
• dizziness
• low blood pressure
• vomiting
• decreased urination

Xospata may cause serious side effects, including:

• Differentiation Syndrome
• Posterior Reversible Encephalopathy Syndrome (PRES)
• QTc prolongation
• pancreatitis

What special precautions should I follow?

• Patients treated with Xospata have experienced symptoms of differentiation syndrome, which can be fatal or life-threatening if not treated. If differentiation syndrome is suspected, initiate corticosteroid therapy and hemodynamic monitoring until symptom resolution.
• Patients treated with Xospata in the clinical trials, 1% experienced posterior reversible encephalopathy syndrome (PRES) with symptoms including seizure and altered mental status. Discontinue Xospata in patients who develop PRES.
• Xospata has been associated with prolonged cardiac ventricular repolarization (QT interval). Interrupt and reduce Xospata dosage in patients who have a QTcF >500 msec. Correct hypokalemia or hypomagnesemia prior to and during Xospata administration.
• Patients treated with Xospata in the clinical trials, experienced pancreatitis. Interrupt and reduce the dose in patients who develop pancreatitis.
• Xospata can cause fetal harm when administered to a pregnant woman. Advise of the potential risk to a fetus and to 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?

• Based on mechanism of action, Xospata can cause fetal harm when administered to a pregnant woman.
• Advise pregnant women of the potential risk to a fetus.

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: gilteritinib
• Inactive ingredients: ferric oxide, hydroxypropyl cellulose, hypromellose, low-substituted hydroxypropyl cellulose, mannitol, magnesium stearate, polyethylene glycol, talc, and titanium dioxide.

Who manufactures and distributes this medicine?

Distributed by: Astellas Pharma US, Inc., Northbrook, Illinois

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

• Store Xospata at room temperature between 68°F to 77°F (20°C to 25°C).
• Keep Xospata in the original container to protect it from light, moisture, and humidity.

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• Dailymed label info on Gilteritinib
• FDA Gilteritinib

Gilteritinib Resources
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Gilteritinib Resources
Need Help Finding a Doctor? Need help finding a doctor or specialist anywhere in the world? Explore our world directory. WikiMD's DocFinder can assist you in locating millions of physicians.	Medical Knowledge Access the latest research - Most recent articles Ongoing trials.