Department of Leukemia, MD Anderson Cancer Center, 1515 Holcombe Boulevard, Unit 428, Houston, TX 77030, USA.
Curr Treat Options Oncol. 2013 Jun;14(2):127-43. doi: 10.1007/s11864-013-0234-8.
Discovery of targeted BCR-ABL protein tyrosine kinase inhibitors (TKI) in the therapy of patients with chronic myeloid leukemia (CML) is perhaps the most popular success story in oncology. Imatinib is the most common TKI modality used as a frontline therapy in CML across the world. Lately, randomized control trials have shown that second-generation TKI, such as dasatinib and nilotinib, are superior to imatinib in terms of tolerability and efficacy. Therefore, second-generation TKI have been used increasingly as a first choice for patients with CML in chronic phase (CML-CP). Recently, ponatinib has shown significant efficacy against the most resistant cases (including those with T315I mutations) with CML. Omacetaxine is a non-TKI agent with a different mechanism of action and has shown benefit in resistant CML. Analysis of other novel agents and newer mechanisms affecting CML stem cells are under exploration. With these developments, the life expectancy of the majority of patients (>90 %) with CML-CP has become comparable to a healthy age-matched individual. The focus has now shifted to achieving faster and deeper responses, considering these parameters as a surrogate for long-term outcome and possibly cures in patients with CML. Adherence to therapy with TKI, proper monitoring by standardized techniques, and adequate use of the available therapies are established rules of managing patients with CML. However, even with these advances, problems of drug resistance, loss of response, kinase domain mutations, transformations in CML (accelerated and blast phase), and patient noncompliance prevail in the community practice. Early identification of resistant cases, feasibility for allogeneic stem cell transplantation (allo-SCT), and enrollment in clinical trials with newer drugs is warranted. This article compares the efficacy and safety results of various TKI and non-TKI modalities and other novel pharmacological agents in the therapy of CML.
发现针对慢性髓性白血病 (CML) 患者的 BCR-ABL 蛋白酪氨酸激酶抑制剂 (TKI) 是肿瘤学中最成功的范例之一。伊马替尼是全球 CML 一线治疗中最常用的 TKI 模式。最近,随机对照试验表明,第二代 TKI,如达沙替尼和尼洛替尼,在耐受性和疗效方面优于伊马替尼。因此,第二代 TKI 已越来越多地作为 CML 慢性期 (CML-CP) 患者的首选药物。最近,ponatinib 已显示出对最耐药病例(包括那些具有 T315I 突变的病例)的显著疗效。Omacetaxine 是一种作用机制不同的非 TKI 药物,在耐药性 CML 中显示出获益。正在分析其他新型药物和影响 CML 干细胞的新机制。随着这些进展,大多数 CML-CP 患者(>90%)的预期寿命已与健康年龄匹配的个体相当。现在的重点已经转移到实现更快和更深的反应,将这些参数作为长期结果和可能治愈 CML 患者的替代指标。遵循 TKI 治疗、通过标准化技术进行适当监测以及充分利用现有治疗方法是管理 CML 患者的既定规则。然而,即使有了这些进展,耐药问题、反应丧失、激酶结构域突变、CML 的转化(加速期和急变期)以及患者不遵医嘱仍然存在于社区实践中。早期识别耐药病例、异体干细胞移植 (allo-SCT) 的可行性以及参与新药物的临床试验是必要的。本文比较了各种 TKI 和非 TKI 模式以及其他新型药理学药物在 CML 治疗中的疗效和安全性结果。