Estetrol: The Future of Hormonal Contraception Unveiled: A literature review


Grebennikova G.A. Jaimbetova A.P. Baimurzayeva L.G. Ilmuratova S.Kh.
31 December 2024Kaz Med Print LLP

Reproductive Medicine (Central Asia)
2024#2024Issue 466 - 74 pp.

Relevance: The evolution of oral contraceptives is a milestone in women’s reproductive health history. This revolutionary medical advance has profoundly impacted society, changing views on sexuality, family planning, and women’s empowerment. Over the years, contraceptives have undergone significant changes in composition, dosage, and administration methods. A good contraceptive should be highly effective, provide reliable cycle control, have a low incidence of side effects, and have non-contraceptive benefits. Innovative research in the field of hormonal contraception continues to this day. The recent introduction of a combined oral contraceptive (COC) that includes a new native estrogen, estetrol (E4), in combination with drospirenone (DRSP), offers a promising future for hormonal contraception. The study aimed to summarize the data on the characteristics of estetrol and its use as a contraceptive. Materials and Methods: The search for the review was conducted across multiple databases, including Medline, Scopus, Web of Science, Google Scholar, Springer, PubMed, ResearchGate, and CyberLeninka. The analysis encompassed publications in both English and Russian, specifically covering the period from 2014 to 2024. Results: E4 is a native estrogen produced by the liver of the human fetus during pregnancy, has high bioavailability, is not metabolized by cytochrome 450 enzymes, and is the end product of its pathway. E4 is the first known Natural Estrogen with Selective Tissue activity (NEST). A recently launched COC containing E4 in combination with DRSP has demonstrated its effectiveness as a contraceptive, providing reliable control of the menstrual cycle. It is characterized by stable and predictable menstrual bleeding, which is an important factor for the tolerability of the drug in women. In addition, this contraceptive has a high level of safety, which is explained by its minimal impact on the liver, hemostasis system, lipid levels, and breast tissue. E4 has a low risk of drug interactions and a favorable risk profile for venous thromboembolic complications. Clinical trials are currently underway to study the therapeutic potential of E4 treatment for the relief of menopausal symptoms, prevention of bone loss, and its potential use in breast cancer. Conclusion: E4 15 mg/DRSP 3 mg provides safe and effective contraception with high user satisfaction and predictable bleeding.

combined oral contraceptives (COCs) , contraception , drospirenone (DRSP) , estetrol (E4) , estrogen

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Kazakhstan Association on Sexual and Reproductive Health (Kazakhstan Medical and Pedagogical Association), Almaty, Kazakhstan
Institute of Reproductive Medicine, Almaty, Kazakhstan
Kazakhstan Medical University “Kazakhstan’s School of Public Health,”, Almaty, Kazakhstan

Kazakhstan Association on Sexual and Reproductive Health (Kazakhstan Medical and Pedagogical Association)
Institute of Reproductive Medicine
Kazakhstan Medical University “Kazakhstan’s School of Public Health

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