间变性淋巴瘤激酶抑制剂的研究进展

doi:10.16085/j.issn.1000-6613.2016.12.035

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

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 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 Yalin^1,2,3, LI Wei^1,2,3, WANG Tianyang^1,2,3, ZHOU Xueqin^1,2,3, LIU Dongzhi^1,2,3

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/Abstract

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

中图分类号:

TN41

陈雅琳, 李巍, 汪天洋, 周雪琴, 刘东志. 间变性淋巴瘤激酶抑制剂的研究进展[J]. 化工进展, 2016, 35(12): 3985-3990.

CHEN Yalin, LI Wei, WANG Tianyang, ZHOU Xueqin, LIU Dongzhi. Advances in research on anaplastic lympgoma kinase inhibitors[J]. Chemical Industry and Engineering Progress, 2016, 35(12): 3985-3990.

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间变性淋巴瘤激酶抑制剂的研究进展

Advances in research on anaplastic lympgoma kinase inhibitors

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