Introduction. The desire of scientists to create a combined oral contraceptive (COC) with improved properties (low risk of venous complications and side effects) led to the discovery of another estrogen — estetrol (E4). Objective. To review the pharmacology, pharmacokinetics, efficacy and tolerability of COCs containing E4 and drospirenone (DRSP). Material and methods. The analysis of foreign literary sources found by keywords in the international databases PubMed, Google Scholar, Medline (search depth 15 years) was carried out, of which 37 articles were included in the review. Results. The innovative COC containing E4/DRSP demonstrated the absence of significant changes in hemostasis markers, a negligi-ble effect on the lipid spectrum and the level of globulin binding sex steroids. It has a beneficial effect on bone mineral density, vascular system, has a neuroprotective effect, as well as a limited effect on the proliferation of normal and malignant tissues in the mammary glands. The Pearl index is 0.47 to 2.65. The frequency of unplanned bleeding and/or spotting is observed in 19.2% of women (cycle 2), by cycle 11 it decreases to 12.8%. Conclusion. Estherol/drospirenone is a fundamentally new hormonal contraceptive that provides high contraceptive efficacy and good tolerability and an acceptable safety profile compared to other COCs. © T.N. BEBNEVA, M.B. KHAMOSHINA, V.E. RADZINSKY.