Is bosutinib a fourth-generation targeted drug?

Bosutinib (Bosutinib) is not a fourth-generation targeted drug. Bosutinibis a new second-generation tyrosine kinase inhibitor (TKI) targetingBcr-Abl protein. In September 2012, the U.S. Food and Drug Administration (FDA) approved bosutinib for the treatment of adults with chronic myelogenous leukemia who are resistant or intolerant to previous treatments, including chronic phase (CP), accelerated phase (AP) or blast phase (BP)Philadelphia chromosome-positive (Ph+) CML.

Bosutinib, formerly known asSKI-606, is an orally active dual inhibitor of Src and Abl tyrosine kinases, both of which are thought to be involved in the development of malignant tumors. Src is a protein kinase that regulates intracellular signal transduction pathways and is involved in the control of cell growth, differentiation and migration. Studies have shown that the Bcr-Abl domain interacts and activates Lyn and Hck Src kinases through phosphorylation and direct binding. This dual inhibition may help overcome certain types of drug resistance that often occur in advanced stages of chronic myelogenous leukemia. Due to the sequence homology and structural similarity between Src and Abl binding domains, ATP inhibitors targeting the inactive conformation of Src are also effective Abl inhibitors.

The originator drug of bosutinib is not marketed in the country, so it cannot be included in medical insurance. Currently, the original drugs sold overseas include Turkish version and European version. The price of the Turkish version may be more than RMB 2,000 per box of 500mg*28, and the price of the European version may be more than RMB 30,000 (the price may fluctuate due to the exchange rate). There are also bosutinib generic drugs produced overseas in other countries. Their pharmaceutical ingredients are basically the same as those of the original drug. The price of 500mg*30 per box may be more than 2,000 yuan (the price may fluctuate due to the exchange rate), and the price is relatively cheap.