Abstract: Lung cancer is the leading cause of cancer death and non-small cell lung cancer (NSCLC) accounts for >85% of all cancer deaths. Although chemotherapy and targeted therapy have improved clinical outcomes, prognosis remains poor. With the development of immunotherapy, the treatment strategy for patients with NSCLC has changed. Nivolumab, a human immunoglobulin G4 monoclonal antibody, was the first programmed cell death protein-1 (PD-1) inhibitor drug to be approved for treating advanced NSCLC and has become the primary drug for treating advanced NSCLC. However, there remains a lack of clinical biomarkers to predict the efficacy of nivolumab. In this review, we discuss the progress of therapeutic mechanisms, pharmacokinetics, pharmacology, clinical trials of monotherapy and combined therapy, adverse events, and predictive biomarkers.