Promising selective progesterone receptor modulators: what's new in female contraception?

IF 4.9 2区 医学 Q1 PHARMACOLOGY & PHARMACY
Anita Nelson, Marit Pearlman Shapiro
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引用次数: 0

Abstract

Introduction: Selective progesterone receptor modulators (SPRMs), such as mifepristone and ulipristal acetate (UPA), have demonstrated high efficacy and safety as single dose treatments for medication abortion and emergency contraception (EC). Other obstetrical and gynecologic applications have emerged, both for episodic and ongoing uses. The potential of these compounds to provide estrogen-free, ongoing contraception is promising; however, the rare, but serious, hepatic injury cases seen with UPA have put at least a temporary halt to further research in this area.

Areas covered: This paper reviews the biophysical impacts and clinical applications of SPRMs in women's reproductive health, with a focus on the roles of mifepristone and UPA in family planning. Given the political environment, especially in the United States where these applications may be threatened, extensive description is dedicated to mechanisms of action of these agents.

Expert opinion: Both mifepristone and ulipristal acetate are first-line options for single use applications. There continues to be a need for estrogen-free ongoing contraception that does not have unpopular impacts on bleeding caused by contraceptive methods and for treatments for heavy menstrual bleeding. However, current restrictions on UPA limit longer term use. Perhaps other SPRMs without hepatic impacts may emerge to fill this need.

前景看好的选择性孕酮受体调节剂:女性避孕的新动向?
简介:选择性孕酮受体调节剂(SPRMs),如米非司酮和醋酸乌利司他(UPA),作为药物流产和紧急避孕(EC)的单剂量治疗,已被证明具有很高的有效性和安全性。其他妇产科应用也已出现,既有偶发性应用,也有持续性应用。这些化合物具有提供不含雌激素的持续避孕的潜力,前景广阔;然而,UPA 罕见但严重的肝损伤病例至少暂时停止了这一领域的进一步研究:本文回顾了 SPRM 在妇女生殖健康中的生物物理影响和临床应用,重点关注米非司酮和 UPA 在计划生育中的作用。鉴于目前的政治环境,尤其是在美国,这些药物的应用可能会受到威胁,因此对这些药物的作用机制进行了广泛的描述:专家意见:米非司酮和醋酸乌利司他都是一次性使用的一线选择。人们仍然需要不含雌激素的持续避孕药物,这种药物不会对避孕方法引起的出血造成不受欢迎的影响,也需要治疗大量月经出血的药物。然而,目前对 UPA 的限制限制了其长期使用。也许会出现其他不会对肝脏造成影响的 SPRM 来满足这一需求。
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来源期刊
CiteScore
10.00
自引率
0.00%
发文量
71
审稿时长
6-12 weeks
期刊介绍: Expert Opinion on Investigational Drugs (ISSN 1354-3784 [print], 1744-7658 [electronic]) is a MEDLINE-indexed, peer-reviewed, international journal publishing review articles and original papers on drugs in preclinical and early stage clinical development, providing expert opinion on the scope for future development. The Editors welcome: Reviews covering preclinical through to Phase II data on drugs or drug classes for specific indications, and their potential impact on future treatment strategies Drug Evaluations reviewing the clinical and pharmacological data on a particular drug Original Research papers reporting the results of clinical investigations on agents that are in Phase I and II clinical trials The audience consists of scientists, managers and decision-makers in the pharmaceutical industry, and others closely involved in R&D.
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