gilteritinib

Contraindicated in:

Hypersensitivity;
OB: Pregnancy;
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.

Adv. Reactions/Side Effects ⬆ ⬇

CV: hypotension, peripheral edema, QT interval prolongation

Derm: rash

F and E: hypophosphatemia, hypocalcemia, hyponatremia

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

GU: renal impairment

Hemat: DIFFERENTIATION SYNDROME

Metab: hypertriglyceridemia

MS: arthralgia, myalgia, ↑creatine kinase

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

Resp: cough, dyspnea

Misc: fever

Interactions ⬆ ⬇

Drug-drug:

Combined P-glycoprotein (P-gp) 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.
May ↑ levels and toxicity of P-gp substrates, breast cancer resistant protein substrates, and organic cation transporter 1 substrates.

Availability ⬆ ⬇

Route/Dosage ⬆ ⬇

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.

US Brand Names ⬆ ⬇

Action ⬆ ⬇

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

Therapeutic effects:

Improved survival.

Classifications ⬆ ⬇

Therapeutic Classification: antineoplastics

Pharmacologic Classification: kinase inhibitors

Pharmacokinetics ⬆ ⬇

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.

Time/Action Profile ⬆ ⬇

(plasma concentrations)

ROUTE	ONSET	PEAK	DURATION
PO	unknown	4–6 hr	24 hr

Patient/Family Teaching ⬆ ⬇

Instruct patient to take gilteritinib as directed. Take missed doses as soon as remembered on the same day and at least 12 hr 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 light-headedness, 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, light-headedness, 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 cause fetal harm. 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.

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Indications ⬇

Contraind./Precautions ⬆ ⬇