非小細胞肺癌（NSCLC）是嚴重危害人類生命的疾病之一，其中ALK陽性患者占3%～5%。近年來，眾多小分子ALK抑制劑被開發(fā)出來，用于ALK陽性NSCLC的治療。與傳統(tǒng)化療藥物相比，第1代ALK抑制劑克唑替尼對ALK陽性NSCLC患者效果顯著，已經(jīng)成為ALK陽性NSCLC治療的一線用藥，但是耐藥性的出現(xiàn)限制了其臨床應(yīng)用。新一代ALK抑制劑色瑞替尼和艾樂替尼也相繼被FDA批準上市。更多安全性更佳、選擇性更高或活性更好的新型ALK抑制劑正在開發(fā)中，這些藥物有望克服克唑替尼和其他已上市藥物的耐藥性，從而給ALK陽性NSCLC患者帶來更多的選擇。

Non-small cell lung cancer (NSCLC) is one of the most common causes of death. ALK rearrangements occur in 3%-5% of patients with NSCLC. Over the past decade, multiple small molecule ALK inhibitors have been developed in treatment of ALK⁺ NSCLC. Compared to conventional chemotherapy drugs, the first generation ALK inhibitor crizotinib is currently approved for first line in ALK⁺ NSCLC due to its significant activity. However, the emergence of drug resistance restricted its clinical use. The next generation ALK inhibitor ceritinib and alectinib have been approved by FDA successively. More agents with improved safety, selectivity, and activity profiles are in the pipeline. These agents may have the potential to concur the emerging resistance of crizotinib and other approved drugs, which provides more options for ALK⁺ NSCLC patients.