表皮生长因子受体酪氨酸激酶抑制剂（EGFR-TKI）继发性耐药的机制及对策

摘要

Lung cancer, in which about 80% are non-small cell lung cancers (NSCLC), is one of the most common malignant tumors, and also the leading cause of cancer death currently. The epidermal growth factor receptor (EGFR) driver gene plays an important role in the occurrence and development of lung cancer. In recent years, the epidermal growth factor receptor tyrosine ki-nase inhibitors (EGFR-TKI), especially gefitinib and erlotinib, have played a significant role in the molecular and targeted therapy of NSCLC, and brought in good news for NSCLC patients. However, no matter how effective it is in the short term, the patients will inevitably develop into drug resistance and progressive disease in the long run. In this paper, we made a review on the mechanism of EGFR-TKI secondary drug resistance and the countermeasures on drug resistance after treatment, so as to guide the treatment of NSCLC better.%肺癌是最常见的恶性肿瘤之一，也是目前癌症死亡的首要原因，其中约80％为非小细胞肺癌（Non-small Cell Lung Cancers，NSCLC）。表皮生长因子受体（Epidermal Growth Factor Receptor，EGFR）驱动基因在肺癌的发生发展过程中起重要作用，近年来，以吉非替尼和厄洛替尼为代表的表皮生长因子受体酪氨酸激酶抑制剂（Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors，EGFR-TKI）在 NSCLC 的分子靶向治疗中发挥了巨大的作用，给NSCLC 患者带来了福音。然而，无论近期效果如何，最终患者都不可避免地产生耐药及病情进展。本文主要对近年来EGFR-TKI 继发性耐药的发生机制及耐药后的对策作一综述，以期更好地指导 NSCLC 的治疗。