非小细胞肺癌EGFR-TKIs及其获得性耐药机制的研究进展

Advances on EGFR-TKIs and acquired resistance mechanisms in non-small cell lung cancer

摘要: EGFR酪氨酸激酶抑制剂（EGFR-TKIs）目前已成为具有EGFR敏感突变的非小细胞肺癌（non-small cell lung cancer, NSCLC）患者的首选一线治疗，然而获得性耐药仍然是其临床应用无法回避的瓶颈问题．本文首先回顾了获得性耐药机制，包括EGFR二次突变、MET基因扩增、IGF1R及HER2扩增，随后对EGFR-TKIs耐药后的治疗选择做了相关阐述，包括一代、二代、三代、四代EGFR-TKIs及联合治疗策略．

Abstract: Nowadays, EGFR tyrosine kinase inhibitors (EGFR-TKIs) have become the first-line treatment for non-small cell lung cancer (NSCLC) patients with EGFR-sensitive mutations. However, acquired drug resistance remains an unavoidable bottleneck in clinical application. Herein, the mechanisms of acquired drug resistance were reviewed first, including secondary mutation of EGFR, amplification of MET gene, IGF1R and amplification of HER2. Then, therapeutic