Role of Progesterone Antagonists and New Selective Progesterone Receptor Modulators in Reproductive Health

David L. Olive, Olive DL
Obstetrical & gynecological survey · 2002 · vol. 57(11 Suppl 4) , pp. S55–S63 · doi:10.1097/00006254-200211004-00001 · PMID:12454529 · W2052994607
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⚙ AI-generated summary by gemini-2.5-flash-lite, 2026-06-28 ⓘ

This review discusses progesterone antagonists and selective progesterone receptor modulators, detailing their mechanisms, effects on reproductive tissues, and potential clinical applications for gynecologic conditions.

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This review examines the mechanisms and clinical applications of progesterone antagonists and selective progesterone receptor modulators in female reproductive health. The author contrasts established uses of antagonists, such as pregnancy termination and cervical dilation, with the emerging potential of SPRMs for conditions like endometriosis, uterine fibroids, and dysfunctional uterine bleeding. While noting that SPRMs have diminished efficacy for abortion induction compared to traditional antagonists, the paper highlights their dual agonist-antagonist activities across various tissues. Relevance to endometriosis: listed as one indication for SPRMs, though the paper's main focus is a broad overview of progesterone receptor modulators.

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Abstract

UNLABELLED: Given the importance of progesterone in female reproductive health, it was inevitable that analogues of this molecule would be developed to treat a variety of gynecologic maladies. Such medications, termed progesterone antagonists, act to counteract the effect of progesterone. A newer class of molecules, the selective progesterone receptor modulators (SPRMs), have both agonist and antagonist activities depending upon the site of action. These compounds have been studied for their effect on endometrial growth, endometrial vascular development, the hypothalmic-pituitary-ovarian axis and cervical integrity. Such research has led to a number of potential clinical applications. Progesterone antagonists are well established in their use for termination of pregnancy, although SPRMs seem to have a diminished capacity for induction of abortion. Similarly, antagonists work well to soften and dilate the cervix before surgery, but such efficacy by SPRMs is unlikely. Other applications for progesterone antagonists include induction of labor, the treatment of endometriosis, fibroids and contraception; SPRMs also may prove useful in the treatment of endometriosis and fibroids, as well as for postmenopausal hormone replacement therapy and the treatment of dysfunctional uterine bleeding. Finally, these compounds may aid investigators in unraveling many of the nuances of the role of progesterone in reproductive function. TARGET AUDIENCE: Obstetricians & Gynecologists, Family Physicians Learning Objectives: After completion of this article, the reader will be able to describe the receptor action and selective modulation of progesterone, explain the effects of progesterone receptor modulators, and list the potential clinical applications of progesterone antagonists and selective progesterone receptor modulators.
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Role of Progesterone Antagonists and New Selective Progesterone Receptor Modulators in Reproductive Health - David L. Olive Given the importance of progesterone in female reproductive health, it was inevitable that analogues of this molecule would be developed to treat a variety of gynecologic maladies. Such medications, termed progesterone antagonists, act to counteract the effect of progesterone. A newer class of molecules, the selective progesterone receptor modulators (SPRMs), have both agonist and antagonist activities depending upon the site of action. These compounds have been studied for their effect on endometrial growth, endometrial vascular development, the hypothalmic-pituitary-ovarian axis and cervical integrity. Such research has led to a number of potential clinical applications. Progesterone antagonists are well established in their use for termination of pregnancy, although SPRMs seem to have a diminished capacity for induction of abortion. Similarly, antagonists work well to soften and dilate the cervix before surgery, but such efficacy by SPRMs is unlikely. Other applications for progesterone antagonists include induction of labor, the treatment of endometriosis, fibroids and contraception; SPRMs also may prove useful in the treatment of endometriosis and fibroids, as well as for postmenopausal hormone replacement therapy and the treatment of dysfunctional uterine bleeding. Finally, these compounds may aid investigators in unraveling many of the nuances of the role of progesterone in reproductive function. Target Audience: Obstetricians & Gynecologists, Family Physicians Learning Objectives: After completion of this article, the reader will be able to describe the receptor action and selective modulation of progesterone, explain the effects of progesterone receptor modulators, and list the potential clinical applications of progesterone antagonists and selective progesterone receptor modulators.

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Condition tags

endometriosis

MeSH descriptors

Genital Diseases, Female Hormone Antagonists Progesterone Receptors, Progesterone Female Genital Diseases, Female Hormone Antagonists Hormone Antagonists Humans Pregnancy Progesterone Receptors, Progesterone Receptors, Progesterone Receptors, Progesterone Reproductive Medicine Women's Health

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