Gilteritinib is used to treat adult patients with relapsed or refractory acute myeloid leukemia (AML) and FLT3.

Gilentinib Instructions

Product Name: LuciGil           

Manufacturer: Lucius Pharmaceuticals

Chinese name : Gilentinib

English Name: Gilteritinib 

Drug approval number : 07 L 099 5 /23

 

 

【Summary】

Gilteritinib is a small molecule that inhibits multiple receptor tyrosine kinases, including FMS-like tyrosine kinase 3 (FLT3). Gilteritinib has the ability to inhibit FLT3 receptor signaling and proliferation in exogenously expressing FLT3 cells FLT3-ITD, tyrosine kinase domain mutation (TKD) FLT3-D835Y and FLT3-ITD-D835Y, and induce 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 FLT3. 

 

【Specification】  

40 mg/ tablet , 90 tablets /box .

 

【Storage】

 Store at 20 ° C to 25 ° C (68 ° C to 77 ° F) ; short-distance transportation is permitted within the temperature range of 15 to 30 ° C (59 – 86 ° F) .

 

【Usage and Dosage】

Take orally once a day, 120 mg each time .

 

【Adverse Reactions】

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

 

【Taboo】

Hypersensitivity to gilteritinib or any of the excipients.

 

【 Notes 】

1. Posterior reversible encephalopathy syndrome (PRES): Gilteritinib should be discontinued in patients who develop PRES .

Prolonged QT interval: Interrupt and reduce the dose of LUCIGIL in hospitalized patients with QTcF>500msec. Correct 1. Hypokalemia or hypomagnesemia before and during Gilteritinib administration.

2. Pancreatitis: Interrupt and reduce dose in patients who develop pancreatitis.

3. Embryo-fetal toxicity: Gilteritinib can cause fetal damage

4. If the drug is given to pregnant women, inform them of the potential risks to the fetus and use effective contraceptive methods.

 

Safety and efficacy

Based on the results of the Phase III ADMIRAL trial, the trial investigated the efficacy and safety of Gilteritinib compared with salvage chemotherapy in the treatment of patients with relapsed or refractory FLT3mut+AML. The results showed that compared with the salvage chemotherapy group, the overall survival of patients in the Gilteritinib treatment group was significantly prolonged, the one-year survival rate was doubled, and the complete remission rate with complete or partial hematological recovery was doubled. In terms of 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 with FLT3 mutations. At the end of November 2018, LUCIGIL was approved by the US FDA, becoming the first FLT3-targeted agent for the relapsed or refractory AML patient population, marking Astellas' entry into the field of blood cancer treatment in the United States. In May 2019, the FDA approved a supplemental new drug application (sNDA) for Gilteritinib , updating the US product label of Gilteritinib to include final OS data from the Phase III ADMIRAL trial. In the European Union, Gilteritinib was approved in October 2019 for monotherapy in adult patients with relapsed or refractory AML carrying FLT3 mutations (FLT3mut+).