The rediscovery of estetrol and its implications for estrogen treatment.

IF 3 3区医学 Q1 OBSTETRICS & GYNECOLOGY

Menopause: The Journal of The North American Menopause Society Pub Date : 2025-07-01 DOI:10.1097/GME.0000000000002537

Herjan J T Coelingh Bennink, Roger Gosden, Frank Z Stanczyk, Eli Y Adashi

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引用次数: 0

Abstract

Objectives: To summarize the literature on the rediscovery and clinical exploration of the fourth natural estrogen estetrol (E4), more than 100 years after the discovery of estrone (E1), estradiol (E2), and estriol (E3).

Methods: Literature review of E4 publications.

Results: Preclinical and clinical research and development of E4 revealed that: (1) contrary to the other 3 natural estrogens, E4 has a high oral bioavailability, and (2) oral E4 has limited effect on hemostasis and other liver functions, and is, therefore, expected to be a safer estrogen. Since 2022, E4 combined with drospirenone has been registered worldwide as an oral contraceptive. E4 for menopausal hormone therapy is expected to become available in 2026. Clinical development of the use of E4 for the treatment of advanced breast cancer and advanced prostate cancer is ongoing, and E4 has been proposed as a component of an oral male contraceptive.

Conclusion: The recognition of E4 as a useful and safe natural estrogen for human use is expected to change the scene of estrogen treatment in women and men significantly.

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重新发现甾醇及其对雌激素治疗的意义。

目的：总结继雌酮（E1）、雌二醇（E2）、雌三醇（E3）发现100多年后，关于第四种天然雌激素——雌二醇（E4）的再发现和临床探索的文献。方法：查阅E4相关文献。结果：E4的临床前和临床研究与开发表明：(1)与其他3种天然雌激素相反，E4具有较高的口服生物利用度；(2)口服E4对止血等肝功能的影响有限，有望成为一种更安全的雌激素。自2022年以来，E4与螺螺酮联合作为口服避孕药在全球范围内注册。用于更年期激素治疗的E4预计将于2026年上市。使用E4治疗晚期乳腺癌和晚期前列腺癌的临床开发正在进行中，并且E4已被提议作为口服男性避孕药的组成部分。结论：认识到E4是一种有效且安全的天然雌激素，有望显著改变女性和男性雌激素治疗的现状。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Menopause: The Journal of The North American Menopause Society 医学-妇产科学

CiteScore

5.40

自引率

7.40%

发文量

330

审稿时长

3-8 weeks

期刊介绍： Menopause, published monthly, provides a forum for new research, applied basic science, and clinical guidelines on all aspects of menopause. The scope and usefulness of the journal extend beyond gynecology, encompassing many varied biomedical areas, including internal medicine, family practice, medical subspecialties such as cardiology and geriatrics, epidemiology, pathology, sociology, psychology, anthropology, and pharmacology. This forum is essential to help integrate these areas, highlight needs for future research, and enhance health care.