Mifepristone: a novel estrogen-free daily contraceptive pill

Baird, D. T.; Brown, A. G.; Liu, Cheng; Critchley, Hilary; Lin, Suiqin; Narvekar, Nitish; Williams, Alistair

doi:10.1016/j.steroids.2003.07.002

Cited by 39 publications

(29 citation statements)

References 42 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Some PRMs exert anti-estrogenic effects, either through partial progesterone receptor agonist activity, 6,7 or, exert these effects independently of the progesterone receptor itself, that is by upregulation of the androgen receptor response. 8,9 These PRM effects are evident as dose-dependent suppression of estrogen-induced mitotic activity, [10][11][12] and appearance of glandular secretory changes. 7 Assessment of PRM induced changes in the endometrium by pathologists is not only a prerequisite step to determine suitability for widespread clinical use, but also indicates how community pathologists are likely to respond to endometrial biopsies from women on these agents.…”

mentioning

confidence: 99%

The spectrum of endometrial pathology induced by progesterone receptor modulators

Bergeron²,

et al. 2008

View full text Add to dashboard Cite

Progesterone receptor modulators (PRM) are hormonally active drugs effective in the management of endometriosis and uterine leiomyomata. The endometrial effects of progestin blockade by PRMs in premenopausal women are currently being evaluated in several clinical trials, but few pathologists have had access to these materials and published information of the histological changes is scanty. Eighty-four endometrial specimens from women receiving one of four different PRMs were reviewed by a panel of seven experienced gynecologic pathologists to develop consensus observations and interpretive recommendations as part of an NIH-sponsored workshop. Although the pathologists were blinded to agent, dose, and exposure interval, the review was intended to provide an overview of the breadth of possible findings, and a venue to describe unique features. Endometrial histology included inactive and normal-appearing cycling endometrium. Overtly premalignant lesions (atypical hyperplasia or EIN) were not seen. In a subset of cases, asymmetry of stromal and epithelial growth resulted in prominent cystically dilated glands with admixed estrogen (mitotic) and progestin (secretory) epithelial effects of a type not encountered in contemporary clinical practice. The variety of endometrial appearances suggested that findings might differ by agent and dose over time according to relationships that must be specified for each agent. The constellation of changes seen in those endometria with cystically dilated glands is so novel that new terminology and diagnostic criteria are required for pathologists to recognize them. The panel has designated these changes as PRM-associated endometrial changes (PAEC). Additional follow-up studies will be needed to fully define their natural history and relationship to specific agents and administration regimens.

show abstract

mentioning

confidence: 99%

The spectrum of endometrial pathology induced by progesterone receptor modulators

Bergeron²,

et al. 2008

View full text Add to dashboard Cite

show abstract

“…Nevertheless, we have not seen any alteration in intervillous space, neither in placental volume. We expected some modification because it has been described an edema, microhematoma and a venous dilatation in the stromal compartment in endometrial tissue under RU effect [11][12][13]. However, these studies were carried out in non-pregnant women and it could be possible that the effect would be different during gestation.…”

Section: Discussionmentioning

confidence: 99%

Three-Dimensional Angiogenic Evaluation of the Effect of Mifepristone in Early Gestation: Pilot Study

Pellicer-Iborra¹,

Herraiz²,

Morales³

et al. 2017

Gynecol Obstet

View full text Add to dashboard Cite

Mifepristone (RU486) it is known as an effective abortifacient and postcoital contraceptive method, whose mechanism is not yet known. We carried on a pilot study with the aim of determining the effect that Mifepristone could have in utero-placental vascular compartment during the first trimester of pregnancy compared with placebo. This is a randomized, double-blind, placebo-controlled research. We randomly assigned to two groups patients requesting pregnancy termination with a gestational age between 9th and 11st weeks: Group A receiving placebo and Group B receiving RU. With transvaginal ultrasound tridimensional probe we measured at an initial time (t1) and then 4 hours after administration of Mifepristone or placebo (t2) Doppler parameters: uterine arteries mean Resistance Index, spiral arteries Resistance Index, intervillous flow, umbilical Resistance Index and tridimensional vascular settings and the placental volume. We observed how Mifepristone shows an immediate selective hemodynamic effect in trophoblastic tissue in the first hours of administration. A significant decrease in spiral arteries pulsatility index was demonstrated, without modifying uterine maternal and fetal territories or the other studied parameters. Angiopower 3D evaluation of the interface maternal fetal is complex and encourages to carry further investigations carry further investigations.

show abstract

“…These observations strike a resounding chord with those data acceded in the macaque described earlier. The potential value of PRAs as alternative contraceptives to current combined or progestin-only pills have been long recognised and evaluated in a number of different dosing and delivery strategies (Baird et al, 2003;Brown et al, 2002;Chabbert-Buffet et al, 2007;Heikinheimo et al, 2007;Lakha et al, 2007;Nayak et al, 2007). Whilst no pregnancies were reported after 200 months in women who received 2-5 mg RU-486 daily (Brown et al, 2002), lower doses appeared to be less effective (Croxatto et al, 1998).…”

Section: Clinical Evaluation In Healthy Women and Women With Endometrmentioning

confidence: 99%

“…Whether these effects on the endometrium are mediated by the unopposed effects of persistent follicular phase levels of estradiol, the pharmacological class or some non-specific effect of PRAs on the endometrium is not clear, but this appears to be a common feature of all steroidal PRAs assessed so far. Individuals on prolonged exposure to asoprisnil/J-867 were at a higher risk of developing endometrial changes sufficient to raise concern with regulatory authorities indicates that more research is needed to understand the phenomenon of PRA associated endometrial changes and whether this might be in part mitigated by an alternative dosing regimen from continuous dosing (Baird et al, 2003).…”

Section: Clinical Evaluation In Healthy Women and Women With Endometrmentioning

confidence: 99%

Progesterone Resistance and Targeting the Progesterone Receptors: A Therapeutic Approach to Endometriosis

Pullen¹

2012

Endometriosis - Basic Concepts and Current Research Trends

View full text Add to dashboard Cite

Mifepristone: a novel estrogen-free daily contraceptive pill

Cited by 39 publications

References 42 publications

The spectrum of endometrial pathology induced by progesterone receptor modulators

The spectrum of endometrial pathology induced by progesterone receptor modulators

Three-Dimensional Angiogenic Evaluation of the Effect of Mifepristone in Early Gestation: Pilot Study

Progesterone Resistance and Targeting the Progesterone Receptors: A Therapeutic Approach to Endometriosis

Contact Info

Product

Resources

About