Ni Jun, Zhang Li
Department of Respiratory Medicine, Peking Union Medical College Hospital, Peking Union Medical College and Chinese Academy of Medical Sciences, Beijing 100730, China.
Chin Med J (Engl). 2016 Feb 5;129(3):332-40. doi: 10.4103/0366-6999.174484.
To guide the optimal selection among first-generation epidermal growth factor receptor-tyrosine kinase inhibitors (EGFR-TKIs) in clinical practice. This review attempted to provide a thorough comparison among three first-generation EGFR-TKIs, namely icotinib, erlotinib, and gefitinib, with regard to their molecular structure, pharmacokinetic parameters, clinical data, adverse reactions, and contraindications.
An electronic literature search of the PubMed database and Google Scholar for all the available articles regarding gefitinib, icotinib, and erlotinib in the English language from January 2005 to December 2014 was used.
The search terms or keywords included but not limited to "lung cancer", "nonsmall cell lung cancer (NSCLC)", "epidemiology", "EGFR", "TKIs", and "optimal selection ".
As suggested by this review, even though the three first-generation EGFR-TKIs share the quinazoline structure, erlotinib had the strongest apoptosis induction activity because of its use of a different side-chain. The pharmacokinetic parameters indicated that both erlotinib and icotinib are affected by food. The therapeutic window of erlotinib is narrow, and the recommended dosage is close to the maximum tolerable dosage. Icotinib enjoys a wider therapeutic window, and its concentration in the blood is within a safe dosage range even if it is administered with food. Based on multiple large-scale clinical trials, erlotinib is universally applied as the first-line treatment. In marked contrast, icotinib is available only in China as the second- or third-line therapeutic approach for treating advanced lung cancer. In addition, it exhibits a similar efficacy but better safety profile than gefitinib.
Although there is a paucity of literature regarding whether icotinib is superior to erlotinib, its superior toxicity profile, noninferior efficacy, and lower cost indicate that it is a better alternative for Chinese patients living with advanced NSCLC.
指导临床实践中第一代表皮生长因子受体酪氨酸激酶抑制剂（EGFR-TKIs）的最佳选择。本综述试图对三种第一代EGFR-TKIs，即埃克替尼、厄洛替尼和吉非替尼，在分子结构、药代动力学参数、临床数据、不良反应和禁忌证方面进行全面比较。
使用PubMed数据库和谷歌学术进行电子文献检索，查找2005年1月至2014年12月期间所有关于吉非替尼、埃克替尼和厄洛替尼的英文可用文章。
检索词或关键词包括但不限于“肺癌”、“非小细胞肺癌（NSCLC）”、“流行病学”、“EGFR”、“TKIs”和“最佳选择”。
本综述表明，尽管三种第一代EGFR-TKIs具有喹唑啉结构，但厄洛替尼因其使用不同的侧链而具有最强的凋亡诱导活性。药代动力学参数表明，厄洛替尼和埃克替尼均受食物影响。厄洛替尼的治疗窗较窄，推荐剂量接近最大耐受剂量。埃克替尼的治疗窗较宽，即使与食物一起服用，其血药浓度也在安全剂量范围内。基于多项大规模临床试验，厄洛替尼被普遍用作一线治疗。与之形成鲜明对比的是，埃克替尼仅在中国作为治疗晚期肺癌的二线或三线治疗方法可用。此外，它显示出与吉非替尼相似的疗效，但安全性更好。
尽管关于埃克替尼是否优于厄洛替尼的文献较少，但其优越的毒性特征、非劣效的疗效和较低的成本表明，它是中国晚期NSCLC患者的更好选择。
