非小细胞肺癌吉非替尼耐药机制及治疗研究进展.PDF

非小细胞肺癌吉非替尼耐药机制及治疗研究进展 1 2 2* 赵佳 ，陈建业 ，汤建才 (1.川北医学院药学院，四川 南充 637000 ；2.川北医学院生化教研室，四川 南充 637000)  摘要：吉非替尼是一种选择性表皮生长因子受体酪氨酸激酶抑制剂(EGFR-TKIs) ，主要用于治疗既往接受过化学治疗或不 适于化疗的局部晚期或转移性非小细胞肺癌，治疗效果显著，但最终多数患者会发生耐药。近年来研究表明，其耐药机 制主要有表皮生长因子受体二次突变、代偿信号通路的建立及调节因子基因表达的改变、肿瘤微环境的改变等。本文围 绕吉非替尼的耐药机制做一综述，为肿瘤的靶向治疗提供参考。 关键词：吉非替尼；抗药性；肿瘤；非小细胞肺癌 中图分类号：R965 文献标志码：A 文章编号：1007-7693(2017)06-0923-05 DOI: 10.13748/ki.issn1007-7693.2017.06.030 引用本文：赵佳, 陈建业, 汤建才. 非小细胞肺癌吉非替尼耐药机制及治疗研究进展[J]. 中国现代应用药学, 2017, 34(6): 923-927. Research Progress on the Mechanism of Gefitinib Resistance and Treatment in Non-small Cell Lung Cancer 1 2 2* ZHAO Jia , CHEN Jianye , TANG Jiancai (1.Department of Pharmacy, North Sichuan Medical College, Nanchong 637000, China; 2.Department of Biochemistry, North Sichuan Medical College, Nanchong 637000, China) ABSTRACT: Gefitinib, a kind of epidermal growth factor receptor tyrosine kinase inhibitors (EGFR-TKIs), which is used to the treatment of ever received chemotherapy or unsuitable for chemotherapy in advanced or metastatic non-small cell lung cancer, although the treatment effect is remarkable, in the end, most patients with drug resistance will happen. In recent years, the research showed that the resistant mechanisms are connected with a secondary mutation in exon 20 of EGFR, T790M, the establishment of compensatory signaling pathway and regulating factor to the change of gene expression, and the changes of the tumor microenvironment etc. This review aims to study the mechanisms of drug resistance based on the recent researches, and providing a reference for targeting therapy of tumor. KEY WORDS: gefitinib; drug resistance; neoplasm; non-small cell lung cancer 吉非替尼是一种表皮生长因子受体酪氨酸激