Bosutinib is a several-generation TKI

Bosutinib (Bosutinib) is a second-generation tyrosine kinase inhibitor (TKI). It is a breakpoint colony region/Abelson murine leukemia (BCR-ABL) gene TKI approved by the US Food and Drug Administration (FDA) in September 2012. It is used for the second-line treatment of chronic phase, accelerated phase and blast phase chronic myelogenous leukemia. In second-line treatment, bosutinib is effective in some patients with chronic myelogenous leukemia who are resistant or intolerant to imatinib, dasatinib and/or nilotinib, but is not effective in patients whose disease expresses the BCR-ABL T315I point mutation.

In a Phase 3 trial, bosutinib was also compared with imatinib, the standard first-line treatment, in 502 patients with newly diagnosed chronic phase chronic myelogenous leukemia. Complete cytogenetic response (the primary efficacy endpoint) at 12 months was similar for bosutinib and imatinib; therefore, bosutinib is not indicated in the first-line setting. Common adverse events associated with bosutinib include diarrhea, nausea, and vomiting. Grade 3 and 4 adverse events reported in at least 5% of patients treated with bosutinib included increased serum lipase and hepatic transaminases, anemia, thrombocytopenia, neutropenia, and diarrhea.

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.