Impressive response rates and good tolerability have led imatinib 400 mg once a day to become the standard frontline therapy for chronic myeloid leukemia (CML) patients. However, approximately one-third of the treated patients do not respond in an optimal manner to this drug, and the appropriate type and rhythm of CML monitoring, as well as the correct action to be undertaken in case of failure or suboptimal responses to imatinib therapy have been published in specific recommendations by European Leukemia Net and National Comprehensive Cancer Network. Failure and also cytogenetic suboptimal responses strongly demand for a change in treatment and for a switch from imatinib to one of the two second-generation tyrosine kinase inhibitors (TKIs) so far registered, dasatinib and nilotinib, for which efficacy as second-line therapy in imatinib-resistant or intolerant cases has been clearly demonstrated in phase II studies, and for which 4-year updates are now available. Other TKIs, at the moment, still under clinical investigation for imatinib-resistant patients include bosutinib and the next-generation TKI ponatinib. Different efficacy and safety criteria characterize each of the mentioned compounds and may help to decide on the one to be preferably used in individual patients.

令人印象深刻的反应率和良好的耐受性使伊马替尼 400 mg 每天一次成为慢性粒细胞白血病 (CML) 患者的标准一线治疗。然而，大约三分之一的接受治疗的患者对这种药物没有最佳反应，CML 监测的适当类型和节律，以及在伊马替尼治疗失败或反应不佳时应采取的正确行动已在欧洲白血病网和国家综合癌症网络的具体建议中发表。失败和细胞遗传学次优反应强烈要求改变治疗方法并从伊马替尼转换为迄今为止注册的两种第二代酪氨酸激酶抑制剂（TKI）中的一种，达沙替尼和尼罗替尼，在 II 期研究中清楚地证明了作为二线治疗对伊马替尼耐药或不耐受病例的疗效，并且现在可以获得 4 年更新。目前仍在对伊马替尼耐药患者进行临床研究的其他 TKI 包括博舒替尼和下一代 TKI 波纳替尼。不同的功效和安全性标准表征了每种提到的化合物，并且可能有助于决定一种更适合用于个体患者的化合物。