Selective progesterone receptor modulators (SPRMs) have been developed since the late 70s when mifepristone was first described. They act through nuclear progesterone receptors and can have agonist or mixed agonist antagonist actions depend…
ObjectiveTo discuss the mechanism of action of selective progesterone receptor modulators (SPRMs) and summarize the preclinical and clinical efficacy and safety data supporting the potential use of these compounds for gynecologic indication…
Currently developed progesterone receptor modulators (PRMs) are steroid-derived compounds with mild or potent antiprogestin activity. PRMs may exert a contraceptive activity by different mechanisms such as blockade of ovulation and endometr…
Progesterone-receptor modulators (PRMs) are progesterone-receptor ligands that can exert agonistic, antagonistic or mixed agonist-antagonist effects depending on the cellular context. The mechanisms of action of these compounds are still in…
Progesterone antagonists belong to the family of selective progesterone receptor modulators. SPRMs already have several applications in women's health. Their main value lies in their effect on endometrium. For example, they can be used to r…
CONTEXT: Progestin-only pills, the main hormonal alternative to ethinyl estradiol-containing pills in women bearing vascular risk factors, are poorly tolerated due to irregular bleeding. In contrast, progesterone receptor modulators can inh…
Antagonists act by competitive inhibition of pituitary GnRH receptors for which they have a high affinity with a dose-dependent activity. The inhibition concerns LH but also FSH by inhibiting their secretion for 24 hours. At this time, only…
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 its…
Two byproducts of in vitro fertilization, transvaginal ultrasonography and hormonal preparation of endometrial receptivity for oocyte donation, have been the source of great progress in endometrial physiology. In practical terms, transvagin…
The mechanism by which progesterone modifies uterine smooth muscle cell contraction is still unknown. We investigated the biochemical basis of progesterone effects on myometrium of estradiol-primed rabbits. Progesterone did not affect adeny…