第三代EGFR-TKI奥希替尼临床研究进展

奥希替尼是第三代表皮生长因子受体酪氨酸激酶抑制剂（EGFR-TKI），被批准用于治疗EGFR T790M突变阳性的局部晚期或转移性非小细胞肺癌（NSCLC）的抗肿瘤药物。其疗效显著，耐受性较好，副作用较第一、二代EGFR-TKI更易被接受。对已接受其他EGFR-TKI治疗且出现耐药的患者，奥希替尼可为该类患者带来新的选择。2017年3月22日国家食品药品监督管理总局（CFDA）加速批准了阿斯利康公司的甲磺酸奥希替尼片的进口申请。现就奥希替尼的作用机制、上市情况、临床实验、药动学、耐受性和安全性进行综述，为临床应用提供参考。

Clinical research progress of the third generation EGFR-TKI osimertinib

Osimertinib is a third generation epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI). It is an antineoplastic drug approved for the treatment of EGFR T790M mutation positive for locally advanced or metastatic non small cell lung cancer (NSCLC). It is significantly efficiency, well tolerated, with side effects more likely to be accepted compared with the first and second generation of EGFR-TKI. For persons received other EGFR-TKIs which become resistant, osimertinib would bring a new choice for them. On March 22, 2017, CFDA accelerated the approval of the Astrazeneca application of the imported mesylate osimertinib tablets. In this paper, we review the osimertinib in terms of mechanism of action, market experience, clinical trial, pharmacokinetics, safety and tolerability, to provide a reference for clinical application.