Literature DB >> 18778184

Selective progesterone receptor modulators 1: use during pregnancy.

Giuseppe Benagiano1, Carlo Bastianelli, Manuela Farris.   

Abstract

BACKGROUND: A large number of synthetic compounds known as selective progesterone receptor modulators can bind to progesterone receptors: the ligands exhibit a spectrum of activities ranging from pure antagonism to a mixture of agonism and antagonism.
OBJECTIVES: Only a dozen or so selective progesterone receptor modulators have been tested to any significant extent: among them are mifepristone (RU 486), asoprisnil (J867), onapristone (ZK 98 299), ulipristal (CDB 2914), Proellex() (CDB 4124), ORG 33628 and ORG 31710. Their clinical applications during pregnancy are discussed.
METHODS: A careful evaluation of existing major review papers and recently published articles was carried out focusing on mifepristone, the most widely studied selective progesterone receptor modulator, which was first used for the voluntary interruption of an early gestation. Other selective progesterone receptor modulators, especially those with partial agonist action, have shown little activity during pregnancy in animal models. RESULTS/
CONCLUSIONS: Besides early and late voluntary interruption of gestation, selective progesterone receptor modulators have been tested in a variety of obstetrical situations: to obtain a ripening of the cervix, for the medical management of early embryonic loss and foetal death, for the induction of labour at term and for the medical treatment of extra-uterine pregnancies. The only applications that seem worthy of large-scale utilisation during pregnancy are voluntary interruption of early and late gestation, medical management of early delayed miscarriage and late foetal demise.

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Year:  2008        PMID: 18778184     DOI: 10.1517/14656566.9.14.2459

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


  9 in total

1.  Progesterone receptor antagonist CDB-4124 increases depression-like behavior in mice without affecting locomotor ability.

Authors:  Ethan H Beckley; Angela C Scibelli; Deborah A Finn
Journal:  Psychoneuroendocrinology       Date:  2010-12-15       Impact factor: 4.905

2.  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

3.  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

4.  Postcoital administration of asoprisnil inhibited embryo implantation and disturbed ultrastructure of endometrium in implantation window in mice.

Authors:  Xiao-Li Wu; Zhi-Hong Yu; Jun Qiu; Yi-Hong Yang; Xiao-Li Shen; Ping Su
Journal:  J Huazhong Univ Sci Technolog Med Sci       Date:  2013-04-17

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.  Mifepristone prevents repopulation of ovarian cancer cells escaping cisplatin-paclitaxel therapy.

Authors:  Carlos D Gamarra-Luques; Alicia A Goyeneche; Maria B Hapon; Carlos M Telleria
Journal:  BMC Cancer       Date:  2012-06-22       Impact factor: 4.430

8.  Resistance to cisplatin and paclitaxel does not affect the sensitivity of human ovarian cancer cells to antiprogestin-induced cytotoxicity.

Authors:  Carlos D Gamarra-Luques; Maria B Hapon; Alicia A Goyeneche; Carlos M Telleria
Journal:  J Ovarian Res       Date:  2014-04-27       Impact factor: 4.234

9.  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

  9 in total

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