Detailed instructions for giritinib

1. Generic name: Giritinib

Product name:Xospata, Xigatan

Other names: Gilitinib fumarate tablets,Gilteritinib, gilteritinib, ASP-2215, gilitinib

2. Indications:

Gilteritinib is indicated for the treatment of adult patients with relapsed or refractory (R/R) acute myeloid leukemia (AML) who have an FMS-like tyrosine kinase 3 (FLT3) mutation as detected by a treatment-relevant test.

3. Usage and dosage:

1. Before treatment: Doctors will choose to treat AML patients with geritinib based on the presence of FLT3 mutations in the blood or bone marrow. Before starting geritinib, assess blood counts and blood chemistries, including creatine kinase, at least weekly for the first month, every other week for the second month, and monthly during treatment; and perform an electrocardiogram on days 8 and 15 of cycle 1 and before the start of the next two cycles.

2. Recommended dose: The recommended starting dose of gilitinib is 120 mg taken orally once a day, with or without food. Response may be delayed. In the absence of disease progression or unacceptable toxicity, patients are recommended to be treated for at least 6 months to allow time for clinical response.

4. Adverse reactions:

In clinical studies of giritinib, the most common (≥10%) all-grade non-hematologic adverse reactions were increased transaminases, myalgia/arthralgia, fatigue/malaise, fever, mucositis and edema, rash, non-infectious diarrhea, dyspnea, dizziness, hypotension, and vomiting , renal function impairment, abdominal pain, neuropathy, insomnia and dysgeusia; the most common (≥5%) non-hematological serious adverse reactions are fever, dyspnea, renal function impairment, increased transaminases and non-infectious diarrhea; the most common (>1%) adverse reactions leading to discontinuation are increased aspartate aminotransferase and increased alanine aminotransferase.

5. Storage:

Giritinib will be stored at a temperature of 20ºC to 25ºC (68°F to 77°F); excursions allowed between 15ºC and 30ºC (59°F to 86°F). Store in original container until dispensed. Protect from light, moisture and moisture.

6. Taboo:

Gilitinib is contraindicated in patients who are allergic to Gilteritinib or any excipient, and allergic reactions have been observed in clinical trials.

7. Mechanism of action:

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

8. Special groups:

1. Women: Take a pregnancy test for women of reproductive potential within 7 days before starting treatment with giritinib. Pregnant women should take it.Giritinibcan cause harm to the fetus. Therefore, it is recommended that females of reproductive potential use effective contraception during treatment and for 6 months after the last dose; lactating women are advised not to breastfeed during treatment and for 2 months after the last dose.

2. Men: It is recommended that men of childbearing potential use effective contraceptive measures during treatment and within 4 months after the last dose of giritinib.