Bosutinib/bosutinib Chinese usage guide

1. Generic name Bosutinib

Product name:BOSULIF

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

2. Indications:

Bosutinib is a targeted therapy indicated for adult patients with:

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

2) Patients aged 1 year old and above, showing Ph+CML in chronic phase, accelerated phase or blast phase, and have developed resistance or intolerance to previous treatments.

3. Usage and dosage

1) Recommended dosage: Take orally once a day with a meal. The tablet must be swallowed whole and cannot be broken. The details are as follows:

Adult:

Newly diagnosedCP Ph+CML patients: starting dose 400 mg/day;

Chronic phase, accelerated phase or blast phasePh+CML patients, as well as patients who are resistant or intolerant to previous treatment: starting dose is 500 mg/day.

Children:

Calculate dose based on body surface area.

Newly diagnosedCP Ph+CML patients: 300mg/m² is recommended;

Patients with CP Ph+CML who are resistant or intolerant to previous treatments: 400mg/m² is recommended.

2) Dosage adjustment: If adverse reactions occur or the therapeutic effect is not achieved during treatment, the doctor can adjust the dose according to the specific situation. The maximum dose can be increased to 600 mg/day. Adjustments include:

Elevated liver enzymes: If it exceeds the upper limit of normal5 times, temporarily stop taking the drug and continue with 400 mg after recovery.

Diarrhea:For grade 3 or 4 diarrhea, medication needs to be suspended and resumed after symptoms improve.

Myelosuppression: When platelets fall below50,000×10^6/L, medication is suspended and the dose is adjusted.

Kidney function impairment: adjusted according to creatinine clearance, patients in newly diagnosed chronic phase can be adjusted to 200 mg/day.

4. Adverse reactions

In clinical trials,Common adverse reactions in ≥20% of newly diagnosed adult CP Ph+CML patients who were resistant or intolerant to treatment were: diarrhea, rash, nausea, abdominal pain, vomiting, fatigue, abnormal liver function, respiratory infection, fever and headache. Common adverse reactions in pediatric patients include diarrhea, abdominal pain, vomiting, nausea, rash, fatigue, abnormal liver function, headache, fever, decreased appetite and constipation. Serious adverse events observed post-marketing include thrombotic microangiopathy and Stevens-Johnson syndrome.

5. Supply and storage conditions

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

6. Contraindications

It is contraindicated for use by those who are allergic to bosutinib ingredients to reduce the risk of severe allergic reactions.

7. Mechanism of action

Bosutinib, as a tyrosine kinase inhibitor, exerts anti-cancer effects by inhibitingBCR-ABL kinase and Src family kinases (such as Src, Lyn, Hck). It plays an important role in the treatment of chronic myelogenous leukemia, especially in the case of imatinib resistance, effectively inhibiting multiple drug-resistant forms of BCR-ABL kinase.

8. Special groups

Female patients should be aware that animal studies have shown that use of bosutinib during pregnancy may cause harm to the fetus and it is recommended that effective contraception be used during treatment and for at least two weeks after the last dose. Bosutinib is also not recommended during breastfeeding until at least two weeks after the last dose.

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