Abstract: Of all malignant tumors, lung cancer has the highest morbidity and mortality worldwide. In recent years, with the emergence of new drugs and the optimization of treatment models, the prognosis of patients with lung cancer has improved. Neoadjuvant therapy refers to the treatment provided to patients with a resectable tumor prior to surgery. This treatment can reduce tumor volume and downstage the tumor; it is also reported to remove circulating tumor cells and micrometastasis, and enable patients to achieve longer survival. Targeted therapy and immunotherapy have been used as the first-line treatment for non-small cell lung cancer (NSCLC). Some clinical trials have proposed the use of targeted therapy and immunotherapy as neoadjuvant therapy. This review intends to summarize the efficacies and potential risks of neoadjuvant targeted therapy and immunotherapy in patients with NSCLC and to discuss future developments in neoadjuvant therapy.