非小细胞肺癌EGFR-TKIs耐药分子靶向研究进展.pdf

药物与临床 Drugs and Clinic 非小细胞肺癌EGFR-TKIs耐药分子靶向研究进展 张亚龙，尤嘉琮 天津医科大学总医院，天津市肺癌研究所，天津市肺癌转移与肿瘤微环境重点实验室，天津 300052 ， [摘要] 肺癌是当今世界上对人类健康和生命威胁最大的恶性肿瘤，也是临床治疗疗效最差的恶性肿瘤。非小细胞肺癌 (NSCLC)组织中常可检测到表皮生长因子受体(EGFR)的高表达，而EGFR与肿瘤血管生成、肿瘤细胞扩散及增殖有关，其突变 可以增强NSCLC对酪氨酸激酶抑制剂(EGFR-TKIs)的敏感性。早期的以吉非替尼为代表的EGFR-TKIs借助于高敏感性用于治疗 NSCLC患者效果均较为显著，一度成为治疗非小细胞肺癌的主要治疗药物。但经过长期的使用NSCLC患者对EGFR-TKIs药物 产生了耐药性表现，病情出现复发甚至恶化的情况。因此，对于吉非替尼等EGFR-TKIs耐药性进行研究，以期通过靶向耐药 性相关分子联合治疗NSCLC具有重要意义。本文对EGFR-TKIs耐药相关的分子靶点及针对该靶点的分子抑制剂治疗NSCLC 的 最新研究进展进行综述。 [关键词] 非小细胞肺癌；表皮生长因子受体；酪氨酸激酶抑制剂；靶向治疗 [中图分类号] R974　　[文献标识码]　A　　[文章编号]　1672-2809(2015)14-0014-06 Progress of drug resistance of EGFR-TKIs in non small cell lung cancer ZHANG Ya-long, YOU Jia-cong Tianjin MedicalUniversity General Hospital,Tianjin Lung Cancer Institute,Tianjin Key Laboratory of Lung Cancer Metastasis and Tumor Microenvironment, Tianjin 300052, China [Abstract] Lung cancer is one of the most malignant tumors in the world, which is the biggest threat to human health and life. The expression of epidermal growth factor receptor was detected in non small cell lung cancer tissues, and EGFR was associated with tumor angiogenesis, tumor cell proliferation and proliferation, and the mutation could enhance the sensitivity of NSCLC to tyrosine kinase inhibitors. Early in the treatment of NSCLC patients with the help of the EGFR-TKIs with the help of Gao Mins sensibility is more remarkable, once became the treatment of non small cell lung cancer. But after a long period of use of EGFR-TKIs patients on the drug resistance of NSCLC, the disease has a relapse or even worse. Therefore, it is important to study the drug resistance of EGFR-TKIs in the combination of targeted drug resistance related molecules in order to study the drug resistance of NSCLC. In this article, we reviewed the latest research progress of EGFR-TKIs drug resistance related molecular targets and the molecular inhibitors of NSCLC. [Key words] Non small cell lung cancer; Epidermal grow