Department of Medical Oncology, Kinki University School of Medicine, 377-2 Ohno-higashi, Osaka-Sayama, Osaka 589-8511, Japan.
Ther Adv Med Oncol. 2010 Sep;2(5):301-7. doi: 10.1177/1758834010370698.
Gefitinib and erlotinib, small-molecule tyrosine kinase inhibitors (TKIs) of the epidermal growth factor receptor (EGFR), were the first molecularly targeted agents to become clinically available for the treatment of non-small cell lung cancer (NSCLC). During the course of their clinical development, it has become clear that the substantial clinical benefit associated with EGFR-TKIs is limited to patients harboring activating mutations of EGFR. Accumulating clinical outcomes in patients with EGFR mutation-positive NSCLC treated with EGFR-TKIs support the notion that this group of individuals constitutes a clinically distinct population. These findings have prompted investigations of the potential role of first-line treatment with EGFR-TKIs in molecularly selected patients, with platinum-based doublet chemotherapy currently being the standard of care for most individuals with advanced NSCLC. This review summarizes the results of recent clinical trials of EGFR-TKIs in selected patients and highlights the efficacy of these drugs in first-line treatment as a form of personalized medicine aimed at improving therapy for advanced NSCLC.
吉非替尼和厄洛替尼是表皮生长因子受体（EGFR）的小分子酪氨酸激酶抑制剂（TKI），它们是首批可供临床应用于治疗非小细胞肺癌（NSCLC）的靶向药物。在其临床开发过程中，很明显，与 EGFR-TKIs 相关的显著临床获益仅限于携带 EGFR 激活突变的患者。在接受 EGFR-TKIs 治疗的 EGFR 突变阳性 NSCLC 患者中积累的临床结果支持这样一种观点，即这群人构成了一个具有明显临床特征的人群。这些发现促使人们研究一线使用 EGFR-TKIs 在分子选择患者中的潜在作用，铂类双联化疗目前是大多数晚期 NSCLC 患者的标准治疗方法。这篇综述总结了最近在选定患者中进行的 EGFR-TKI 临床试验结果，并强调了这些药物在一线治疗中的疗效，这是一种旨在改善晚期 NSCLC 治疗的个体化药物形式。
