新型酪氨酸激酶抑制剂研究进展

The development of novel tyrosine kinase inhibitors

20世纪末，小分子酪氨酸激酶抑制剂伊马替尼（IM）的研制成功使慢性粒细胞白血病（CML）的治疗迈出了革命性一步。然而，随着时问的推移和临床应用范围的扩大，其耐药现象也逐渐凸现，尤其在CML加速期和急变期病例，已成为影响IM疗效的新问题，这就促使了新型酪氨酸激酶抑制剂的问世。

At the end of last century, the small-molecule selective kinase inhibitor, imatinib mesylate （IM）, was successfully exploited. This resulted in a revolutionary step in the treatment of chronic myeloid leukemia（CML）. However, along with the expansion of its clinical application and the process, drug resistance was commonly observed in patients, especially during a＇ccelerated or blast phases, and has become a significant therapeutic problem in clinical application. The problem has prompted the appearance of novel small molecule tyrosine kinase inhibitors, and its development is reviewed.