LuciGil Gilteritinib Tablets XOSPATA

Product Name: LuciGil

Chinese Name: Gilteritinib

English Name: Gilteritinib

[Summary]

Gilteritinib is a small-molecule inhibitor of multiple receptor tyrosine kinases, including FMS-like tyrosine kinase 3 (FLT3). Gilteritinib demonstrates the ability to inhibit FLT3 receptor signaling and proliferation in cells exogenously expressing FLT3—specifically FLT3-ITD, the tyrosine kinase domain (TKD) mutation FLT3-D835Y, and FLT3-ITD-D835Y—and induces apoptosis in leukemia cells expressing FLT3-ITD.

[Indications]

Gilteritinib is a kinase inhibitor indicated for the treatment of adult patients with relapsed or refractory acute myeloid leukemia (AML) with a FLT3 mutation.

[Specification]

40 mg/tablet; 90 tablets/box.

[Storage]

Store at 20°C to 25°C (68°F to 77°F); excursions are permitted between 15°C and 30°C (59°F and 86°F).

[Dosage and Administration]

Take orally once daily at a dose of 120 mg.

[Adverse Reactions]

The most common adverse reactions (≥20%) are myalgia/arthralgia, elevated transaminases, fatigue/malaise, pyrexia, non-infectious diarrhea, dyspnea, edema, rash, pneumonia, nausea, stomatitis, cough, headache, hypotension, dizziness, and vomiting.

[Contraindications] Hypersensitivity to Gilteritinib or to any of the excipients.

[Precautions]

1. Posterior Reversible Encephalopathy Syndrome (PRES): Discontinue Gilteritinib in patients who develop PRES.

QT Interval Prolongation: Interrupt and reduce the dose of LuciGil in hospitalized patients with a QTcF > 500 msec. Correct hypokalemia or hypomagnesemia prior to and during Gilteritinib administration. 2. Pancreatitis: Interrupt or reduce the dose in patients who develop pancreatitis.

3. Embryo-fetal Toxicity: Gilteritinib may cause fetal harm.

4. Advise pregnant women of the potential risk to the fetus and recommend the use of effective contraception.

[Safety and Efficacy]

Based on the results of the Phase III ADMIRAL trial, which investigated the efficacy and safety of Gilteritinib versus salvage chemotherapy in patients with relapsed or refractory FLT3-mutated (FLT3mut+) AML, the results demonstrated that, compared to the salvage chemotherapy group, the Gilteritinib treatment group showed significantly prolonged overall survival, a doubling of the one-year survival rate, and a doubling of the complete remission rate (with complete or partial hematologic recovery). Regarding safety, the most common Grade ≥3 adverse events in the Gilteritinib treatment group were febrile neutropenia, anemia, and thrombocytopenia.

In October 2018, Gilteritinib was first approved in Japan for the treatment of adult patients with relapsed or refractory AML harboring FLT3 mutations. In late November 2018, LUCIGIL was approved by the U.S. FDA, becoming the first FLT3-targeted agent approved for the treatment of patients with relapsed or refractory AML; this also marked Astellas' entry into the U.S. hematologic oncology treatment landscape. In May 2019, the FDA approved a Supplemental New Drug Application (sNDA) for Gilteritinib, updating the U.S. product labeling to include final overall survival (OS) data from the Phase III ADMIRAL trial. In the European Union, Gilteritinib was approved in October 2019 as a monotherapy for adult patients with relapsed or refractory AML harboring FLT3 mutations (FLT3mut+).