Yanada Masamitsu, Ohno Ryuzo, Naoe Tomoki
Department of Hematology and Oncology, Nagoya University Graduate School of Medicine, 65 Tsurumai, Showa-ku, Nagoya, 466-8550, Japan.
Aichi Cancer Center, Nagoya, Japan.
Int J Hematol. 2009 Jan;89(1):3-13. doi: 10.1007/s12185-008-0223-z. Epub 2008 Dec 18.
The advent of imatinib, a selective inhibitor of the ABL tyrosine kinase, has revolutionized the treatment of Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+ ALL). Combined with chemotherapy, imatinib exerts remarkable efficacy in patients with newly diagnosed disease with a complete remission (CR) rate of 95% and a survival rate of 55% at 3 years. Profound eradication of leukemia cells not only provides patients with a better chance for receiving allogeneic hematopoietic stem cell transplantation during first CR but also contributes to durable CR even without transplantation. Despite such improvement, however, relapse does occur, mainly owing to acquisition of resistance. Growing comprehension of the molecular mechanisms of resistance to imatinib has led to the development of novel BCR-ABL inhibitors that yield higher affinity for BCR-ABL and/or potent inhibitory activity against other target molecules such as SRC family kinases. The second-generation ABL kinase inhibitors, namely dasatinib and nilotinib, are already showing clinical activity in patients with imatinib-resistant Ph+ ALL, and other novel agents are undergoing preclinical and early clinical evaluation. Further improvement in treatment results will be achieved by identifying each patient's disease profile based on information obtained before and during treatment and by optimizing subsequent treatment accordingly.
伊马替尼是一种ABL酪氨酸激酶的选择性抑制剂,它的出现彻底改变了费城染色体阳性急性淋巴细胞白血病(Ph+ ALL)的治疗方法。与化疗联合使用时,伊马替尼对新诊断的患者具有显著疗效,完全缓解(CR)率为95%,3年生存率为55%。深度清除白血病细胞不仅为患者在首次CR期间接受异基因造血干细胞移植提供了更好的机会,而且即使不进行移植也有助于实现持久的CR。然而,尽管有这样的改善,复发仍然会发生,主要是由于获得了耐药性。对伊马替尼耐药分子机制的深入理解导致了新型BCR-ABL抑制剂的开发,这些抑制剂对BCR-ABL具有更高的亲和力和/或对其他靶分子(如SRC家族激酶)具有强大的抑制活性。第二代ABL激酶抑制剂,即达沙替尼和尼洛替尼,已在伊马替尼耐药的Ph+ ALL患者中显示出临床活性,其他新型药物正在进行临床前和早期临床评估。通过根据治疗前和治疗期间获得的信息确定每位患者的疾病特征,并相应地优化后续治疗,将实现治疗效果的进一步改善。