Gilteritinib is an oral small molecule tyrosine kinase inhibitor that exerts anti-tumor effects by selectively inhibiting the activity of FMS like tyrosine kinase 3 (FLT3). Its mechanism of action includes blocking FLT3 receptor signaling, inhibiting leukemia cell proliferation, and inducing cell apoptosis.

1、 Drug name

1. Common name: Gilteritinib

2. Product Name: XOSPATA ®

2、 Indications

Used to treat adult patients with relapsed or refractory acute myeloid leukemia (AML) confirmed by FDA approved testing to have FLT3 mutations.

3、 Specifications and characteristics

Specification: 40mg/tablet

Appearance: Round film coated sheet.

4、 Main components

1. Active ingredient: Jiretinib Fumarate (equivalent to 40mg Jiretinib Free Base)

2. Accessories: mannitol, hydroxypropyl cellulose, magnesium stearate, etc.

5、 Usage and dosage

1. Recommended dosage: 120mg orally once daily, can be taken with food or on an empty stomach.

2. Medication requirements: Swallow the entire tablet, do not break, crush or chew. If missed, it should be taken as soon as possible on the same day and at least 12 hours after the next dose.

6、 Dose adjustment

Dose needs to be adjusted based on toxicity reactions:

1. QT interval prolongation: Discontinue administration when QTcF>500ms, and reduce to 80mg after recovery.

2. Pancreatitis: Suspend medication and reduce to 80mg after symptom relief.

3. Other toxicity levels ≥ 3: Suspend administration until it returns to ≤ 1, then reduce to 80mg.

7、 Medication precautions

1. Dietary impact: A high-fat diet may delay drug absorption, but does not significantly affect drug efficacy.

2. Vomiting treatment: If vomiting occurs after taking medication, there is no need to take the next dose according to the original plan.

3. Monitoring requirements: Regular blood routine, electrolyte, electrocardiogram, etc. should be tested before and during treatment.

8、 Medication for special populations

1. Pregnant women: Prohibited, may cause fetal damage, effective contraceptive measures should be taken.

2. Breastfeeding period: Breastfeeding is prohibited during the treatment period and within 2 months after discontinuation of medication.

3. Elderly: No need to adjust dosage, but close monitoring of adverse reactions is necessary.

9、 Adverse reactions

Common symptoms (≥ 20%) include muscle/joint pain (42%), elevated transaminase levels (41%), fatigue (40%), fever (35%), diarrhea (34%), dyspnea (34%), rash (30%), pneumonia (30%), etc.

10、 Contraindications

Prohibited for individuals allergic to gefitinib or excipients; Allergic reactions have been reported in clinical trials.

11、 Drug interactions

1. Strong CYP3A inducers (such as rifampicin): Avoid combination therapy as it may reduce efficacy.

2. Strong CYP3A inhibitors (such as itraconazole): Close monitoring of adverse reactions is required when used in combination.

3. 5HT2B/σ receptor targeted drugs (such as fluoxetine): may weaken the efficacy of the latter and avoid combination therapy.

12、 Storage method

1. Store at 20 ° C-25 ° C (short-term storage at 15 ° C-30 ° C is allowed).

2. Keep in original packaging, away from light and moisture, and keep out of reach of children.

Gilteritinibinformation