Gilteritinib

Products

Gilteritinib was approved in the form of film-coated tablets in the United States in 2018, in the EU in 2019, and in many countries in 2020 (Xospata).

Structure and properties

Gilteritinib (C₂₉H₄₄N₈O₃, M_r = 552.7 g/mol) is present in the drug as gilteritinib fumarate, a light yellow to yellow powder or crystals that are sparingly soluble in water.

Effects

Gilteritinib (ATC L01XE54) has antitumor, antiproliferative, and proapoptotic properties. The drug belongs to the tyrosine kinase inhibitors. The effects are based on inhibition of FLT3 (FMS-like tyrosine kinase 3) and AXL. FLT3 is involved in white blood cell growth and proliferation. Gilteritinib has a long half-life of approximately 113 hours.

Indications

For the treatment of adult patients with relapsed or refractory acute myeloid leukemia (AML) with FLT3 mutations.

Dosage

According to the SmPC. Tablets are taken once daily, independent of meals.

Contraindications

• Hypersensitivity

For complete precautions, see the drug label.

Interactions

Gilteritinib is a substrate of CYP3A4 and corresponding drug-drug interactions may occur.

Adverse effects

The most common potential adverse effects include:

• Diarrhea, nausea, constipation.
• Fatigue, dizziness
• Cough, shortness of breath
• Peripheral edema
• Altered laboratory parameters
• Low blood pressure
• Pain in the limbs, weakness, joint pain, muscle pain.