Information about Gilteritinib
Gilteritinib is an orally available small molecule inhibitor of FMS-like tyrosine kinase 3 (FLT3) which is used as an antineoplastic agent in the treatment of acute myeloid leukemia with FLT3 mutations.
Liver safety of Gilteritinib
Gilteritinib is associated with a moderate rate of serum aminotransferase elevations during therapy and is suspected to cause rare instances of clinically apparent acute liver injury.
Mechanism of action of Gilteritinib
Gilteritinib (gil" te ri' ti nib) is a potent small molecule inhibitor of FLT3 (FMS-like tyrosine kinase 3), a tyrosine kinase receptor that is mutated in to up one-third of patients with acute myeloid leukemia (AML). The mutated FLT3 activates an intracellular signaling cascade of RAS-MEK-PI3K-AKT-STAT-5, promoting unregulated cell growth and proliferation. Gilteritinib has been found to inhibit mutated FLT3 and in several clinical trials was found to induce objective responses in a proportion of patients with refractory AML with detectable FLT3 mutations.
FDA approval information for Gilteritinib
Gilteritinib received accelerated approval for this indication in the United States in 2018 and is available in tablets of 40 mg under the brand name Xospata.
Dosage and administration for Gilteritinib
The recommended dose is 120 mg once daily, continued until progressive disease or intolerable toxicity occurs.
Side effects of Gilteritinib
Side effects are common and can include fatigue, myalgia, arthralgia, fever, diarrhea, nausea, abdominal pain, dizziness, headache, hypotension, cough and stomatitis. Uncommon, but potentially severe side effects include posterior reversible encephalopathy syndrome, febrile neutropenia and sepsis, QTc prolongation, pancreatitis, and embryo-fetal toxicity.