Literature DB >> 18778185

Selective progesterone receptor modulators 2: use in reproductive medicine.

Giuseppe Benagiano1, Carlo Bastianelli, Manuela Farris.   

Abstract

BACKGROUND: Synthetic compounds can bind to progesterone receptors and these progesterone receptor ligands exhibit a spectrum of activities ranging from pure antagonism to a mixture of agonism and antagonism. These substances have been classified as antiprogestins or as selective progesterone receptor modulators.
OBJECTIVE: There are several hundred selective progesterone receptor modulators available, although only a dozen or so have been evaluated to any significant extent. The best-known selective progesterone receptor modulators are mifepristone (RU 486), asoprisnil (J 867), onapristone (ZK 98299), ulipristal (CDB 2914), Proellex() (CDB 4124), ORG 33628 and ORG 31710.
METHODS: A careful evaluation of existing major review papers and of recently published articles was carried out for the indications under review, focusing not only on mifepristone, but also on those other selective progesterone receptor modulators for which data are available. RESULTS/
CONCLUSIONS: Outside pregnancy, selective progesterone receptor modulators are used or have been tested clinically for a number of indications in reproductive medicine: as oral contraceptives, alone or in combination with a progestin, to improve cycle control in users of progestin-only contraceptives, as emergency contraceptives, for the medical treatment of uterine fibroids, in cases of endometriosis and premenstrual syndrome and to improve ovarian stimulation prior to in vitro fertilisation. In the authors' opinion, as of today, few applications outside pregnancy seem worthy of large-scale use: emergency contraception and long-term medical management of uterine fibroids and possibly of endometriosis.

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Year:  2008        PMID: 18778185     DOI: 10.1517/14656566.9.14.2473

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


  8 in total

1.  X-ray structures of progesterone receptor ligand binding domain in its agonist state reveal differing mechanisms for mixed profiles of 11β-substituted steroids.

Authors:  Scott J Lusher; Hans C A Raaijmakers; Diep Vu-Pham; Bert Kazemier; Rolien Bosch; Ross McGuire; Rita Azevedo; Hans Hamersma; Koen Dechering; Arthur Oubrie; Marcel van Duin; Jacob de Vlieg
Journal:  J Biol Chem       Date:  2012-04-25       Impact factor: 5.157

2.  Structural basis for agonism and antagonism for a set of chemically related progesterone receptor modulators.

Authors:  Scott J Lusher; Hans C A Raaijmakers; Diep Vu-Pham; Koen Dechering; Tsang Wai Lam; Angus R Brown; Niall M Hamilton; Olaf Nimz; Rolien Bosch; Ross McGuire; Arthur Oubrie; Jacob de Vlieg
Journal:  J Biol Chem       Date:  2011-08-17       Impact factor: 5.157

3.  Novel 3-aryl indoles as progesterone receptor antagonists for uterine fibroids.

Authors:  Timothy I Richardson; Christian A Clarke; Kuo-Long Yu; Ying K Yee; Thomas J Bleisch; Jose E Lopez; Scott A Jones; Norman E Hughes; Brian S Muehl; Charles W Lugar; Terry L Moore; Pamela K Shetler; Richard W Zink; John J Osborne; Chahrzad Montrose-Rafizadeh; Nita Patel; Andrew G Geiser; Rachelle J Sells Galvin; Jeffrey A Dodge
Journal:  ACS Med Chem Lett       Date:  2010-12-09       Impact factor: 4.345

4.  Drug Repurposing for Cancer Therapy.

Authors:  Carlos M Telleria
Journal:  J Cancer Sci Ther       Date:  2012-07-21

5.  Growth inhibition induced by antiprogestins RU-38486, ORG-31710, and CDB-2914 in ovarian cancer cells involves inhibition of cyclin dependent kinase 2.

Authors:  Alicia A Goyeneche; Erin E Seidel; Carlos M Telleria
Journal:  Invest New Drugs       Date:  2011-03-22       Impact factor: 3.850

6.  Antiprogestin mifepristone inhibits the growth of cancer cells of reproductive and non-reproductive origin regardless of progesterone receptor expression.

Authors:  Chelsea R Tieszen; Alicia A Goyeneche; BreeAnn N Brandhagen; Casey T Ortbahn; Carlos M Telleria
Journal:  BMC Cancer       Date:  2011-05-27       Impact factor: 4.430

7.  The state-of-the-art of emergency contraception with the cutting edge drug.

Authors:  Narendra Nath Sarkar
Journal:  Ger Med Sci       Date:  2011-07-11

8.  EC313-a tissue selective SPRM reduces the growth and proliferation of uterine fibroids in a human uterine fibroid tissue xenograft model.

Authors:  Hareesh B Nair; Bindu Santhamma; Kalarickal V Dileep; Peter Binkley; Kirk Acosta; Kam Y J Zhang; Robert Schenken; Klaus Nickisch
Journal:  Sci Rep       Date:  2019-11-21       Impact factor: 4.379

  8 in total

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