Detailed Dosing Guide for Dasatinib

1. Dasatinib (Dasatinib) applicable population and main treatment areas

Chronic myeloid leukemia (CML) patients:

(1)Adult CML patients who are newly diagnosed, in the chronic phase and carry Philadelphia chromosome-positive (Ph+).

(2)Ph+ CML patients who are resistant or intolerant to imatinib and other other treatments in chronic, accelerated phase, myeloid or lymphoblastic phasePh+ CML.

Acute lymphoblastic leukemia (ALL) patients:

(1)Ph+ALL patients who have developed resistance or intolerance to previous treatmentsPh+ALL.

(2)Used in combination with chemotherapy drugs to treat newly diagnosedPh+ALL patients.

NOTE: The safety and effectiveness of dasatinib in children younger than one year of age have not been established.

2. Possible side effects of dasatinib

Tasatinib may be associated with the following side effects: pleural effusion, diarrhea, headache, bleeding of any kind, fatigue, fever, rash, increased risk of infection, nausea, difficulty breathing, cough, abdominal pain, vomiting, muscle and bone pain, and edema of the limbs and face. Postmarketing surveillance has also reported more serious side effects such as atrial fibrillation/flutter, thrombotic microangiopathy, interstitial lung disease, Stevens-Johnson syndrome, nephrotic syndrome, hepatitis B virus reactivation, and hepatotoxicity.

3. How to take dasatinib

(1) Adult dosage:

Chronic phaseCML: 100mg daily.

Accelerated phase, myeloid or lymphoblastoid phaseCML, or Ph+ ALL: 140mg daily.

(2) Children’s dosage: Adjust according to weight and recalculate every 3 months, or more frequently if necessary.

10-19kg: 40mg/day.

20-29kg: 60mg/day.

30-44kg: 70mg/day.

≥45kg: 100mg/day.

(3) Medication Tips: Dasatinib is an oral tablet that can be taken once a day with or without food. Tablets should be swallowed whole and not crushed, cut or chewed. If the patient is unable to swallow the tablet whole or has children who need the medication, please consult a doctor for guidance.

4. Storage conditions of dasatinib

Please store dasatinib20°C to 25°C, with fluctuations allowed between 15°C and 30°C.

5. Mechanism of action of dasatinib

Dasatinib binds to multiple conformations ofABL kinase and has shown activity in in vitro experiments against leukemia cell lines, including those that are sensitive or resistant to imatinib. It inhibits the growth of CML and ALL cell lines that overexpress BCR-ABL and can overcome imatinib resistance caused by specific gene mutations or overexpression of multidrug resistance genes.

6. Consequences of overdose of dasatinib

Overdose of dasatinib may result in severe myelosuppression and bleeding. Patients should be closely monitored for bone marrow function and receive supportive care if necessary. The cardiotoxicity observed in animal experiments was particularly pronounced at high doses.

7. Contraindicated groups for dasatinib

This medicine is contraindicated in patients who are allergic to dasatinib or any of its ingredients. Before starting treatment, the doctor should ask the patient in detail about his or her allergy history.