Bosutinib belongs to the first generation of targeted drugs

Bosutinib is a second-generation tyrosine kinase inhibitor (TKI) and an important upgrade after imatinib. The advent of the first-generation TKI imatinib completely changed the treatment landscape of chronic myelogenous leukemia, transforming it from a "refractory cancer" to a "long-term controllable disease." However, some patients develop drug resistance or intolerance after long-term medication, so second-generation drugs have emerged. Bosutinib, dasatinib and nilotinib together represent the core camp of second-generation TKIs. Compared with imatinib, bosutinib is structurally more tightly bound to BCR-ABL kinase, can effectively inhibit some drug-resistant mutant strains, and has a strong anti-Src kinase effect, thereby improving the overall anti-cancer efficacy.

Second generationThe research and development direction of TKI is to be “more accurate, more efficient and more tolerable”. The optimized molecular structure of bosutinib makes it more capable of penetrating cell membranes and less dependent on liver metabolism, which means that its drug interactions are relatively few and its safety is more controllable. More importantly, it can maintain long-lasting suppression without significantly increasing side effects, providing a new balance point for CML patients taking long-term medication.

Currently, global targeted drugs for the treatment of CML are generally divided into three generations: first-generation imatinib, second-generation (bosutinib, nilotinib, dasatinib), and third-generation (ponatinib, axitinib, etc.). Bosutinib occupies a "backbone position in the second generation" of this system, with both broad-spectrum inhibitory capabilities and good tolerability, making it an important alternative for many doctors when facing drug-resistant patients. With the continuous development of targeted drug technology, bosutinib is gradually being included in the standard treatment guidelines of more countries, becoming a key part of the precise treatment of chronic myelogenous leukemia.

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