Yuan Ying, Li Xiao-Fen, Chen Jia-Qi, Dong Cai-Xia, Weng Shan-Shan, Huang Jian-Jin
Department of Medical Oncology, the Second Affiliated Hospital, Zhejiang University School of Medicine, Hangzhou, People's Republic of China.
Onco Targets Ther. 2014 May 28;7:841-52. doi: 10.2147/OTT.S34124. eCollection 2014.
Past studies have demonstrated that epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors can significantly improve clinical outcomes in patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) and sensitive EGFR gene mutations. Gefitinib (Iressa(®)), the first oral EGFR tyrosine kinase inhibitor, has been shown to be more effective and better tolerated than chemotherapy either in first-line or second-line treatment for patients with advanced NSCLC harboring sensitive EGFR mutations. Conversely, among patients with wild-type EGFR, gefitinib is inferior to standard chemotherapy in both the first-line and second-line settings. Further, gefitinib is effective in patients with brain metastases because of its low molecular weight and excellent penetration of the blood-brain barrier. In this review, we summarize the current data from clinical trials with gefitinib and appraise its role in the management of locally advanced or metastatic NSCLC.
既往研究表明，表皮生长因子受体（EGFR）酪氨酸激酶抑制剂可显著改善局部晚期或转移性非小细胞肺癌（NSCLC）且EGFR基因突变敏感患者的临床结局。吉非替尼（易瑞沙（®））作为首个口服EGFR酪氨酸激酶抑制剂，已显示在一线或二线治疗中，对于携带敏感EGFR突变的晚期NSCLC患者比化疗更有效且耐受性更好。相反，在EGFR野生型患者中，吉非替尼在一线和二线治疗中均劣于标准化疗。此外，吉非替尼因其分子量低且血脑屏障穿透性极佳，对脑转移患者有效。在本综述中，我们总结了吉非替尼临床试验的当前数据，并评估其在局部晚期或转移性NSCLC治疗中的作用。
