Xospata

Acute myeloid leukemia (AML) — relapsed or refractory, with a FLT3 mutation as detected by an FDA-approved test

120 mg orally once daily until disease progression or unacceptable toxicity
Take with or without food
Strong CYP3A inducers: Increase to 200 mg once daily if needed
Dose reduction: 80 mg once daily for toxicity

Tablets: 40 mg

None listed.

• Differentiation Syndrome: In 3% of patients; can be fatal. Treat with corticosteroids and hemodynamic monitoring.
• Posterior Reversible Encephalopathy Syndrome (PRES): Discontinue if PRES is diagnosed.
• QT Prolongation: QTcF >500 ms in 1.4%. Monitor ECG prior to, at Day 8 and Day 15 of Cycle 1, prior to Cycles 2 and 3, and as clinically indicated.
• Pancreatitis: 4.9% (Grade ≥3: 3.5%). Evaluate in patients developing abdominal pain.
• Embryo-Fetal Toxicity

Myalgia/arthralgia (46%), transaminase increased (41%), fatigue/malaise (36%), fever (35%), noninfectious diarrhea (35%), dyspnea (35%), edema (34%), rash (30%), pneumonia (30%), nausea (27%), stomatitis (26%), cough (24%), headache (21%), hypotension (21%)

Consult the complete prescribing information for a comprehensive list of adverse reactions and their frequencies.

Consult the complete prescribing information for drug interactions, including effects on CYP enzymes, transporters, and concomitant medications that may require dose adjustments or monitoring.

Consult the full prescribing information for pregnancy-related considerations.

Refer to prescribing information for lactation guidance.

Pediatric safety and efficacy information is detailed in the full label.

Dose modifications for organ impairment are specified in the complete prescribing information.

Gilteritinib is an inhibitor of multiple receptor tyrosine kinases including FMS-like tyrosine kinase 3 (FLT3). It inhibits FLT3 receptor signaling and proliferation in cells expressing FLT3 internal tandem duplication (ITD) and tyrosine kinase domain (TKD) mutations (D835Y and D835H). It also inhibits AXL kinase.

Tmax: 4-6 hours. Half-life: approximately 113 hours. Protein binding: 90.7%. Primarily metabolized by CYP3A4. Fecal excretion (64%), urinary excretion (16%).

Clinical efficacy and safety data supporting the approval are available in the full prescribing information and from the clinical trials listed below.

• ADMIRAL — Gilteritinib vs. salvage chemotherapy in FLT3-mutated relapsed/refractory AML. Phase III, n=371.
  🔬 NCT02421939 ↗ 📄 Primary Publication ↗

Xospata has FDA-approved indications across the following cancer types covered on PipelineEvidence: