Bosutinib/Bosutinib is the first generation of targeted drugs

Bosutinib/Bosutinib is a tyrosine kinase inhibitor classified as a second-generation targeted drug. It is mainly used to treat chronic myelogenous leukemia (CML), especially Philadelphia chromosome-positive (Ph+) type cases. As a 7-alkoxy-3-quinolonitrile, it has dual inhibitory effects on SRC and ABL tyrosine kinases, which makes bosutinib effective against tumor cell proliferation caused by BCR-ABL fusion proteins.

In the treatment of chronic myelogenous leukemia, the first-generation targeted drug imatinib (Imatinib) came out in the late 1990s, providing new hope for CML patients. However, over time, some patients gradually develop resistance to imatinib, especially those with BCR-ABL mutations. This resistance limits the efficacy of imatinib and there is an urgent need to develop new treatment options.

The emergence of second-generation BCR-ABL inhibitors such as bosutinib marks a new development in the treatment of CML. These drugs can not only effectively inhibit most BCR-ABL mutations, including common mutation sites, but can also overcome the resistance caused by some first-generation drugs. Bosutinib has shown good therapeutic effects in clinical trials, especially for patients who have developed resistance to imatinib or other first-generation drugs, providing a new treatment approach.

The research and development of Bosutinib aims to improve the inhibitory effect on multipleBCR-ABL mutations, thereby improving the survival rate and quality of life of patients. Its dual mechanism of action makes it more advantageous than pure ABL inhibitors in the treatment of CML. Although some resistance mutations (such as T315I and V299L) may still be effective against bosutinib, overall, its ability to suppress other mutations makes it an ideal choice for second-line treatment.

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