Is bosutinib second or third generation?

Bosutinib (Bosutinib) belongs to the second-generation tyrosine kinase inhibitor (TKI). Imatinib was the first tyrosine kinase inhibitor (TKI) used to treat chronic myelogenous leukemia (CML) to improve overall survival (OS), but new TKIs have identified first-line TKIs for newly diagnosed Philadelphia chromosome-positive (Ph+) chronic phase (CP) CML.

Bosutinib was licensed in the United States in 2012 and in Europe in 2013 for the treatment of adults with CP, AP, or BP Ph+ CML who are resistant or intolerant to prior treatment with 1 or more TKIs; in December 2017, the indication was expanded in the United States to include adults with newly diagnosed Ph+ CP CML. Bosutinib is an orally bioavailable SRC/ABL tyrosine kinase inhibitor active against all stages of drug-resistant chronic myeloid leukemia that do not express the T315I or V299L ABL kinase domain mutations. Bosutinib has unique toxicities that are manageable.

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.