[Durgical](https://durgical.com/en/) › [DurgiPedia](https://durgical.com/en/durgipedia/) › [Pharmacology](https://durgical.com/en/pharmacology/) › [FLT3 inhibitors](https://durgical.com/en/pharmacology/classes/flt3-inhibitors/) › Gilteritinib # Gilteritinib ## FLT3 inhibitors? FLT3 inhibitors ## High 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. Updated Nov 12, 2026 ## Quick facts **Group** [FLT3 inhibitors](https://durgical.com/en/pharmacology/classes/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. On this page - The basics Mechanism of action - Indications - Adverse effects - Pharmacokinetics - Memory aid - Clinical What the labels mean - Safety Contraindications - Key interactions - What is monitored - Administration and safety - Pregnancy and breastfeeding - Nursing care - Study Test yourself - Connections Connections ## Mechanism of action ✂**FLT3 receptor tyrosine kinase (also other receptor tyrosine kinases)**Gilteritinib ⓘ The crystal shows gilteritinib in the ATP site of the human FLT3 kinase domain. **Target in 3D:** FLT3 receptor tyrosine kinase (also other receptor tyrosine kinases). PDB structure 6JQR (RCSB PDB, public domain). [View the structure at RCSB PDB](https://www.rcsb.org/structure/6JQR) · Drag to rotate · pinch to zoom 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) →](https://durgical.com/en/conditions/acute-leukaemia/) ## Adverse effects ### Common - Muscle and joint pain - Fatigue, headache - Nausea, vomiting, diarrhoea, mouth sores - Taste change, decreased appetite - Raised liver enzymes, insomnia ### Serious (rare, important) - Differentiation syndrome (boxed warning): fever, breathlessness, weight gain, swelling, low blood pressure - Brain swelling syndrome with seizures, headache, confusion or vision change - QT prolongation - Pancreatitis ## 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. ## Memory aid «Gilt for the relapse»: gilteritinib is the single-agent FLT3 inhibitor for relapsed AML; midostaurin goes with first-line chemotherapy. ## 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. [Add to my cards (3)](https://durgical.app/estudiar/?add=/en/pharmacology/gilteritinib/) [More Pharmacology questions →](https://durgical.com/en/practice/?f=pharmacology) ## What the labels mean **High 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… ## Connections ## Related drugs 1 - [Midostaurin](https://durgical.com/en/pharmacology/midostaurin/) ## Related conditions 1 - [Acute leukaemia (AML and ALL)](https://durgical.com/en/conditions/acute-leukaemia/) [← Back to the class: FLT3 inhibitors](https://durgical.com/en/pharmacology/classes/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](https://medlineplus.gov/druginfo/meds/a619003.html) (MedlinePlus (U.S. National Library of Medicine), 2019); [Gilteritinib Fumarate - NCI](https://www.cancer.gov/about-cancer/treatment/drugs/gilteritinibfumarate) (National Cancer Institute, 2022); [RCSB PDB - 6JQR: Crystal structure of FLT3 in complex with gilteritinib](https://www.rcsb.org/structure/6JQR) (RCSB Protein Data Bank, 2026); [ATCDDD - ATC/DDD Index](https://atcddd.fhi.no/atc_ddd_index/?code=L01EX13) (WHO Collaborating Centre for Drug Statistics Methodology, 2026). ## **Spotted a mistake?** We are always improving for the community. Tell us what is wrong and our team will review it. Report a mistake Representative model, for educational purposes only. --- Source: https://durgical.com/en/pharmacology/gilteritinib/ License: CC BY 4.0 (https://creativecommons.org/licenses/by/4.0/). Cite as: DurgiPedia (durgical.com), https://durgical.com/en/pharmacology/gilteritinib/