Xospata

gilteritinib (gilteritinib) instructions
Common name: gilteritinib
Trade name: Xospata
Full names: gilteritinib, gilteritinib fumarate, gilteritinib, gilteritinib, gi lteritinib, Xospata

Indications:
XOSPATA is a kinase inhibitor used to treat adult patients with relapsed or refractory acute myeloid leukemia (AML) combined with FLT3.

Usage and dosage:
Take orally once a day, 120 mg each time.

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 gitertinib or any excipients.

Precautions:
Posterior Reversible Encephalopathy Syndrome (PRES): Discontinue XOSPATA in patients who develop PRES.
Prolonged QT Interval: Interrupt and reduce the dose of XOSPATA in hospitalized patients with QTcF>500msec. Correct hypokalemia or hypomagnesemia before and during administration of XOSTATA.
Pancreatitis: Interrupt and reduce dose in patients who develop pancreatitis.
Embryofetal toxicity: XOSPATA can cause fetal damage
If administered to pregnant women, inform the fetus of the potential risks and use effective contraception.

Storage:
Store XOSPATA tablets at 20°C to 25°C (68°F to 77°F); allow movement between 15°C and 30°C (59°F to 86°F)
Keep in original container.

Mechanism of action:
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 signal transduction and proliferation in cells expressing FLT3 exogenously, FLT3-ITD, tyrosine kinase domain mutations (TKD) FLT3-D835Y and FLT3-ITD-D835Y, and induce apoptosis in leukemia cells expressing FLT3-ITD.

Safety and Efficacy:
Based on results from the Phase III ADMIRAL trial, which investigated the efficacy and safety of Xospata compared with salvage chemotherapy in patients with relapsed or refractory FLT3mut+ AML. The results showed that compared with the salvage chemotherapy group, patients in the Xospata treatment group had significantly longer overall survival, doubled the one-year survival rate, and doubled the rate of complete remission with complete or partial hematological recovery. In terms of safety, the most common grade ≥3 adverse events in the Xospata treatment group were febrile neutropenia, anemia, and thrombocytopenia.
In October 2018, Xospata was the first to be approved in Japan for the treatment of adult patients with relapsed or refractory AML harboring FLT3 mutations. At the end of November 2018, Xospata was approved by the US FDA, becoming the first FLT3-targeted agent for patients with relapsed or refractory AML, and also marked Astellas' entry into the US blood cancer treatment field. In May 2019, the FDA approved a supplemental new drug application (sNDA) for Xospata, updating Xospata's U.S. product label to include final OS data from the Phase III ADMIRAL trial. In the EU, Xospata was approved in October 2019 as a monotherapy for the treatment of adult patients with relapsed or refractory AML carrying FLT3 mutations (FLT3mut+).