Gilteritinib

What it is and how it works

Gilteritinib inhibits FMS-like tyrosine kinase 3 (FLT3), including FLT3 internal tandem duplication (ITD) and tyrosine kinase domain (TKD) mutations, as well as AXL. Inhibition of FLT3 signalling blocks proliferation and induces apoptosis of leukaemic cells expressing mutant FLT3.

Indications

Monotherapy for adults with relapsed or refractory acute myeloid leukaemia (AML) with a FLT3 mutation.

Dosage and administration (summary)

Oral, 120 mg once daily with or without food, continued as long as clinical benefit persists and toxicity is acceptable (at least 6 months recommended to allow time for response); dose interruption or reduction may be needed for adverse reactions.

Contraindications

Hypersensitivity to gilteritinib or excipients.

Warnings and precautions

Differentiation syndrome may occur and can be fatal, requiring prompt corticosteroids and haemodynamic monitoring; posterior reversible encephalopathy syndrome, pancreatitis and QT prolongation have been reported, so ECG and electrolytes should be checked before and during treatment. Concomitant strong CYP3A/P-gp inducers should be avoided, and strong CYP3A inhibitors require close monitoring.

Pregnancy

May cause fetal harm; avoid in pregnancy, and effective contraception is required during and for a period after treatment in women and men.

Source: reference summary prepared from the EU SmPC/EPAR, BNF and WHO Model Formulary. The approved product information in Iran governs.