Gilternib Gilteritinib Tablets

【Key Drug Information】

Generic Name: Gilteritinib Fumarate Tablets

Brand Name: Shigatan / Gilternib

English Name: Gilteritinib Fumarate Tablets

Dosage Form & Strength: Oral Tablets; 40 mg/tablet; 90 tablets/box

Manufacturer: Everest Pharma Ltd (Everest Pharma, Bangladesh)

【Indications & Mechanism of Action】

Indications: Indicated for the treatment of adult patients with relapsed or refractory acute myeloid leukemia (AML) who have a FMS-like tyrosine kinase 3 (FLT3) mutation (including internal tandem duplications [ITD] or tyrosine kinase domain [TKD] mutations), as detected by a validated assay.

Mechanism of Action: Gilteritinib is an FLT3/AXL kinase inhibitor that blocks tumor cell proliferation and induces apoptosis by inhibiting the FLT3 signaling pathway.

【Dosage and Administration】

Patient Selection: An FLT3 mutation must be detected in peripheral blood or bone marrow samples prior to initiating treatment.

Recommended Dosage: The recommended starting dose is 120 mg (3 tablets) taken orally once daily.

Administration: May be taken with or without food. Tablets should be swallowed whole with water; they must not be broken or crushed. Take the medication at approximately the same time each day.

Treatment Cycle: Each treatment cycle consists of 28 days. Treatment should be continued until disease progression or unacceptable toxicity occurs.

Dosage Adjustment: The physician will adjust the dosage based on efficacy and the severity of adverse reactions. If specific remission criteria are not met after 4 weeks of treatment, the dose may be increased to 200 mg (5 tablets) once daily, provided the patient tolerates the treatment. [Important Warnings and Precautions] (Dosage Adjustment Guidelines)

The table below lists adverse reactions requiring special attention, along with corresponding principles for dosage management:

Dosage Adjustment (Due to Adverse Reactions):

Adverse Reaction Grade | Adjustment Plan

Grade ≥3 Non-hematologic Toxicity (e.g., elevated liver enzymes, QTc prolongation, edema, etc.) | Suspend treatment; once resolved to Grade ≤2, resume at 80 mg/day.

Recurrence of Grade ≥3 Toxicity | Suspend treatment; resume at 40 mg/day; if still not tolerated, permanently discontinue the drug.

QTc Interval >500 ms | Suspend treatment; correct electrolyte abnormalities; assess concomitant medications; resume at a reduced dose once resolved.

Note: No adjustment to the starting dose is required based on age, gender, or mild-to-moderate hepatic or renal impairment; however, use with caution in patients with severe hepatic impairment (Child-Pugh Class C).

[Adverse Reactions]

Based on a study involving 319 patients, the most common adverse reactions (incidence ≥10%) included:

Laboratory Abnormalities: Elevated alanine aminotransferase (ALT), elevated aspartate aminotransferase (AST), anemia, thrombocytopenia, elevated creatine phosphokinase (CPK).

Clinical Events: Diarrhea, nausea, fatigue.

Serious Adverse Reactions: Differentiation syndrome (potentially life-threatening), Reversible Posterior Leukoencephalopathy Syndrome (RPLS), QTc interval prolongation, febrile neutropenia, etc.

[Drug Interactions]

The current prescribing information does not list specific interacting drugs; however, while taking Gilteritinib, patients should inform their physician before starting or discontinuing any other prescription medications, over-the-counter drugs, or herbal products.

[Use in Specific Populations]

Hepatic Impairment: No dosage adjustment is required for patients with mild-to-moderate impairment; use is not recommended for patients with severe hepatic impairment.

Renal Impairment: No dosage adjustment is required for patients with mild, moderate, or severe impairment; however, clinical experience in patients with severe impairment is limited.

Geriatric Patients: No dosage adjustment is required for patients aged ≥65 years.

Pediatric and Adolescent Patients: Safety and efficacy have not been established; use is not recommended. Pregnant and Lactating Women: Based on its mechanism of action, this medication may cause harm to the fetus. Therefore, effective contraceptive measures must be employed, and breastfeeding should be avoided, both during treatment and for at least one week following the final dose.

【Storage and Pricing Information】

Storage: Protect from light; keep tightly sealed; store at temperatures below 25°C. Shelf life: 48 months.

【Important Note】

This information leaflet synthesizes the official product prescribing information and is intended to serve as a comprehensive reference for you; it does not substitute for a professional physician's prescription or medical guidance. All treatment decisions must be made by a hematologist following a comprehensive assessment, including genetic testing.

Product Specifications

Product Name: Gilteritinib Fumarate Tablets 40 mg × 90 Tablets/Box

Common Name: Gilteritinib Fumarate Tablets

Active Ingredient: Gilteritinib Fumarate

Dosage Form: Oral Film-Coated Tablets

Specification: 40 mg/tablet; 90 tablets/box

Manufacturer: Everest Pharma Ltd (Bangladesh)

Indications: For the treatment of adult patients with relapsed or refractory Acute Myeloid Leukemia (AML) who are confirmed to harbor a FMS-like tyrosine kinase 3 (FLT3) mutation (including ITD or TKD mutations), as detected by a validated assay.

Dosage and Administration: Core Instructions

Administration: For oral use; may be taken with or without food. Swallow tablets whole; do not break, crush, or chew. Take the medication at the same time each day.

Missed Dose: If more than 12 hours remain before the next scheduled dose, take the missed dose as soon as possible. If less than 12 hours remain before the next scheduled dose, skip the missed dose and resume the regular schedule the following day; do not take a double dose.

Vomiting: If vomiting occurs, do not take an additional dose; resume the regular dosing schedule the following day.

Recommended Dosage

Starting Dose: 120 mg (3 tablets × 40 mg) once daily. Each treatment cycle consists of 28 days. Continue treatment until there is no longer clinical benefit or until unacceptable toxicity occurs. Dosage Adjustment: If CR/CRp/CRi is not achieved after 4 weeks of treatment, the dose may be increased to 200 mg (5 tablets × 40 mg) once daily. In the event of Grade 3 or higher toxicity, treatment must be suspended; once the toxicity resolves, the dose may be reduced to 80 mg or 120 mg once daily (adjusted according to the type of adverse reaction).

Special Populations: No dosage adjustment is required for patients with mild to moderate hepatic or renal impairment; use is not recommended in patients with severe hepatic impairment. No dosage adjustment is required for patients aged ≥65 years; use is not recommended in children.

Hematopoietic Stem Cell Transplantation (HSCT): Treatment should be suspended 1 week prior to the conditioning regimen. For patients who have undergone successful transplantation, have achieved CR, and have experienced no acute GVHD of Grade 2 or higher, treatment may be resumed 30 days after HSCT.