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To date, malignant neoplasms are the most pressing medical and social problem both in our country and abroad, despite the introduction of innovative technologies in diagnostics, therapy, and prophylactics. Lung cancer is the most common malignant neoplasm worldwide. Since the beginning of the twentieth century, the incidence of lung cancer has increased, and its growth is especially pronounced in industrially developed countries, where it ranks first in the structure of cancer morbidity. In Russia, over the last ten years, the incidence of lung cancer has decreased, but yet more than 1000000 new cases are diagnosed annually, and lung cancer by remains in first place among all malignant neoplasms among men. Tyrosyl-DNA Phosphodiesterase 1 (Tdpl) that result in stalled Topi are commonly employed against cancer. Nowadays, major methods are used for the treatment of patients with lung cancer: surgery, radiation, chemoradiation, drugs, and combined methods. Combination chemotherapy with DNA repair inhibitors can potentially improve response to these widely used chemotherapeutics.