肺癌為國內癌症死因第一位，非小細胞肺癌(non-small cell lung cancer, NSCLC) 占肺癌85%-90%，大部分病人被診斷時已屬晚期。基於可作用分子標記的個人化治療(personalizedtherapy) 已完全改變了晚期非小細胞肺癌治療的前景，多種分子標靶可用於靶向這些致癌驅動的因子(oncogenic drivers)，自2011 年間變性淋巴瘤激酶(anaplastic lymphoma kinase, ALK)抑制劑核准上市後，陸續有新一代ALK 抑制劑發展出來，能夠增加顱內活性或是針對特定耐藥性基因進行突破。使大多數病人對治療產生反應，並且延長病人之無病惡化存活期(progression-free survival, PFS)。本文針對目前已經核准上市之第一代至第三代的ALK 抑制劑藥物之臨床試驗及治療結果進行文獻回顧。

Lung cancer is the leading cause of cancer death in Taiwan. Non-small cell lung cancer is around 85%-90% of lung cancer. Most patients those have been diagnosed as NSCLC already have advanced stage. Personalized therapy already changes the prospective of advanced NSCLS treatment. There are various multiple molecule targets to oncogenic drivers, such as EGFR, ALK and TKIs. Since Crizotinib as the first ALK TKI for the treatment of ALK-positive metastatic NSCLC in 2011, new generation of ALK inhibitors consequently are being developed until today. The new generation of ALK-TKIs are developed to overcome the acquired resistance to therapy and to improve efficacy in ALK inhibitor pretreated ALK-positive patients, intracranial activity and keep extending the time to progression. This review mentions treatment options of established phase III clinical trials from 1st- generation to 3rd-generation ALK inhibitors.