【摘要】 表皮生长因子受体(EGFR)酪氨酸激酶抑制剂(TKIs)是具有EGFR基因敏感突变的晚期非小细胞肺癌(NSCLC)患者的一线治疗药物。第一、二代EGFR-TKIs可有效治疗EGFR敏感突变的NSCLC,EGFR第20号外显子的T790M突变是第一、二代EGFR-TKIs的主要耐药机制。以奥西替尼为代表的第三代EGFR-TKIs治疗耐药后出现T790M突变的患者疗效显著,给晚期肺癌患者带来更多的生存获益。然而第三代EGFR-TKIs仍不可避免地出现耐药。本文对第三代EGFR-TKIs治疗晚期NSCLC耐药机制及应对策略的研究进展进行综述。更多还原

【Abstract】 Targeted therapy of epidermal growth factor receptor tyrosine kinase inhibitor(EGFR-TKIs) has been the standard modality as the first-line treatment of advanced EGFR-mutated non-small cell lung cancer(NSCLC). The first-and second-generation EGFR-TKIs have shown significant efficacy in NSCLC patients with EGFR-sensitive mutations and EGFR T790 M mutation is the main resistance mechanism of the firstand second-generation EGFR-TKIs. The third-generation EGFR-TKIs, represented by osimertinib, has been approved to overcome the EGFR T790 M mutation in patients who are resistant to the first-or second-generation TKIs, which brings more survival benefits for patients with advanced NSCLC. However, the development of acquired drug resistance is inevitable. In this review, we summarize the research progress in resistance mechanisms of advanced NSCLC to the third-generation EGFR-TKIs and the potential overcoming strategies.更多还原