The paper summarizes information on targeted therapy with epidermal growth factor (EGFR) inhibitors used in neoadjuvant and adjuvant regimens for the treatment of non-small-cell lung cancer (NSCLC). It analyzes the data available in the literature and describes the authors’ clinical case and the results of treating the NSCLC patient with EGFR exon 21 L858R mutation who received neoadjuvant treatment with gefitinib as a component of combination therapy. Targeted therapy is shown to have an advantage over cytostatics as a neoadjuvant in lung cancer. Whether EGFR tyrosine inhibitors may be used as an adjuvant regimen after their previous preoperative administration remains controversial. The use of targeted agents in NSCLC patients with EGFR mutation and locally advanced tumor may become an alternative to chemotherapy and should be studied in large-scale studies.