Must-read for patients: Overview of basic information on dasatinib’s Chinese instructions

1. Name: Dasatinib, Dasatinib, Sprycel, Starase

2. Who can take dasatinib? Indications?

1. Chronic myeloid leukemia (CML):

（1）Dasatinib (Dasatinib) is indicated for the treatment of adult patients with newly diagnosed chronic phase (CP) Philadelphia chromosome-positive (Ph+) CML;

（2）Dasatinib is indicated for the treatment of chronic, accelerated, myeloid or lymphoblastic phasePh+CML that is resistant or intolerant to prior therapy including imatinib(imatinib).

2. Acute lymphoblastic leukemia (ALL):

(1)Dasatinib is indicated for the treatment of Philadelphia chromosome-positive (Ph+) ALL in patients who are resistant or intolerant to previous treatments;

(2)Dasatinib is suitable for the treatment of newly diagnosedPh+ALL in combination with chemotherapy.

It is not known whether dasatinib is safe and effective in children younger than one year old.

3. What are the side effects of dasatinib?

Common side effects of dasatinib include pleural effusion, diarrhea, headache, bleeding, fatigue, fever, rash, infection, nausea, difficulty breathing, cough, abdominal pain, vomiting, musculoskeletal pain, and swelling of the legs and arms and face. After dasatinib was put on the market, adverse events such as atrial fibrillation/atrial flutter, thrombotic microangiopathy, interstitial lung disease, Stevens-Johnson syndrome, nephrotic syndrome, hepatitis B virus reactivation, and hepatotoxicity also occurred.

4. How should you take dasatinib?

1. Recommended dosage:

(1)Adult patients: for chronic phaseFor patients with CML, the recommended dose is 100 mg once daily; for patients with accelerated phase CML, myeloid or lymphoblastic phase CML, or Ph+ ALL, the recommended dose is 140 mg once daily.

(2) Pediatric patients: It needs to be calculated based on body weight. The dose for patients weighing between 10-19kg is 40mg; for patients weighing between 20-29kg, the dose is 60mg; for patients weighing between 30-44kg, the dose is 70mg; for patients weighing at least ≥45kg, the dose is 100mg. Based on changes in body weight, the dose is recalculated every 3 months or more frequently if necessary.

2. Medication management: Dasatinib is an oral tablet that can be taken once a day in the morning or evening with or without food. Tablets should not be crushed, cut, or chewed; swallow whole. Ask your doctor how to take dasatinib tablets if the patient cannot swallow the tablet whole or if the drug is taken by children. Wear latex or nitrile gloves when handling accidentally crushed or broken tablets to prevent contact with the medication.

5. How to store dasatinib?

Dasatinib should be stored at 20°C to 25°C (68°F to 77°F); tolerances are allowed between 15°C and 30°C (59°F and 86°F).

6. How does dasatinib work?

Based on modeling studies, dasatinib is predicted to bind to multiple conformations ofABL kinase. In vitro, dasatinib is active in leukemia cell lines representing imatinib mesylate-sensitive and -resistant disease variants. Dasatinib inhibits the growth of chronic myelogenous leukemia (CML) and acute lymphoblastic leukemia (ALL) cell lines that overexpress BCR-ABL. Under experimental conditions, dasatinib can overcome imatinib resistance caused by mutations in the BCR-ABL kinase domain, activation of alternative signaling pathways involving SRC family kinases (LYN, HCK), and overexpression of multidrug resistance genes.

7. What will happen if you overdose on dasatinib?

In clinical studies, experience with overdose of dasatinib has been limited to isolated cases. It was reported that two patients took the highest dose of 280 mg daily for 1 week and both experienced severe bone marrow suppression and bleeding. Because dasatinib is associated with severe myelosuppression, patients taking doses above the recommended dose should be closely monitored for myelosuppression and given appropriate supportive care. Acute overdose in animals has been associated with cardiotoxicity. Evidence of cardiotoxicity in rodents at single doses ≥100 mg/kg (600 mg/m2) includes ventricular necrosis and valvular/ventricular/atrial hemorrhage. At a single dose of ≥10 mg/kg (120 mg/m2), monkeys' systolic and diastolic blood pressure tended to increase.

8. Who cannot use dasatinib?

Dasatinib is contraindicated in patients allergic to dasatinib or similar drugs.