How does this medication work? What will it do for me?

Gilteritinib belongs to the class of medications called antineoplastics. Specifically, it is a tyrosine kinase inhibitor. Gilteritinib is used to treat adults with acute myeloid leukemia with a FMS-like tyrosine kinase 3 (FLT3) mutation, that has been successfully treated and has returned or has been treated unsuccessfully with other medications.

Gilteritinib works by blocking the activity of proteins that trigger the production of abnormal blood cells in the bone marrow. Gilteritinib stops the cancer cells from growing and dividing and kills the leukemia cells in the bone marrow.

This medication may be available under multiple brand names and/or in several different forms. Any specific brand name of this medication may not be available in all of the forms or approved for all of the conditions discussed here. As well, some forms of this medication may not be used for all of the conditions discussed here.

Your doctor may have suggested this medication for conditions other than those listed in these drug information articles. If you have not discussed this with your doctor or are not sure why you are taking this medication, speak to your doctor. Do not stop taking this medication without consulting your doctor.

Do not give this medication to anyone else, even if they have the same symptoms as you do. It can be harmful for people to take this medication if their doctor has not prescribed it.

What form(s) does this medication come in?

The recommended dose of gilteritinib is 120 mg (three 40 mg tablets) taken by mouth, once daily. It may be taken with food or on an empty stomach and should be taken at the same time each day. Swallow the tablets whole with some water. Do not crush or chew them.

Many things can affect the dose of medication that a person needs, such as body weight, other medical conditions, and other medications. If your doctor has recommended a dose different from the ones listed here, do not change the way that you are taking the medication without consulting your doctor.

It is important to take this medication exactly as prescribed by your doctor.

If you miss a dose, take it as soon as possible and continue with your regular schedule. If it is less than 12 hours until your next dose, skip the missed dose and continue with your regular dosing schedule. If you vomit after taking a dose, do not take another dose, but continue with your regular dosing schedule the next day. Do not take a double dose to make up for a missed one. If you are not sure what to do after missing a dose, contact your doctor or pharmacist for advice .

Store this medication at room temperature, protect it from light and moisture, and keep it out of the reach of children

How should I use this medication?

Each light yellow, round-shaped, film-coated tablet debossed with the Astellas logo and "235" on the same side contains 40 mg of gilteritinib as gilteritinib fumarate. Nonmedicinal ingredients: hydroxypropyl cellulose, hypromellose, low-substituted hydroxypropyl cellulose, magnesium stearate, mannitol, polyethylene glycol, talc, titanium dioxide, and ferric oxide.

Do not dispose of medications in wastewater (e.g. down the sink or in the toilet) or in household garbage. Ask your pharmacist how to dispose of medications that are no longer needed or have expired.

Who should NOT take this medication?

Do not take this medication if you are allergic to gilteritinib or any ingredients of the medication.

What side effects are possible with this medication?

Many medications can cause side effects. A side effect is an unwanted response to a medication when it is taken in normal doses. Side effects can be mild or severe, temporary or permanent.

The side effects listed below are not experienced by everyone who takes this medication. If you are concerned about side effects, discuss the risks and benefits of this medication with your doctor.

The following side effects have been reported by at least 1% of people taking this medication. Many of these side effects can be managed, and some may go away on their own over time.

Contact your doctor if you experience these side effects and they are severe or bothersome. Your pharmacist may be able to advise you on managing side effects.

  • constipation
  • cough
  • decreased appetite
  • diarrhea
  • dizziness
  • fatigue
  • general feeling of being unwell
  • headache
  • joint pain
  • muscle pain
  • nausea
  • skin rash
  • strange taste in the mouth
  • stomach pain
  • swelling in the feel, ankles, hands
  • vomiting
  • weakness

Although most of the side effects listed below don't happen very often, they could lead to serious problems if you do not seek medical attention.

Check with your doctor as soon as possible if any of the following side effects occur:

  • fainting
  • fever
  • fluid build-up around the lungs (e.g., chest pain, cough, hiccups, rapid breathing)
  • increased frequency or severity of infections (symptoms may include fever or chills, severe diarrhea, shortness of breath, prolonged dizziness, headache, stiff neck, weight loss, or listlessness)
  • inflammation of the mouth and lips
  • low magnesium levels in the blood (e.g., weakness, tremor, muscle cramps, seizures)
  • low potassium levels in the blood (e.g., weakness, fatigue, muscle cramps, irregular heartbeat)
  • pain, numbness, or weakness in the hands and feet
  • signs of anemia (low red blood cells; e.g., dizziness, pale skin, unusual tiredness or weakness, shortness of breath)
  • signs of clotting problems (e.g., unusual nosebleeds, bruising, blood in urine, coughing blood, bleeding gums, cuts that don't stop bleeding)
  • signs of heart problems (e.g., fast, irregular heartbeat or pulse; chest pain; sudden weight gain; difficulty breathing; leg swelling)
  • signs of kidney failure (e.g., decreased urine production, swelling, fatigue, abdominal pain)
  • signs of kidney problems (e.g., change in the amount or colour of urine, increased urination at night, blood in the urine, swelling in the feet or legs)
  • symptoms of high blood sugar (e.g., frequent urination, increased thirst, excessive eating, unexplained weight loss, poor wound healing, infections, fruity breath odour)

Stop taking the medication and seek immediate medical attention if any of the following occur:

  • shortness of breath
  • fluid build-up around the heart (e.g., fever, fatigue, muscle aches, shortness of breath, nausea, vomiting, diarrhea, fast or pounding heartbeat, light-headedness)
  • signs of an allergic reaction (e.g., wheezing, tightness in chest, troubled breathing, shortness of breath, or cough)
  • signs of posterior reversible encephalopathy syndrome (e.g., headache, seizures, weakness, confusion, high blood pressure, vision changes, difficulty thinking clearly)

Some people may experience side effects other than those listed. Check with your doctor if you notice any symptom that worries you while you are taking this medication.

Are there any other precautions or warnings for this medication?

Before you begin using a medication, be sure to inform your doctor of any medical conditions or allergies you may have, any medications you are taking, whether you are pregnant or breast-feeding, and any other significant facts about your health. These factors may affect how you should use this medication.

Birth control: Women and men who are taking gilteritinib should use effective birth control. Women should use effective birth control while taking this medication and for at least 6 months after taking the last dose. Men taking gilteritinib and whose partners may become pregnant should use effective birth control while taking this medication and for at least 4 months after taking the last dose.

Driving: Gilteritinib can cause severe dizziness or fainting which may affect your ability to safely drive or operate machinery. Do not drive or perform hazardous tasks such as operating machinery until you know how this medication affects you.

Grapefruit juice: Grapefruit juice affects how gilteritinib is removed from the body and may cause the medication to build up in the body, causing side effects. Do not drink grapefruit juice while taking this medication.

Heart rhythm: Gilteritinib can cause changes to the normal rhythm of the heart, including an irregular heartbeat called QT prolongation. QT prolongation is a serious life-threatening condition that can cause fainting, seizures, and sudden death. If you are at risk for heart rhythm problems (e.g., people with heart failure, angina, low potassium or magnesium levels), discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.

Liver function: If you have liver problems, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.

Pancreatitis: This medication can cause the pancreas to become inflamed. If you have a history of pancreatitis, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.

Report signs of pancreatitis such as abdominal pain on the upper left side, back pain, nausea, fever, chills, rapid heartbeat, or swollen abdomen to your doctor immediately.

Posterior reversible leukoencephalopathy syndrome (PRES): This is a rare disease of the brain that may occur when using medications like gilteritinib. Make sure your doctor knows if you have experienced this before. If you experience signs and symptoms of RPLS, such as headache, seizures, change in awareness or consciousness, or vision changes, contact your doctor immediately.

Respiratory problems: Cases of severe inflammation of the lung and heart have been reported with gilteritinib. These lung and heart problems can be life-threatening and should be considered a medical emergency. If you experience fever, shortness of breath, swelling of the ankles and feet, sudden weight gain, or painful breathing, seek immediate medical attention.

Pregnancy: This medication should not be used during pregnancy due to the risk that it may cause harm to the unborn baby. If you become pregnant while taking this medication, contact your doctor immediately.

Breast-feeding: It is not known if gilteritinib passes into breast milk. If you are breast-feeding and are taking this medication, it may affect your baby. Women are advised to avoid breast-feeding while taking this medication and for 2 months after taking the last dose.

Children: The safety and effectiveness of using this medication have not been established for children.

What other drugs could interact with this medication?

There may be an interaction between gilteritinib and any of the following:

  • alfuzosin
  • antiarrhythmics (e.g., amiodarone, dronedarone, procainamide, quinidine, sotalol)
  • antipsychotics (e.g., chlorpromazine, clozapine, haloperidol, olanzapine, pimozide, quetiapine, risperidone, thioridazine)
  • apalutamide
  • aprepitant
  • "azole" antifungals (e.g., fluconazole, itraconazole, ketoconazole, posaconazole, voriconazole)
  • bosentan
  • carbamazepine
  • chloroquine
  • cobicistat
  • conivaptan
  • dabigatran
  • degarelix
  • digoxin
  • diltiazem
  • domperidone
  • doxepin
  • grapefruit juice
  • HIV non-nucleotide reverse transcriptase inhibitors (e.g., efavirenz, etravirine, rilpiverine)
  • HIV protease inhibitors (e.g., atazanavir, darunavir, indinavir, lopinavir, ritonavir)
  • indacaterol
  • lumacaftor and ivacaftor
  • macrolide antibiotics (e.g., azithromycin, clarithromycin, erythromycin)
  • metformin
  • methadone
  • mifepristone
  • mitotane
  • pentamidine
  • phenobarbital
  • phenytoin
  • primidone
  • other protein kinase inhibitors (e.g., ceritinib, dabrafenib, dasatinib, imatinib, vandetanib, vemurafenib)
  • quinolone antibiotics (e.g., levofloxacin, moxifloxacin)
  • rifabutin
  • rifampin
  • romidepsin
  • rosuvastatin
  • St. John's wort
  • selective serotonin reuptake inhibitors (SSRIs; e.g., citalopram, escitalopram, fluvoxamine, sertraline)
  • serotonin antagonists (anti-emetic medications; e.g., granisetron, ondansetron)
  • trazodone
  • verapamil

If you are taking any of these medications, speak with your doctor or pharmacist. Depending on your specific circumstances, your doctor may want you to:

  • stop taking one of the medications,
  • change one of the medications to another,
  • change how you are taking one or both of the medications, or
  • leave everything as is.

An interaction between two medications does not always mean that you must stop taking one of them. Speak to your doctor about how any drug interactions are being managed or should be managed.

Medications other than those listed above may interact with this medication. Tell your doctor or prescriber about all prescription, over-the-counter (non-prescription), and herbal medications you are taking. Also tell them about any supplements you take. Since caffeine, alcohol, the nicotine from cigarettes, or street drugs can affect the action of many medications, you should let your prescriber know if you use them.

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