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埃克替尼,一种选择性表皮生长因子受体酪氨酸激酶抑制剂,用于治疗非小细胞肺癌。

Icotinib, a selective EGF receptor tyrosine kinase inhibitor, for the treatment of non-small-cell lung cancer.

作者信息

Tan Fenlai, Shi Yuankai, Wang Yinxiang, Ding Lieming, Yuan Xiaobin, Sun Yan

机构信息

Betta Pharmaceuticals Co., Ltd, Hangzhou, China.

出版信息

Future Oncol. 2015;11(3):385-97. doi: 10.2217/fon.14.249.

DOI:10.2217/fon.14.249
PMID:25675121
Abstract

Advanced non-small-cell lung cancer (NSCLC) is the main cause for cancer-related mortality. Treatments for advanced NSCLC are largely palliative and a benefit plateau appears to have reached with the platinum-based chemotherapy regimens. EGF receptor (EGFR) tyrosine kinase inhibitors gefitinib, erlotinib and afatinib came up with prolonged progression-free survival and improved quality of life, especially in EGFR-mutated patients. Icotinib is an oral selective EGFR tyrosine kinase, which was approved by China Food and Drug administration in June 2011 for treating advanced NSCLC. Its approval was based on the registered Phase III trial (ICOGEN), which showed icotinib is noninferior to gefitinib. This review will discuss the role of icotinib in NSCLC, and its potential application and ongoing investigations.

摘要

晚期非小细胞肺癌(NSCLC)是癌症相关死亡的主要原因。晚期NSCLC的治疗主要是姑息性的,基于铂类的化疗方案似乎已达到疗效平台期。表皮生长因子受体(EGFR)酪氨酸激酶抑制剂吉非替尼、厄洛替尼和阿法替尼可延长无进展生存期并改善生活质量,尤其是在EGFR突变的患者中。埃克替尼是一种口服选择性EGFR酪氨酸激酶,于2011年6月获中国食品药品监督管理局批准用于治疗晚期NSCLC。其获批基于注册的III期试验(ICOGEN),该试验表明埃克替尼不劣于吉非替尼。本综述将讨论埃克替尼在NSCLC中的作用及其潜在应用和正在进行的研究。

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