Lung cancer is the leading cause of cancer-related mortality worldwide. Despiting the great progress on target agents, majority of people who do not harbor a mutation could not get benefit from them. Immunotherapy, through stimulating the body's immune system to improve the antitumor immunity effect, has been a new therapeutic method for non-small cell lung cancer (NSCLC). Study had been reported that immune checkpoint molecules, including programmed death-1 (PD-1)/PD-ligand (L) 1 axis, are closedly related with cancer generation and development, and play a key role on clinical significance of NSCLC. Activation of PD-1/PD-L1 pathway contributes to tumor immune escape, and block PD-1/PD-L1 pathway can enhance endogenous antimuor immunity. Currently increasing clinical trials suggested that immune checkpoint inhibitors, including anti-PD-1 and anti-PD-L1 monoclonal antibodies turned out to be beneficial and safe in NSCLC. Here, we provide a review on the progress of PD-1/PD-L1 pathway and immune checkpoint inhibitors in NSCLC. 非小细胞肺癌(non-small cell lung cancer, NSCLC)是肿瘤相关性死亡率第一的恶性肿瘤。虽然近年来靶向治疗进展迅速,但很多基因未突变的患者不能从中受益。目前免疫治疗已成为肿瘤治疗的新方向,它能通过刺激机体免疫系统提高抗肿瘤免疫效应。研究显示免疫检查点分子:程序性死亡分子1(programmed death 1, PD-1)、程序性死亡分子1配体(PD-1 ligand, PD-L1),与肿瘤发生、发展密切相关,在NSCLC中有重要的临床意义。PD-1/PD-L1信号通路的激活有助于肿瘤免疫逃逸,而阻断该通路可以增强机体内源性抗肿瘤免疫效应。目前越来越多的临床试验显示免疫检查点阻滞剂抗PD-1、抗PD-L1抗体在治疗NSCLC中的良好疗效性和安全性。本综述旨在回顾及总结近年来PD-1/PD-L1信号通路及其阻滞剂在NSCLC中的研究进展。