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Drugs. 2016 Jul;76(11):1153-7. doi: 10.1007/s40265-016-0606-z.
Olmutinib (Olita(TM)) is an oral, third-generation epidermal growth factor receptor tyrosine kinase inhibitor (EGFR TKI) that is being developed by Boehringer Ingelheim and Hanmi Pharmaceutical Co. Ltd for the treatment of non-small cell lung cancer (NSCLC). Third-generation EGFR TKIs with covalent binding to the receptors demonstrate irreversible enzymatic inhibition of activating EGFR mutations and T790M mutation (a common reason for acquired EGFR TKI resistance), while sparing wild-type EGFR. In December 2015, olmutinib was granted breakthrough therapy designation in NSCLC by the US FDA. In May 2016, olmutinib received its first global approval in South Korea for the treatment of patients with locally advanced or metastatic EGFR T790M mutation-positive NSCLC. This article summarizes the milestones in the development of olmutinib leading to this first approval.
奥希替尼（Olita(TM)) 是一种口服的第三代表皮生长因子受体酪氨酸激酶抑制剂（EGFR TKI），由勃林格殷格翰和韩美制药有限公司共同开发，用于治疗非小细胞肺癌（NSCLC）。具有共价结合受体的第三代 EGFR TKI 可对激活 EGFR 突变和 T790M 突变（获得性 EGFR TKI 耐药的常见原因）进行不可逆的酶抑制，同时保留野生型 EGFR。2015 年 12 月，奥希替尼被美国 FDA 授予 NSCLC 突破性治疗药物认定。2016 年 5 月，奥希替尼在韩国获得全球首次批准，用于治疗局部晚期或转移性 EGFR T790M 突变阳性 NSCLC 患者。本文总结了奥希替尼开发过程中的重要里程碑，直至获得首次批准。
