国际肿瘤学杂志 ›› 2016, Vol. 43 ›› Issue (7): 532-534.doi: 10.3760/cma.j.issn.1673422X.2016.07.013

• 综述 • 上一篇    下一篇

克唑替尼治疗肺癌的疗效及其耐药后的治疗

朱礼阳, 于忠和   

  1. 陆军总医院全军肿瘤内科诊治中心
  • 出版日期:2016-07-08 发布日期:2016-06-03
  • 基金资助:

    国家自然科学基金(81372489);北京市科技计划(2131100006813032)

Therapeutic effects of crizotinib in lung cancer and the treatment after drug resistance

ZHU  Li-Yang, YU  Zhong-He   

  1. Center for Diagnosis and Treatment of Tumor of the Whole Army, Army General Hospital, Beijing 100700, China
  • Online:2016-07-08 Published:2016-06-03
  • Supported by:

    National Natural Science Foundation of China (81372489); Science and Technology Project of Beijing of China (2131100006813032)

摘要: 以棘皮动物微管相关蛋白4间变性淋巴瘤激酶(EML4ALK)融合基因突变为靶点的酪氨酸激酶抑制剂(TKI)克唑替尼能够显著延长晚期ALK阳性非小细胞肺癌(NSCLC)患者的无进展生存期(PFS),一线、二线单药治疗的中位PFS分别为10.9个月和7.7个月。尽管克唑替尼的初始疗效良好,但大部分患者于治疗1年内出现耐药并显示疾病复发,其原因是ALK融合基因扩增和二次突变。临床试验证实二代ALK抑制剂、联合热休克蛋白等能有效克服克唑替尼耐药。

关键词: 肺肿瘤, 抗药性, 肿瘤, 治疗

Abstract: Crizotinib is a tyrosine kinase inhibitor (TKI), which is a target for echinoderm microtubule associated protein like 4anaplastic lymphoma kinase (EML4ALK). It can prolong the progression free survival (PFS) of ALK positive patients with advanced nonsmall cell lung cancer (NSCLC). The median PFS in the firstline and secondline mPFS is 10.9 months and 7.7 months. However, despite an initial benefit, patients inevitably experience tumor progression, due to the ALK fusion gene amplification and secondary mutations of ALK kinase domain. Clinical trials show the promising efficacy like next generation ALK inhibitors and heat shock protein 90 (HSP90) can overcome acquired resistance.

Key words: Lung neplasms, Drug resistance, neoplasm, Therapy