晚期非小細胞肺癌的治療選擇，除了傳統的化學治療以外，在2003年以及2006年以後又分別增加了gefitinib以及erlotinib這兩個可逆性的(reversible)表皮生長因子接受器酪胺酸酶抑制劑(epidermal growth factor receptor tyrosine kinase inhibitor, EGFR-TKl)。過去這兩個藥物的使用時機，都是在病人接受過化學治療以後腫瘤仍持續惡化，才會拿來當作第二線或是第三線的治療藥物；但是近年來由於腫瘤分子生物學的發展，知道若病人的腫瘤是帶有特定的表皮生長因子接受器酪胺酸酶基因突變（EGFR mutation)，則這些病人對於EGFR-TK的治療反應特別好，尤其是exon 21 L858R mutation以及deletion in exon 19兩個常見的突變。因此近年來的EGFR-TK治療發展方向，都是在特定的病人族群用EGFR-TK取代傳統的化學治療來當作第一線的治療。本篇文章將針對這個主題來回顧近年來大型的第三期臨床試驗結果，並且說明最新的非小細胞肺癌治療趨勢。此外，也會介紹第二代的不可逆性的(irreversible)表皮生長因子接受器酪胺酸酶抑制劑afatinib目前在臨床上的使用。

Gefitinib and erlotinib are reversible tyrosine kinase inhibitors (TKIs) of epidermal growth factor receptor (EGFR), and have been available in 2003 and 2006, respectively in Taiwan for treatment of advanced non-small cell lung cancer (NSCLC) after failing prior cytotoxic chemotherapy. Objective responses have been observed frequently in patients with NSCLC harboring activating EGFR mutations, mainly, the exon 21 L858R mutation and deletions in exon 19. In recent years, EGFR-TKIs have been evaluated as the first-line treatment of advanced NSCLC harboring activating EGFR mutations. Here in we review phase III trials focusing on this topic, and elucidate the trend of the treatment for NSCLC, as well as the clinical development of second-generation irreversible EGFR-TKI, afatinib.