gilteritinib fumarate: clinical use

Prescribing considerations

• Confirm an FLT3-ITD or FLT3-TKD mutation using a validated test before initiation.
• Treatment must be initiated and supervised by a clinician experienced in anticancer therapy.
• Act promptly on suspected differentiation syndrome, PRES, pancreatitis or clinically significant QT prolongation.
• Correct hypokalaemia and hypomagnesaemia and review other QT-prolonging or interacting medicines.
• Severe hepatic impairment has not been adequately studied and use is not recommended.
• Exposure may be increased in severe renal impairment or end-stage renal disease; monitor closely for toxicity and QT prolongation.

Contraindications and cautions

• Hypersensitivity to gilteritinib or any product excipient.

Monitoring

• Blood chemistry, including liver and renal indices, electrolytes and creatine phosphokinase.
• ECG before treatment and during the early treatment period, with additional checks when clinically indicated.
• Pregnancy testing before treatment where relevant.
• Clinical assessment for differentiation syndrome, neurological symptoms, pancreatitis, cardiac toxicity and treatment response.

Clinical pharmacology

Gilteritinib inhibits FLT3 and AXL. It is primarily metabolised by CYP3A4, is a P-gp and BCRP substrate, distributes extensively into tissues and has a long elimination half-life, making interactions and delayed toxicity clinically relevant.

Formulation and product differences

• The selected product is a light-yellow film-coated oral tablet supplied in blisters.
• Tablets must be swallowed whole and should not be broken or crushed.
• Store in the original package to protect from light; no special temperature conditions are required.

Tablet

Route: Oral

Strengths: 40 mg