化工进展 ›› 2016, Vol. 35 ›› Issue (12): 3985-3990.DOI: 10.16085/j.issn.1000-6613.2016.12.035

• 生物与医药化工 • 上一篇    下一篇

间变性淋巴瘤激酶抑制剂的研究进展

陈雅琳1,2,3, 李巍1,2,3, 汪天洋1,2,3, 周雪琴1,2,3, 刘东志1,2,3   

  1. 1 天津大学化工学院, 天津 300072;
    2 天津化学化工协同创新中心, 天津 300072;
    3 天津市功能精细化学品技术工程中心, 天津 300072
  • 收稿日期:2016-05-10 修回日期:2016-05-24 出版日期:2016-12-05 发布日期:2016-12-05
  • 通讯作者: 刘东志,教授,博士生导师,研究方向为精细化工产品,E-mail:dzliu@tju.edu.cn。
  • 作者简介:陈雅琳(1990-),女,硕士研究生。
  • 基金资助:

    天津市科技创新平台计划(14TXGCCX00017)项目。

Advances in research on anaplastic lympgoma kinase inhibitors

CHEN Yalin1,2,3, LI Wei1,2,3, WANG Tianyang1,2,3, ZHOU Xueqin1,2,3, LIU Dongzhi1,2,3   

  1. 1 School of Chemical Engineering and Technology, Tianjin University, Tianjin 300072, China;
    2 Collaborative Innovation Center of Chemical Science and Engineering, Tianjin 300072, China;
    3 Tianjin Engineering Research Center of Functional Fine Chemicals, Tianjin 300072, China
  • Received:2016-05-10 Revised:2016-05-24 Online:2016-12-05 Published:2016-12-05

摘要: 研究发现非小细胞肺癌的形成与多种致癌突变密切相关,其中间变性淋巴瘤激酶重排备受关注,针对棘皮动物微管相关蛋白质4-间变性淋巴瘤激酶融合基因的抑制剂克唑替尼对于治疗晚期ALK阳性非小细胞肺癌患者是有效的,2011年获得美国食品药品监督管理局批准上市,但出现了耐药性,第二代间变性淋巴瘤激酶抑制剂的出现,克服了耐药机制,并显示出治疗非小细胞肺癌患者的活性。本论文按化学结构的不同介绍了克唑替尼、Ceritinib、Alectinib、Brigatinib、RXDX-101、PF-06463922、ASP3026、X-396、CEP-37440等间变性淋巴瘤激酶抑制剂及临床研究等,为非小细胞肺癌的靶向治疗药物的开发提供了参考。

关键词: 非小细胞肺癌, EML4-ALK基因重排, 克唑替尼

Abstract: Researchers have found that multiple oncogenic driver multations are closely related with the progression and prognosis of NSCLC. In the era of molecular targeted treatment,rearrangements in anaplastic lymphoma kinase(ALK)gene and echinoderm microtubule-associated protein-like 4(EML4)gene were applied in patients with non-small cell lung cancer(NSCLC). Crizotinib,an ALK inhibitor,is effective in treating advanced ALK-positive NSCLC,and the US Food and Drug Administration(FDA)approved it for treating ALK-positive NSCLC. Several mechanisms of acquired resistance to crizotinib have recently been reported. Second-generation ALK inhibitors were developed to overcome these resistance mechanisms and showed activity against ALK positive NSCLC. The latest development of crizotinib,ceritinib,alectinib etc. were reviewed.

Key words: non small cell lung cancer, echinoderm microtubule-associated protein-like 4-anaplastic lymphoma kinase rearrangement, crizotinib

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