Bosutinib/bosutinib Chinese version instructions

1. Generic name:Bosutinib

Product name:BOSULIF

Other names: bosutinib, bosutinib, bosutinib, bosutinib, posutinib (transliteration)

2. Indications

Bosutinib/Bosutinib is a targeted drug. Its indications mainly include the following types of adult patients:

1. Newly diagnosed chronic phase Philadelphia chromosome-positive chronic myelogenous leukemia (CP Ph+CML).

2. Patients aged 1 year old and above, showing chronic phase, accelerated phase (AP) or blast phase (BP) Ph+CML, and cases of drug resistance or intolerance to previous treatments.

3. Usage and dosage

1. The recommended usage of bosutinib is to take it orally once a day with a meal. The tablet should be swallowed whole and should not be broken or cut. The specific dosage is as follows:

1), Adult patients:

(1) For newly diagnosed CP Ph+CML patients, the recommended starting dose is 400 mg daily;

(2) For patients with Ph+ CML in chronic, accelerated or blast phase, and patients who are resistant or intolerant to previous therapy: the recommended starting dose is 500 mg daily.

2) Pediatric patients: The dosage is calculated based on body surface area.

(1) For newly diagnosed CP Ph+CML patients, the recommended dose is 300mg/m2;

(2) For patients with CP Ph+CML who are resistant or intolerant to previous treatments, the recommended dose is 400mg/m2.

2. During the patient's treatment, if adverse reactions occur or the expected treatment effect fails to be achieved, the doctor may adjust or increase the dosage according to the patient's specific condition. For patients who achieve or maintain a response, consider increasing the dose by 100 mg increments, up to a maximum of 600 mg daily. Dose adjustment situations include:

(1) Elevated liver transaminase: If the transaminase value exceeds 5 times the upper limit of normal, the drug should be temporarily discontinued, and treatment should be continued with 400 mg per day after recovery.

(2) Diarrhea: If grade 3 or 4 diarrhea occurs, the medication needs to be suspended and can be resumed after the symptoms are relieved.

(3) Myelosuppression: If the platelet count is lower than 50,000×10^6/L, suspend the medication and adjust the dose according to recovery.

(4) Renal impairment: Adjust the dose according to creatinine clearance, and newly diagnosed chronic phase patients can be adjusted to 200 mg daily.

4. Adverse reactions

In clinical studies of bosutinib , ≥20% of newly diagnosed CP Ph+ CML or CP, AP, or BP Ph+ were resistant or intolerant to prior therapy. In adult patients with CML, the most common adverse reactions are diarrhea, rash, nausea, abdominal pain, vomiting, fatigue, liver dysfunction, respiratory infection, fever and headache; in pediatric patients, the most common adverse reactions are diarrhea, abdominal pain, vomiting, nausea, rash, fatigue, abnormal liver function, headache, fever, decreased appetite and constipation. After bosutinib was launched, adverse events such as thrombotic microangiopathy and Stevens-Johnson syndrome also occurred

5. Supply and storage conditions

Bosutinib tablets are available in three oral strengths: 100mg, 400mg, 500mg; should be stored at 20°C to 25°C (68°F to 77°F), with a permitted temperature deviation of 15°C to 30°C (59°F to 86°F). Tablets should be avoided from being crushed or broken, and unused medicine should be disposed of appropriately in accordance with local regulations.

6. Contraindications

Bosutinib is contraindicated in patients with a history of hypersensitivity to its components to reduce the risk of serious allergic reactions.

7. Mechanism of action

Bosutinib, as a tyrosine kinase inhibitor (TKI), exerts anti-cancer effects by inhibiting BCR-ABL kinase and Src family kinases (such as Src, Lyn and Hck). It is of great significance for the treatment of chronic myelogenous leukemia, especially in the case of resistance to imatinib. Bosutinib can inhibit multiple drug-resistant forms of BCR-ABL kinase.

8. Special groups

In female patients, animal studies have shown that bosutinib use in pregnant women may cause harm to the fetus, so effective contraception is recommended during treatment and for at least two weeks after the last dose. Additionally, breastfeeding is not recommended while taking bosutinib and for at least 2 weeks after the last dose.

Reference materials:https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=adc84ad5-a04d-4fee-9ba8-91f7abd928e3