肺癌EGFR-TKI继发耐药的主要机制与应对策略

doi:10.3760/cma.j.issn.1673-422X.2015.01.015

国际肿瘤学杂志 ›› 2015, Vol. 42 ›› Issue (1): 56-59.doi: 10.3760/cma.j.issn.1673-422X.2015.01.015

肺癌EGFR-TKI继发耐药的主要机制与应对策略

刘思文, 于韶荣, 冯继锋

210009南京医科大学附属江苏省肿瘤医院肿瘤内科

收稿日期:2014-06-18 修回日期:2014-08-04 出版日期:2015-01-08 发布日期:2015-01-07
通讯作者: 冯继锋 E-mail:fjif@vip.sina.com
基金资助:
国家自然科学基金（81372396）

Mechanism and strategy of the secondary resistance to EGFR-TKI in patients with lung cancer

Liu Siwen, Yu Shaorong, Feng Jifeng

Department of Medical Oncology, Jiangsu Province Tumor Hospital Affiliated to Nanjing Medical University, Nanjing 210009, China

Received:2014-06-18 Revised:2014-08-04 Online:2015-01-08 Published:2015-01-07
Contact: Feng Jifeng E-mail:fjif@vip.sina.com

摘要/Abstract

摘要： 表皮生长因子受体-酪氨酸激酶抑制剂（EGFR-TKI）是含有EGFR敏感突变的肺腺癌患者重要的靶向治疗药物，但几乎所有治疗有效的患者最终都会对EGFR-TKI治疗产生继发耐药。目前较公认的耐药机制主要包括T790M突变、MET扩增、PIK3CA突变、人第10号染色体缺失的磷酸酶及张力蛋白同源的基因表达下调、Fas核转录因子-κB激活等。近年针对以上耐药机制，诞生了一批克服EGFRTKI继发耐药的新药物，这些药物大部分仍停留在细胞或动物实验阶段，但也有少数药物获得了比较肯定的临床结果。

Abstract: Epidermal growth factor receptortyrosine kinase inhibitor (EGFRTKI) is one of the most important targeted drugs for lung cancer patients carrying EGFR sensitive mutations. However, almost all patients that are effective to this treatment will eventually develop secondary resistance to EGFRTKI. The most accepted mechanisms of resistance mainly include T790M mutation, MET amplification, PIK3CA mutation, downregulation of PTEN expression and activation of Fastranscription factorκB. Recent years, many new drugs are developed to overcome this resistance. Although most of drugs are in the stages of cell or animal experiment, some new drugs get positive clinical results.

Key words: Lung neoplasms, Drug resistance, neoplasm, EGFR-TKI

中图分类号:

肺肿瘤|抗药性，肿瘤|表皮生长因子受体|酪氨酸激酶抑制剂

刘思文, 于韶荣, 冯继锋. 肺癌EGFR-TKI继发耐药的主要机制与应对策略[J]. 国际肿瘤学杂志, 2015, 42(1): 56-59.

Liu Siwen, Yu Shaorong, Feng Jifeng. Mechanism and strategy of the secondary resistance to EGFR-TKI in patients with lung cancer[J]. Journal of International Oncology, 2015, 42(1): 56-59.

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肺癌EGFR-TKI继发耐药的主要机制与应对策略

Mechanism and strategy of the secondary resistance to EGFR-TKI in patients with lung cancer

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