Literature DB >> 24787486

Selective progesterone receptor modulators: an update.

Giuseppe Benagiano1, Carlo Bastianelli, Manuela Farris, Ivo Brosens.   

Abstract

INTRODUCTION: Several selective progesterone receptor modulators (SPRMs) show promise in several areas of medicine and this work has been summarized by us in 2008. AREAS COVERED: Since the publication of our reviews, several developments have taken place in the field of reproductive medicine. The first is emergency contraception (EC). Two SPRMs are clinically utilized today: mifepristone (MFP) and ulipristal acetate (UPA). MFP is available for EC in up to 120 h following unprotected intercourse. A dose of 10 mg is significantly more effective than levonorgestrel (LNG). In a metanalysis of the use of UPA versus LNG up to 72 h after unprotected intercourse, failure rates of 1.4 versus 2.2% were reported. The second is contraception. A daily dose of 2 mg MFP can block ovulation and several MFP regimens are being tested, including a vaginal ring releasing MFP. The third is the preoperative administration in women harboring leiomyomas, where clinical testing of several SPRM has shown that they can decrease uterine leiomyomas' size and substantially reduce uterine bleeding. SPRM can induce unusual, specific endometrial appearances. Many believe that these changes should not cause concern, but the issue remains controversial. EXPERT OPINION: SPRMs are very effective in EC and for the preoperative treatment of uterine leiomyomas.

Entities:  

Keywords:  adenomyosis; asoprisnil; contraception; emergency contraception; endometriosis; mifepristone; proellex; selective progesterone receptor modulators; ulipristal acetate; uterine leiomyomas

Mesh:

Substances:

Year:  2014        PMID: 24787486     DOI: 10.1517/14656566.2014.914494

Source DB:  PubMed          Journal:  Expert Opin Pharmacother        ISSN: 1465-6566            Impact factor:   3.889


  9 in total

1.  Development of N-(4-Phenoxyphenyl)benzenesulfonamide Derivatives as Novel Nonsteroidal Progesterone Receptor Antagonists.

Authors:  Ayumi Yamada; Yuko Kazui; Hiromasa Yoshioka; Aya Tanatani; Shuichi Mori; Hiroyuki Kagechika; Shinya Fujii
Journal:  ACS Med Chem Lett       Date:  2016-09-15       Impact factor: 4.345

Review 2.  Physiological Action of Progesterone in the Nonhuman Primate Oviduct.

Authors:  Ov D Slayden; Fangzhou Luo; Cecily V Bishop
Journal:  Cells       Date:  2022-05-03       Impact factor: 7.666

3.  Phase I/II Trial of Enzalutamide and Mifepristone, a Glucocorticoid Receptor Antagonist, for Metastatic Castration-Resistant Prostate Cancer.

Authors:  Anthony V Serritella; Daniel Shevrin; Elisabeth I Heath; James L Wade; Elia Martinez; Amanda Anderson; Joseph Schonhoft; Yen-Lin Chu; Theodore Karrison; Walter M Stadler; Russell Z Szmulewitz
Journal:  Clin Cancer Res       Date:  2022-04-14       Impact factor: 13.801

4.  Osteoprotegerin (OPG), The Endogenous Inhibitor of Receptor Activator of NF-κB Ligand (RANKL), is Dysregulated in BRCA Mutation Carriers.

Authors:  Martin Widschwendter; Matthew Burnell; Lindsay Fraser; Adam N Rosenthal; Sue Philpott; Daniel Reisel; Louis Dubeau; Mark Cline; Yang Pan; Ping-Cheng Yi; D Gareth Evans; Ian J Jacobs; Usha Menon; Charles E Wood; William C Dougall
Journal:  EBioMedicine       Date:  2015-09-09       Impact factor: 8.143

Review 5.  A Comprehensive Review of the Pharmacologic Management of Uterine Leiomyoma.

Authors:  Terrence D Lewis; Minnie Malik; Joy Britten; Angelo Macapagal San Pablo; William H Catherino
Journal:  Biomed Res Int       Date:  2018-01-28       Impact factor: 3.411

6.  Markers of Cellular Proliferation, Apoptosis, Estrogen/Progesterone Receptor Expression and Fibrosis in Selective Progesterone Receptor Modulator (Ulipristal Acetate)-Treated Uterine Fibroids.

Authors:  Iwona Szydłowska; Marta Grabowska; Jolanta Nawrocka-Rutkowska; Małgorzata Piasecka; Andrzej Starczewski
Journal:  J Clin Med       Date:  2021-02-03       Impact factor: 4.241

Review 7.  Selective progesterone receptor modulators (SPRMs): progesterone receptor action, mode of action on the endometrium and treatment options in gynecological therapies.

Authors:  Andrea Wagenfeld; Philippa T K Saunders; Lucy Whitaker; Hilary O D Critchley
Journal:  Expert Opin Ther Targets       Date:  2016-05-14       Impact factor: 6.902

8.  Progesterone receptor ligands for the treatment of endometriosis: the mechanisms behind therapeutic success and failure.

Authors:  Fernando M Reis; Larissa M Coutinho; Silvia Vannuccini; Frédéric Batteux; Charles Chapron; Felice Petraglia
Journal:  Hum Reprod Update       Date:  2020-06-18       Impact factor: 15.610

9.  Phase I study of onapristone, a type I antiprogestin, in female patients with previously treated recurrent or metastatic progesterone receptor-expressing cancers.

Authors:  Paul H Cottu; Jacques Bonneterre; Andrea Varga; Mario Campone; Alexandra Leary; Anne Floquet; Dominique Berton-Rigaud; Marie-Paule Sablin; Anne Lesoin; Keyvan Rezai; François M Lokiec; Catherine Lhomme; Jacques Bosq; Alice S Bexon; Erard M Gilles; Stefan Proniuk; Veronique Dieras; David M Jackson; Alexander Zukiwski; Antoine Italiano
Journal:  PLoS One       Date:  2018-10-10       Impact factor: 3.240

  9 in total

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