Introduction to Bosutinib Overview

Bosutinib/Bosutinib. The trade name BOSULIF, also known as bosutinib, bosutinib or posutinib, is an oral targeted drug used to treat chronic myelogenous leukemia (CML). As a second-generation tyrosine kinase inhibitor (TKI), bosutinib is mainly used to treat patients who have developed resistance or intolerance to other TKI treatments. It interferes with the proliferation of CML cells by targeting BCR-ABL kinase, thereby effectively controlling the disease process.

1. Indications

Bosutinib is mainly used to treat adult patients with chronic myelogenous leukemia (CML). The indications include:

1. Newly diagnosed chronic phase (CP) Philadelphia chromosome-positive CML patients

2. Ph+ CML patients 1 year old and older in chronic phase, accelerated phase (AP) or blast phase (BP), especially those who have developed resistance or intolerance to previous treatments.

In clinical studies, bosutinib has shown significant efficacy in CML patients at different stages and can maintain disease control for a long time, providing an effective option for the treatment of drug-resistant CML patients.

2. Usage and dosage

Bosutinib is an oral tablet and is usually recommended to be taken with food to reduce gastrointestinal adverse effects. The recommended dosage is as follows:

1. Newly diagnosedCP Ph+ CML patients: 400mg daily.

2. Patients with CP, AP or BP Ph+ CML who are resistant or intolerant to previous treatment: 500mg daily. If the patient does not experience serious adverse reactions, the dose can be gradually increased, up to a maximum of 600 mg per day.

During treatment, the dose may need to be adjusted based on the patient's individual response and adverse effects. For example, when liver function is abnormal, the drug should be suspended and continued after liver enzymes recover; when severe diarrhea occurs, treatment needs to be suspended until it returns to mild; patients with thrombocytopenia or bone marrow suppression need to adjust the dose based on blood pictures.

3. Adverse reactions

Common side effects of bosutinib include:

1. Diarrhea: The most common adverse reaction usually occurs in the early stages of treatment.

2. Rash, nausea, vomiting, fatigue: these are common side effects during treatment.

3. Abnormal liver function: may be manifested as elevated liver enzymes.

4. Respiratory tract infection: Some patients may develop it.

In addition, adverse reactions such as decreased hemoglobin, decreased platelets, and decreased white blood cell count may be found in laboratory tests. A small number of patients may develop serious adverse events such as thrombotic microangiopathy and Stevens-Johnson syndrome during treatment, so regular monitoring is required during treatment.

4. Storage conditions

Bosutinib should be stored20°C to 25°C, with an allowable deviation of 15°C to 30°C. Medications should be protected from moisture and breakage, and unused medications should be safely disposed of in accordance with local drug recycling regulations.

5. Taboo

This drug should be contraindicated in patients who are allergic to bosutinib or its components. Allergic reactions may include rash, respiratory symptoms, and systemic anaphylaxis. If allergic symptoms occur, stop using bosutinib immediately and seek medical help.

6. Mechanism of action

Bosutinib effectively blocks the proliferation of abnormal white blood cells and inhibits the progression of Ph+ CML by inhibitingBCR-ABL kinase. In addition, bosutinib can also inhibit Src family kinases (including Src, Lyn and Hck), which has good activity against imatinib-resistant BCR-ABL mutations. However, it does not inhibit T315I and V299L mutations, which requires attention during treatment.

Bosutinib’s unique mechanism of action makes it a superior choice among second-generationTKIs, especially for those CML patients who are resistant to traditional therapeutic drugs.

Keyword tags: Bosutinib,Bosutinib, chronic myelogenous leukemia, TKI, Philadelphia chromosome, side effects, drug dosage, BCR-ABL kinase, drug resistance

Reference materials:https://go.drugbank.com/drugs/DB06616