Introduction to the targeted genes and treatment principles of Bosutinib

Bosutinib is an oral tyrosine kinase inhibitor (TKI) that mainly targets the tyrosine kinase produced by the BCR-ABL fusion gene. BCR-ABLGene fusion is a key pathogenic factor in chronic myeloid leukemia (CML). The abnormal tyrosine kinase encoded by the fusion gene is continuously activated, leading to abnormal proliferation of bone marrow cells and the development of leukemia. In addition, bosutinib inhibits the SRC family of kinases, which also play an important role in the growth and survival of leukemia cells.

Bosutinib competitively binds to the ATP binding site of BCR-ABLtyrosine kinase, blocking its enzymatic activity and inhibiting downstream signaling pathways. This can prevent the proliferation of leukemia cells and induce their apoptosis, achieving the purpose of controlling disease progression. Its inhibitory effect on SRCkinase can also enhance the anti-tumor effect, reduce the occurrence of drug resistance, and improve the comprehensiveness and effectiveness of treatment.

Compared with otherTKIssuch as imatinib and dasatinib, bosutinib is effective against certainBCR-ABL mutants (such as span>T315I mutation) has limited efficacy, but bosutinib has shown good efficacy in the treatment of imatinib-resistant or intolerant CML patients. Its characteristic of simultaneously inhibiting SRC family kinases gives it unique advantages in some relapsed or refractory patients.

Bosutinib is mainly used for patients with chronic myelogenous leukemia in the chronic, intermediate and blast phases, especially those who have poor response to imatinib treatment. During use, blood routine and liver function must be monitored regularly, and gastrointestinal and skin adverse reactions must be paid attention to. Reasonable dose adjustment and side effect management are key to ensuring efficacy and patient quality of life.

Reference materials:https://www.drugs.com/