Gilteritinib
FLT3 inhibitors
FLT3 inhibitorsHigh alert
An error with this medicine can cause serious harm: double checks and protocols are used.Pregnancy: avoid
Avoid in pregnancy. Gilteritinib may harm the fetus: a pregnancy test is done first, women and men use contraception during and for months after treatment, and breastfeeding is…
An oral FLT3 inhibitor for relapsed or refractory FLT3-mutated AML. Watch for differentiation syndrome, QT prolongation and brain swelling.
Quick facts
- Group
- FLT3 inhibitors
- Target
- FLT3 receptor tyrosine kinase (also other receptor tyrosine kinases)
- Key effects
- Muscle and joint pain · Fatigue · Nausea
- Monitor
- FLT3 mutation test before starting · Blood counts
- ATC
- L01EX13
No doses: the clinician sets them by the current guideline.
Mechanism of action
The crystal shows gilteritinib in the ATP site of the human FLT3 kinase domain.
Gilteritinib binds the ATP pocket of FLT3 and inhibits wild-type and mutant FLT3, including internal tandem duplications, as well as several other receptor tyrosine kinases. Leukaemic blasts lose their growth signal; rapid proliferation and differentiation of myeloid cells can cause differentiation syndrome.
- Gilteritinib fills the ATP pocket of FLT3, including FLT3-ITD
- FLT3 growth signals stop
- Blasts die or mature, which can cause differentiation syndrome
Indications
- Relapsed or refractory acute myeloid leukaemia with an FLT3 mutation in adults. Acute leukaemia (AML and ALL) →
Adverse effects
Common
- Muscle and joint pain
- Fatigue, headache
- Nausea, vomiting, diarrhoea, mouth sores
- Taste change, decreased appetite
- Raised liver enzymes, insomnia
Contraindications
- Hypersensitivity to gilteritinib
Key interactions
- St John's wort
- Can lower gilteritinib levels; avoided.
- Drugs that prolong the QT interval, low potassium or magnesium
- Add to QT risk; ECG and electrolytes are checked.
What is monitored
- FLT3 mutation test before starting
- Signs of differentiation syndrome, especially in the first months
- ECG and electrolytes
- Blood counts, liver tests and creatine kinase
Administration and safety
- Oral tablets swallowed whole with water, not split, crushed or chewed.
- Taken at the same time each day; it is not stopped without the treating team.
Pregnancy and breastfeeding
Avoid in pregnancy. Gilteritinib may harm the fetus: a pregnancy test is done first, women and men use contraception during and for months after treatment, and breastfeeding is stopped.
Nursing care
- Teach the signs of differentiation syndrome and to report them at once.
- Teach to report seizures, severe headache, confusion or vision change.
- Check ECG and electrolytes as ordered.
- Contraception during treatment and for months after by women and men; breastfeeding is stopped.
Pharmacokinetics
- Absorption
- Oral tablets once a day, with or without food.
Test yourself
Think of the answer, then tap the question to see it.
Where on FLT3 does gilteritinib bind?
In the ATP-binding pocket of the kinase.
What is the boxed warning of gilteritinib?
Differentiation syndrome.
In which AML setting is gilteritinib used?
Relapsed or refractory FLT3-mutated AML, as a single agent.
Connections
← Back to the class: FLT3 inhibitors
Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.
Sources: Gilteritinib: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2019); Gilteritinib Fumarate - NCI (National Cancer Institute, 2022); RCSB PDB - 6JQR: Crystal structure of FLT3 in complex with gilteritinib (RCSB Protein Data Bank, 2026); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026).
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Representative model, for educational purposes only.