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ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ANTINEOPLASTIC AGENTS › PROTEIN KINASE INHIBITORS › Other protein kinase inhibitors
gilteritinib
L01EX13
Adult Dosing
- Acute myeloid leukemia (AML): 120 mg orally once daily with or without food for at least 2 cycles; continue until disease progression or unacceptable toxicity
Pediatric Dosing
- Safety and efficacy in pediatric patients have not been established
Indications
- Relapsed or refractory acute myeloid leukemia (AML) with a FLT3 mutation (FLT3-ITD or FLT3-TKD) as detected by an FDA-approved test
Mechanism of Action
- Small-molecule inhibitor of FLT3 receptor tyrosine kinase; inhibits FLT3 receptor signaling and induces apoptosis in leukemia cells expressing FLT3-ITD, mutant FLT3-TKD, FLT3-D835Y, and FLT3-F691L
Contraindications
- Hypersensitivity to gilteritinib or any of its excipients
Adverse Reactions
- Elevated transaminases
- Fatigue
- Fever
- Edema
- Musculoskeletal pain
- Diarrhea
- Dyspnea
- Nausea
- Cough
- Rash
- Headache
- Dizziness
- Vomiting
- QT prolongation
- Posterior reversible encephalopathy syndrome (PRES)
- Differentiation syndrome
Drug Interactions
- Strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole) may increase gilteritinib exposure
- Strong or moderate CYP3A4 inducers (e.g., rifampin, carbamazepine, phenytoin, St. John's wort) may significantly decrease gilteritinib efficacy
- Drugs that prolong the QT interval (e.g., antiarrhythmics, fluoroquinolones, triazole antifungals) increase the risk of ventricular arrhythmias
Curated Content: Needs Vetting Before Put to Clinical Use