Aim. To analyze the advanced non-small cell lung cancer course during high dose antiestrogen therapy use in complex chemoradiotherapy treatment of patients. Methods and results. With the help of immunohistochemcial method the low expression of estrogen α and progesteron (1.7%) receptors but rather high expression of estrogen β receptors (50.8%) were established. Separation of patients into the groups with the presence or absence of estrogen β receptors allowed to show in clinical terms different mechanisms of action and the possibility of antiestrogen therapy use in the treatment of advanced non-small cell lung cancer. Conclusion. Effectiveness of treatment and overall survival were shown to be statistically better in patients who received high doses of tamoxifen in addition to standard treatment regimens (one-year and median survival – 48.9% and 12 months, respectively) than in patients who received only standard conservative anticancer treatment (one-year and median survival – 28.2% and 9 months, respectively), which was caused by the antiestrogenic effect of tamoxifen and its non-hormonal mechanisms of antitumor action.