• Relapsed or refractory acute myeloid leukemia (AML) with a FMS-like tyrosine kinase 3 (FLT3) mutation.

Contraindicated in:

• Hypersensitivity
• OB: Pregnancy (may cause fetal harm)
• Lactation: Lactation.

Use Cautiously in:

• Electrolyte abnormalities
• Rep: Women of reproductive potential and men with female partners of reproductive potential
• Pedi: Safety and effectiveness not established in children.

CV: hypotension, peripheral edema, QT interval prolongation.

Derm: rash.

F and E: hypocalcemia, hyponatremia, hypophosphatemia.

GI: pancreatitis, abdominal pain, constipation, ↑liver enzymes, metallic taste, mucositis, nausea, vomiting, diarrhea.

GU: renal impairment.

Hemat: DIFFERENTIATION SYNDROME.

Metab: hypertriglyceridemia.

MS: arthralgia, myalgia, ↑ creatine kinase.

Neuro: neuropathy , POSTERIOR REVERSIBLE ENCEPHALOPATHY SYNDROME (PRES), dizziness, fatigue, headache, insomnia.

Resp: cough, dyspnea.

Misc: fever.

Drug-Drug:

• Combined P-glycoprotein and strong CYP3A inducers may ↓ levels and effectiveness; avoid concurrent use.
• Strong CYP3A inhibitors may ↑ levels and risk of toxicity; consider an alternative therapy that does not inhibit CYP3A.
• May ↓ levels of escitalopram, fluoxetine, and sertraline; avoid concurrent use.

• Tablets: 40 mg;

• PO (Adults): 120 mg once daily; continue treatment for 6 mo (provided that disease progression and/or unacceptable toxicity do not occur) to determine clinical response.

Xospata

• Inhibits FLT3 receptor signaling and cell proliferation, and induces apoptosis in leukemic cells expressing FLT3–ITD.

• Improved survival in AML.

Therapeutic Classification: antineoplastics

Pharmacologic Classification: kinase inhibitors

Absorption: Absorption ↓ and delayed with high-fat food.

Distribution: Extensively distributed to tissues.

Metabolism/Excretion: Primarily metabolized via the liver by the CYP3A4 isoenzyme. Primarily excreted in the feces (64.5%), 16.4% excreted in urine.

Half-life: 113 hr.

(plasma concentrations)

• Instruct patient to take gilteritinib as directed. Take missed doses as soon as remembered on the same day and at least 12 hrs before next scheduled dose; do not double doses. Advise patient to read Medication Guide before starting therapy and with each Rx refill in case of changes.
• Advise patient to notify health care professional immediately if signs and symptoms of differentiation syndrome fever, cough, dizziness or lightheadedness, rapid weight gain, trouble breathing, swelling of arms or legs, rash, decreased urination), PRES (headache, decreased alertness, confusion, reduced eyesight, blurred vision, other visual problems), QT prolongation (dizziness, lightheadedness, feeling faint), or pancreatitis occur.
• Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care professional before taking other medications.
• Rep: May be teratogenic. Advise females of reproductive potential to use effective contraception during and for at least 6 mo after last dose and to avoid breastfeeding during and for at least 2 mo after last dose of gilteritinib. Advise males with female partners of reproductive potential to use effective contraception during and for at least 4 mo after last dose.

GIL-te-RI-ti-nib

NDC Code^*

• 0469- Astellas Pharma US, Inc.
  • 0469-1425- Xospata
    • 0469-1425-90- 1 BOTTLE in 1 CARTON (0469-1425-90) > 90 TABLET in 1 BOTTLE