Selective progesterone receptor modulators and progesterone antagonists: mechanisms of action and clinical applications

Nathalie Chabbert-Buffet, Chabbert-Buffet N, Nathalie Chabbert‐Buffet, Geri Meduri, Geri Méduri, Meduri G, Bouchard P, Philippe Bouchard, Spitz IM, Irving M. Spitz
Human Reproduction Update · 2005 · vol. 11(3) , pp. 293–307 · doi:10.1093/humupd/dmi002 · PMID:15790602 · W2147700987
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Progesterone receptor modulators and antagonists have varied mechanisms and applications, including contraception, uterine fibroids, endometriosis, and potential hormone replacement therapy.

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Abstract

Since the discovery of the antiprogestin mifepristone, hundreds of similar compounds have been synthesized, which can be grouped in a large family of progesterone receptor ligands. This family includes pure agonists such as progesterone itself or progestins and, at the other end of the biological spectrum, pure progesterone receptor antagonists (PA). Selective progesterone receptor modulators (SPRM) have mixed agonist-antagonist properties, and occupy an intermediate position of the spectrum. These compounds have numerous applications in female health care. Mifepristone is used to terminate pregnancy, and as such is commercially available in many countries. The negative abortion-related image of mifepristone has clearly limited the involvement of the major pharmaceutical companies in the development of PA and SPRM. Many PA and SPRM display direct antiproliferative effects in the endometrium, although with variable actions which seem product- and dose-dependent. This property justifies their use in the treatment of myomas and endometriosis. PA also suppress late follicular development, block the LH surge and retard endometrial maturation, which renders them potential estrogen-free contraceptive drugs. SPRM such as asoprisnil are not as effective in blocking the LH surge and appear to target the endometrium directly and produce amenorrhoea. Interestingly, clinical data show that treatment with these compounds is not associated with hypo-estrogenism and bone loss. The potential clinical applications of these compounds cover a broad field and are very promising in major public health areas. These include emergency contraception, long-term estrogen-free contraception (administered alone, or in association with a progestin-only pill to improve bleeding patterns), myomas (where they induce a marked reduction in tumour volume and produce amenorrhoea) and endometriosis. Further developments might also include hormone replacement therapy in post-menopausal women, as well as the treatment of hormone-dependent tumours.

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Condition tags

endometriosis

MeSH descriptors

Endometriosis Leiomyoma Progesterone Receptors, Progesterone Receptors, Progesterone Endometriosis Estrenes Estrenes Estrenes Female Gonanes Gonanes Gonanes Humans Leiomyoma Norpregnadienes Norpregnadienes Norpregnadienes Oximes Oximes

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