用于非小细胞肺癌治疗的第三代EGFR-TKIs研究进展

Research Progress in the Third Generation EGFR-TKIs for Non-small Cell Lung Cancer

肺癌是全球致死率最高的恶性肿瘤,其中非小细胞肺癌(NSCLC)占全部肺癌病例的80%左右。相较于传统化疗,表皮生长因子受体酪氨酸激酶抑制剂(EGFR-TKIs)用于EGFR突变型NSCLC患者,可获得更为卓越的疗效。但是,EGFR-TKIs长期使用会产生获得性耐药,主要机制为EGFRT790M突变。临床研究表明,以奥希替尼、rociletinib和HM61713为代表的第三代EGFR-TKIs对EGFRT790M突变阳性NSCLC具有较好的疗效,为EGFRT790M突变阳性患者的有效治疗带来了新的希望。综述第三代EGFR-TKIs的最新临床研究及耐药机制研究进展。

Lung cancer is a malignant tumor with the highest mortality over the world, in which non-small cell lung cancer（NSCLC） accounts for about 80%. Compared with conventional chemotherapies, epidermal growth factor receptor-tyrosine kinase inhibitors（EGFR-TKIs） have shown remarkable efficacy in NSCLC patients with EGFR mutation. However, acquired resistance due to EGFR T790 M mutation develops after long-term use of EGFR-TKIs. It has been suggested that the third generation EGFR-TKIs such as osimertinib, rociletinib and HM61713 are highly efficacious for EGFR T790M-positive NSCLC, bringing new hope to the effective treatment of EGFR T790M-positive NSCLC patients. In this article, the latest progress in clinical researches and resistance mechanisms of the third generation EGFR-TKIs were reviewed.