gilteritinib fumarate at a glance
Medicine class
Targeted protein kinase inhibitor that blocks FLT3 and AXL.
Licensed use
Used alone in adults with relapsed or refractory AML confirmed to have a FLT3 mutation.
Taking the tablets
Swallow whole with water; do not break or crush. They may be taken with or without food.
Safety monitoring
Blood tests and heart-rhythm checks are required before and during treatment.
What is gilteritinib fumarate used for?
It is licensed for:
Use alone in adults with relapsed or refractory acute myeloid leukaemia that has a confirmed FLT3 mutation.
How does gilteritinib fumarate work?
FLT3 mutations can produce signals that help abnormal leukaemia cells survive and multiply. Gilteritinib inhibits FLT3 and AXL kinases, reducing these growth signals and promoting the death of susceptible leukaemia cells.
gilteritinib fumarate preparations and strengths
Tablet
Route: Oral
Strengths: 40 mg
How to take gilteritinib fumarate
Follow the instructions provided by the specialist cancer team.
Swallow the tablets whole with water.
Do not break, crush or chew them.
They may be taken with or without food.
gilteritinib fumarate side effects
Common or expected effects
- Diarrhoea, nausea or constipation
- Tiredness, weakness or dizziness
- Cough or shortness of breath
- Fluid retention and swelling
- Low blood pressure
- Muscle, joint or limb pain
- Changes in liver enzymes, alkaline phosphatase or creatine phosphokinase on blood tests
Get urgent medical advice
- Fever, breathlessness, swelling, rapid weight gain, rash or light-headedness suggesting differentiation syndrome
- Seizure, worsening headache, confusion or visual disturbance suggesting posterior reversible encephalopathy syndrome
- Palpitations, fainting or altered heartbeat suggesting QT prolongation
- Severe upper abdominal or back pain with nausea or vomiting suggesting pancreatitis
- Facial, mouth or throat swelling, hives or breathing difficulty suggesting anaphylaxis
- Reduced urine output with leg swelling suggesting acute kidney injury
gilteritinib fumarate in pregnancy
Gilteritinib may harm an unborn baby and is not recommended during pregnancy. Pregnancy testing and effective contraception are required where relevant; hormonal contraception should be supplemented with a barrier method. Anyone who is pregnant, may be pregnant or is planning pregnancy should speak promptly with the specialist team.
gilteritinib fumarate while breastfeeding
Breastfeeding should stop during treatment and remain stopped for the post-treatment period specified by the specialist team because exposure through breast milk and harm to the child cannot be excluded.
gilteritinib fumarate interactions
The cancer team and pharmacist should review prescribed, over-the-counter and herbal products before treatment.
Rifampicin, phenytoin and St John’s wort
Strong CYP3A/P-gp induction can substantially reduce gilteritinib exposure and may reduce effectiveness, so combined use should be avoided.
Azole antifungals such as itraconazole, posaconazole and voriconazole
Strong CYP3A, P-gp or BCRP inhibition can increase gilteritinib exposure and toxicity; alternatives or closer monitoring may be needed.
Macrolide antibiotics such as clarithromycin, erythromycin and azithromycin
These may increase gilteritinib exposure, requiring specialist review and toxicity monitoring.
Common questions about gilteritinib fumarate
Answers are fully visible for fast scanning and source review.
Why is gilteritinib fumarate used only for some types of AML?
It targets abnormal FLT3 signalling, so the AML must have a confirmed FLT3 mutation before treatment is started.
Is gilteritinib fumarate chemotherapy?
It is an anticancer treatment, but more specifically it is a targeted protein kinase inhibitor rather than conventional cytotoxic chemotherapy.
Can gilteritinib fumarate be taken with food?
Sources
These sources were used to prepare and review this medicine page.
Prepared and reviewed by the iatroX editorial team.