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[摘要]
非小细胞肺癌(NSCLC)是严重危害人类生命的疾病之一,其中ALK阳性患者占3%~5%。近年来,众多小分子ALK抑制剂被开发出来,用于ALK阳性NSCLC的治疗。与传统化疗药物相比,第1代ALK抑制剂克唑替尼对ALK阳性NSCLC患者效果显著,已经成为ALK阳性NSCLC治疗的一线用药,但是耐药性的出现限制了其临床应用。新一代ALK抑制剂色瑞替尼和艾乐替尼也相继被FDA批准上市。更多安全性更佳、选择性更高或活性更好的新型ALK抑制剂正在开发中,这些药物有望克服克唑替尼和其他已上市药物的耐药性,从而给ALK阳性NSCLC患者带来更多的选择。
[Key word]
[Abstract]
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.
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