Selective progesterone receptor modulators in reproductive medicine: pharmacology, clinical efficacy and safety

Bouchard, Philippe; Chabbert-Buffet, Nathalie; Fauser, Bart C.J.M.

doi:10.1016/j.fertnstert.2011.08.021

Cited by 166 publications

(117 citation statements)

References 150 publications

(199 reference statements)

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“…48,[112][113][114] Antiprogestins have a number of applications in reproductive medicine, including use as contraceptives due to their ability to prevent implantation or ovulation. 115 The currently available PR antagonists are all competitive inhibitors of P binding to the PR LBD. 115 Type I antiprogestins, such as ZK 98299 (onapristone), bind PR but fail to induce receptor phosphorylation and induce weak receptor binding to HREs.…”

Section: Receptor Antagonistsmentioning

confidence: 99%

Steroid Receptors in the Uterus and Ovary

Binder

Winuthayanon

Hewitt

et al. 2015

Knobil and Neill's Physiology of Reproduction

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Section: Receptor Antagonistsmentioning

confidence: 99%

Steroid Receptors in the Uterus and Ovary

Binder

Winuthayanon

Hewitt

et al. 2015

Knobil and Neill's Physiology of Reproduction

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“…61 Its use as an antidepressant and in central serous chorioretinopathy has also been proposed. 62,63 Daily doses of 200 to 600 mg are recommended but, to our knowledge, visual adverse effects have not been reported.…”

Section: Main Conclusionmentioning

confidence: 99%

Mifepristone, a Blocker of Glucocorticoid Receptors, Promotes Photoreceptor Death

Cubilla¹,

Bermúdez²,

Marquioni-Ramella³

et al. 2013

Invest. Ophthalmol. Vis. Sci.

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PURPOSE. Glucocorticoids are best known by their protective effect on retinal photoreceptor damage. However, they could also be involved in photoreceptor homeostasis under basal, nonstressful conditions. Therefore, we aimed to study glucocorticoid-induced changes of survival-related molecules in male mice retinas under standard illumination conditions (12 hours light, 60 lux/12 h dark).METHODS. Male Balb-c mice were injected with dexamethasone (DEX), a selective glucocorticoid receptor a (GRa) agonist, its antagonist mifepristone (MFP), or both drugs (DþM) at noon. A group of mice was subjected to surgical adrenalectomy (AdrX). Retinas were studied by histology, immunohistochemistry, TUNEL procedure, and Western blotting at different periods after pharmacological or surgical intervention (6 hours, 48 hours, or 7 days). RESULTS.The antiapoptotic molecule Bcl-X L significantly increased 6 hours after DEX injection. By contrast, this molecule could no longer be found after MFP injection. At the same time, high levels of cleaved caspase-3 (CC-3) and Bax appeared in retinal extracts, and TUNEL þ nuclei selectively showed in the outer nuclear layer (ONL). After MFP, retinal extracts also contained phosphorylated histone H2AX (p-H2AX), a marker of DNA breakage and repair. Loss of ONL nuclear rows and decrease of rhodopsin levels were evident 7 days after MFP administration. These changes were minimized when DEX was given together with MFP (DþM). In the absence of MFP, DEX increased Bcl-X L in every retinal layer, with a marked intensification in photoreceptor inner segments. Numerous TUNEL þ nuclei rapidly appeared in the ONL after AdrX. CONCLUSIONS.A single dose of MFP induced selective photoreceptor damage in the absence of other environmental stressors. Because damage was prevented by DEX, and was reproduced by AdrX, our findings suggest that glucocorticoids play a critical role in photoreceptor survival. (Invest Ophthalmol Vis Sci. 2013;54:313-322)

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“…Yalnızca progesteron antagonisti olarak etki etmekte ve endometriumda östrojen aktivitesini inhibe etmemektedir (42). Telapriston asetat da bir selektif progesteron reseptör modülatörüdür; kanama miktarının ve leiomyom ve uterus boyutunu azalttığı gösterilmiştir (43). Ancak; karaciğer toksisitesi nedeniyle klinik çalışmalar durdurulmuş olup daha düşük dozlarda yeni çalışmalar yapıl-maktadır.…”

Section: Selektif Progesteron Reseptör Modülatörleriunclassified

Medical Treatment of Leiomyomas

Uğurlucan¹,

Demir²,

Yaşa³

et al. 2017

İstanbul Tıp Fakültesi Dergisi

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ÖZETLeiomyomlar, reprodüktif çağda en sık görülen jinekolojik tümörlerdir. Leiomyomlar çoğu kadında bulunmakla beraber, bazı kadınlarda semptomatik hale gelmektedir. Genetik veya hormonal kökenli olabilirler. Leiomyomların üzerinde östrojen ve progesteron reseptörleri olması, onları hormona duyarlı hale getirmektedir. Leiomyomların ana tedavisi cerrahi olmakla beraber, cerrahi istemeyen veya fertilitesini korumak isteyen kadınlarda medikal tedaviler gündeme gelmektedir. Medikal tedavilerin çıkış noktası, leiomyomların hormona duyarlı olmasıdır. Medikal tedavi seçenekleri arasında gonadotropin-releasing-3 hormon analogları ve antagonistleri, aromataz inhibitörleri ve selektif progesteron reseptör modülatörleri yer almaktadır. Bu tedaviler kanama kontrolünün yanında leiomyom volümünde de küçülme sağlamaktadır. Bu derlemede bu tedavi yöntemlerine değinilecektir. Anahtar Kelimeler: Leiomyom; anormal uterin kanama; selektif progesteron reseptör modülatörleri; ulipristal asetat; anemi ABSTRACTLeiomyomas are the most common benign gynecological tumors observed during the reproductive period. Although, they are exceedingly common, not all are symptomatic. Leiomyomas are of genetic or hormonal origin and have estrogen and progesterone receptors, making them sensitive to hormones. The main treatment for leiomyomas is surgery, but in women who are not willing to undergo surgery or who want to preserve their fertility, medical treatment options may be used. The main basis of medical treatment in leiomyomas are hormones due to positive response to anti-hormonal therapies. Medical treatment options comprise gonadotropin-releasing-hormone agonists and antagonists, aromatase inhibitors, and selective progesterone receptor modulators. In addition to controlling bleeding, these treatment regimens cause a decrease in the volume of the tumor. In this review, treatment options are discussed.

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Selective progesterone receptor modulators in reproductive medicine: pharmacology, clinical efficacy and safety

Cited by 166 publications

References 150 publications

Steroid Receptors in the Uterus and Ovary

Steroid Receptors in the Uterus and Ovary

Mifepristone, a Blocker of Glucocorticoid Receptors, Promotes Photoreceptor Death

Medical Treatment of Leiomyomas

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