1,575
Views
10
CrossRef citations to date
0
Altmetric
Editorial

Gynaecological uses of a new class of steroids: the selective progesterone receptor modulators

, &
Pages 67-73 | Received 01 Jun 2008, Accepted 01 Jul 2008, Published online: 07 Jul 2009

References

  • Chwalisz K, Perez M C, DeManno D, Winkel C, Schubert G, Elger W. Selective progesterone receptor modulator development and use in the treatment of leiomyomata and endometriosis. Endocr Rev 2005; 26: 423–438
  • Philibert D. RU38486: an original multifacted antihormone in vivo. Adrenal Steroid Antagonism, M Agarwal. Walter de Gruyter and Co, Berlin 1984; 77–101
  • Neef G, Beier S, Elger W, Henderson D, Wiechert R. New steroids with anti-progestational and anti-glucocorticoid activities. Steroids 1984; 44: 349–372
  • Kloosterboer H J, Deckers G H, Van de Heuvel M J, Loozen H J. Screening of anti-progestagens by receptor studies and bioassays. J Steroid Biochem 1988; 31: 567–571
  • Chabbert-Buffet N, Meduri G, Bouchard P, Spitz E. Selective progesterone receptor modulator and progesterone antagonist: mechanism of action and clinical application. Hum Reprod Update 2005; 11: 293–307
  • Csapo A. Progesterone block. Am J Anat 1956; 98: 273–291
  • Padykula H A. Regeneration in the primate uterus: the role of stem cells. Ann NY Acad Sci 1991; 622: 47–56
  • Brandon D D, Bethea C L, Strawn E Y, Novy M J, Burry K A, Harrington M S, Erickson T E, Warner C, Keenan E J, Clinton G M. Progesterone receptor messenger ribonucleic acid and protein are over expressed in human uterine leiomyomas. Am J Obstet Gynecol 1993; 169: 78–85
  • Nisolle M, Gillerot S, Casanas-Roux F, Squifflet J, Berliere M, Donnez J. Immunohistochemical study of the proliferation index, oestrogen receptors and progesterone receptors A and B in leiomyomata and normal myometrium during the menstrual cycle and under gonadotrophin-releasing hormone agonist therapy. Hum Reprod 1999; 14: 2844–2850
  • Kawaguchi K, Fujii S, Konishi I, Nanbu Y, Nonogaki H, Mori T. Mitotic activity in uterine leiomyomas during the menstrual cycle. Am J Obstet Gynecol 1989; 160: 637–641
  • Lundstrom E, Wilczek B, von Palffy Z, Soderqvist G, von Schoultz B. Mammographic breast density during hormone replacement therapy: differences according to treatment. Am J Obstet Gynecol 1999; 181: 348–352
  • Rossouw J E, Anderson G L, Prentice R L, LaCroix A Z, Kooperberg C, Stefanick M L, Jackson R D, Beresford S A, Howard B V, Johnson K C, et al. Risks and benefits of estrogen plus progestin in healthy post-menopausal women: principal results from the Women's Health Initiative randomized controlled trial. JAMA 2002; 288: 321–333
  • Beral V. Breast cancer and hormone-replacement therapy in the million women study. Lancet 2003; 362: 419–427
  • Poole A J, Li Y, Kim Y, Lin S C, Lee W H, Lee E Y. Prevention of Brca1-mediated mammary tumorigenesis in mice by a progesterone antagonist. Science 2006; 314: 1467–1470
  • Mahajan D K, London S N. Mifepristone (RU 486): a review. Fertil Steril 1997; 86: 967–976
  • Hermann W L, Schlindler A M, Wyss R, Bischoff P. Effects of anti-progesterone RU 486 in early pregnancy and during the menstrual cycle. The Antiprogestin Steroid RU 486 and Human Fertility Control, E E Beaulieu, S Siegel. Plenum, New York 1985; 259–262
  • Schreiber C, Creinin M. Mifepristone in abortion care. Semin Reprod Med 2005; 23: 82–91
  • Tang O S, Ho P C. Clinical applications of mifepristone. Gynecol Endocrinol 2006; 22: 655–659
  • Kovacs L, Sas M, Resch B A, Ugocsai G, Swahn M L, Bygdeman M, Rowe P J. Termination of very early pregnancy by RU 486, an anti-progestational compound. Contraception 1984; 29: 399–410
  • Shoupe D, Mishell D R, Jr, Brenner P F, Spitz I M. Pregnancy termination with a high and medium dosage regimen of RU-486. Contraception 1986; 33: 455–461
  • Peyron R, Aubény E, Targosz V, Silvestre L, Renault M, Elkik F, Leclerc P, Ulmann A, Baulieu E E. Early termination on pregnancy with mifepristone (RU 486) and the orally active prostaglandin misoprostol. N Engl J Med 1993; 328: 1509–1513
  • Aubeny E, Peyron R, Turpin C L, Renault M, Targosz V, Silvestre L, Ulmann A, Baulieu E E. Termination of early pregnancy (up to 63 days of amenorrhea) with mifepristone (RU 486) and increasing doses of misoprostol. Int J Fertil Menopausal Stud 1995; 40(Suppl 2)85–91
  • Spitz I M, Bardin C W, Benton L, Robbins A. Early pregnancy termination with mifepristone and misoprostol in the United States. N Engl J Med 1998; 338: 1241–1247
  • Aubeny E. A two-stage increase in the dose of misoprostol improves the efficacy of medical abortion with mifepristone and prostaglandins (letter). Eur J Contracept Reprod Health Care 2001; 6: 54–55
  • World Health Organization Task Force on Post-ovulatory Methods for Fertility Regulation. Termination of pregnancy with reduced doses of mifepristone. BMJ 1993; 307: 532–537
  • McKinley C, Thong K J, Baird D T. The effect of dose of mifepristone and gestation on efficacy of medical abortion with mifepristone and misoprostol. Hum Reprod 1993; 8: 1502–1505
  • World Health Organization Task Force on Post-ovulatory Methods for Fertility Regulation. Comparison of two-doses of mifepristone in combination with misoprostol for early medical abortion: a randomised trial. BJOG 2000; 107: 524–530
  • Schaff E A, Eisinger S H, Stadalius L S, Franks P, Gore B Z, Poppema S. Low-dose mifepristone 200 mg and vaginal misoprostol for abortion. Contraception 1999; 59: 1–6
  • Ashok P, Penney G, Flett G, Templeton A. An effective regimen for early medical abortion: a report of 2000 consecutive cases. Hum Reprod 1998; 13: 2962–2965
  • Schaff E A, Fielding S L, Eisinger S H, Stadalius L S, Fuller L. Low-dose mifepristone followed by vaginal misoprostol at 48 hours for abortion up to 63 days. Contraception 2000; 61: 41–46
  • Schaff E A, Fielding S L, Westhoff C, Ellertson C, Eisinger S H, Stadalius L S, Fuller L. Vaginal misoprostol administrated 1, 2, or 3 days after mifepristone for early medical abortion: a randomized trial. JAMA 2000; 284: 1948–1953
  • Ashok P W, Gilian F, Templeton A. Mifepristone versus vaginally administered misoprostol for cervical priming before first-trimester termination of pregnancy: a randomized, controlled study. Am J Obstet Gynecol 2000; 183: 998–1002
  • Ngai S W, Yeung K C, Lao T, Ho P C. Oral misoprostol versus mifepristone for cervical dilatation before vacuum aspiration in first trimester nulliparous pregnancies: a double blind prospective randomized study. BJOG 1996; 103: 1120–1123
  • Tang O S, Ho P C. Clinical applications of mifepristone. Gynecol Endocrinol 2006; 22: 655–659
  • Westley E, von Hertzen H, Faundes A. Expanding access to emergency contraception. Int J Gynaecol Obstet 2007; 97: 235–237
  • Creinin M D, Schlaff W, Archer D F, Wan L, Frezieres R, Thomas M, Rosenberg M, Higgins J. Progesterone receptor modulator for emergency contraception: a randomized controlled trial. Obstet Gynecol 2006; 108: 1089–1097
  • von Hertzen H, Piaggio G, Ding J, Chen J, Song S, Bartfai G, Ng E, Gemzell-Sanielsson K, Oyunbileg A, Wu S. Low dose mifepristone and two regimens of levonorgestrel for emergency contraception: a WHO multicentre randomised trial. Lancet 2002; 360: 1803–1810
  • Comparison of three single doses of mifepristone as emergency contraception: a randomized trial. Task force on post-ovulatory methods of fertility regulation. Lancet 1999; 353: 697–702
  • Kulier R, Gulmezoglu A M, Hofmeyr G J, Cheng L N, Campana A. Medical methods for first trimester abortion (review). Cochrane Database Syst Rev 2004; 1, CD002855
  • Jin J, Weisberg E, Fraser I S. Comparison of three single doses of mifepristone as emergency contraception: a randomised controlled trial. Aust NZ J Obstet Gynaecol 2005; 45: 489–494
  • Roblero L S, Croxatto H B. Effects of RU 486 on development and implantation of rat embryos. Mol Reprod Dev 1991; 29: 342–346
  • Pisarska M D, Carson S A, Buster J E. Ectopic pregnancy. Lancet 1998; 351: 1115–1120
  • Spitz I M. Progesterone receptor antagonists. Curr Opin Investig Drugs 2006; 7: 882–890, (review)
  • Lalitkumar P GL, Lalitkumar S, Meng C X, Stavreus-Evers A, Hambiliki F, Bentin-Ley U, Gemzell-Danielsson K. Mifepristone, but not levonorgestrel, inhibits human blastocyst attachment to an in vitro endometrial three-dimensional cell culture model. Hum Reprod 2007; 22: 3031–3037
  • Croxatto H B, Salvatierra A M, Fuentealba B, Leiva L. Follicle stimulating hormone-granulosa cell axis involvement in the anti-folliculotrophic effect of low dose mifepristone (RU486). Hum Reprod 1995; 10: 1987–1991
  • Marions L, Viski S, Danielsson K G, Resch B A, Swahn M L, Bygdeman M, Kovâcs L. Contraceptive efficacy of daily administration of 0.5 mg mifepristone. Hum Reprod 1999; 14: 2788–2790
  • Bygdeman M, Danielsson K G, Marions L, Swahn M L. Contraceptive use of antiprogestin. Eur J Contracept Reprod Health Care 1999; 4: 103–107, (review)
  • Spitz I M, Chwalisz K. Progesterone receptor modulators and progesterone antagonists in women's health. Steroids 2000; 65: 807–815, (review)
  • Swahn M L, Bygdeman M, Chen J K, Gemzell-Danielsson K, Song S, Yang Q Y, Yang P J, Qian M L, Chang W F. Once-a-month treatment with a combination of mifepristone and the prostaglandin analogue misoprostol. Hum Reprod 1999; 14: 485–488
  • Gainer E E, Ulmann A. Pharmacologic properties of CDB(VA)- 2914. Steroids 2003; 68: 1005–1011
  • Attardi B J, Burgenson J, Hild S A, Reel J R. In vitro anti-progestational/anti-glucocorticoid activity and progestin and glucocorticoid receptor binding of the putative metabolites and synthetic derivatives of CDB-2914, CDB-4124, and mifepristone. J Steroid Biochem Mol Biol 2004; 88: 277–288
  • Reel J R, Hild-Petito S, Blye R P. Anti-ovulatory and post-coital antifertility activity of the antiprogestin CDB-2914 when administered as single, multiple, or continuous doses to rats. Contraception 1998; 58: 129–136
  • Chabbert-Buffet N, Pintiaux-Kairis A, Bouchard, VA2914 Study Group. Effects of the progesterone receptor modulator VA2914 in a continuous low dose on the hypothalamic-pituitary-ovarian axis and endometrium in normal women: a prospective, randomized, placebo-controlled trial. J Clin Endocrinol Metab 2007; 92: 3582–3589
  • Ravet S, Munaut C, Blacher S, Brichant G, Labied S, Beliard A, Chabbert-Buffet N, Bouchard P, Foidart J-M, Pintiaux A, Persistence of an intact endometrial matrix and vessels structure in women exposed to VA-2914, a selective progesterone receptor modulator. J Clin Endocrinol Metab 2008;93:4525–4531. Epub 2008 Aug
  • Whiteman M K, Hillis S D, Jamieson D J, Morrow B, Podgornik M N, Brett K M, Marchbanks P A. Inpatient hysterectomy surveillance in the United States, 2000–2004. AM J Obstet Gynecol 2008; 198: 34.e1–e7
  • Dodin S, Lemay A, Maheux R, Dumont M, Turcot-Lemay L. Bone mass in endometriosis patients treated with GnRH agonist implant or danazol. Obstet Gynecol 1991; 77: 410–415
  • Wang P H, Yang A H, Yuan C C, Lee W L, Chao H T. Uterine myoma after cessation of gonadotropin-releasing hormone agonist: ultrasound and histopathologic findings. Zhonghua Yi Xue Za Zhi (Taipei) 1998; 61: 625–629
  • Pavlovich S V, Volkov N I, Burlev V A. Proliferative activity and level of steroid hormone receptors in the myometrium and myoma nodes in different phases of menstrual cycle. Bull Exp Biol Med 2003; 136: 396–398
  • Nisolle M, Gillerot S, Casanas-Roux F, Squifflet J, Berliere M, Donnez J. Immunohistochemical study of the proliferation index, oestrogen receptors and progesterone receptors A and B in leiomyomata and normal myometrium during the menstrual cycle and under gonadotrophin-releasing hormone agonist therapy. Hum Reprod 1999; 14: 2844–2850
  • Brandon D D, Bethea C L, Strawn E Y, Novy M J, Burry K A, Harrington M S, Erickson T E, Warner C, Keenan E J, Clinton G M. Progesterone receptor messenger ribonucleic acid and protein are over expressed in human uterine leiomyomas. Am J Obstet Gynecol 1993; 169: 78–85
  • Harrison-Woolrych M L, Charnock-Jones D S, Smith S K. Quantification of messenger ribonucleic acid for epidermal growth factor in human myometrium and leiomyomata using reverse transcriptase polymerase chain reaction. J Clin Endocrinol Metab 1994; 78: 1179–1184
  • Matsuo H, Maruo T, Samoto T. Increased expression of Bcl-2 protein in human uterine leiomyoma and its up-regulation by progesterone. J Clin Endocrinol Metab 1997; 82: 293–299
  • Carr B R, Marshburn P B, Weatherall P T, Bradshaw K D, Breslau N A, Byrd W, Roark M, Steinkampf M P. An evaluation of the effect of gonadotropin-releasing hormone analogues and medroxyprogesterone acetate on uterine leiomyomata volume by magnetic resonance imaging: a prospective, randomized, double blind, placebo-controlled, crossover trial. J Clin Endocrinol Metab 1993; 76: 1217–1223
  • Zeng C, Gu M, Huang H, [A clinical control study on the treatment of uterine leiomyoma with gonadotrophin releasing hormone agonist or mifepristone] Zhonghua Fu Chan Ke Za Zhi 1998;33:490–492
  • Mizutani T, Sugihara A, Honma H, Komura H, Nakamuro K, Terada N. Effect of steroid add-back therapy on the proliferative activity of uterine leiomyoma cells under gonadotropin-releasing hormone agonist therapy. Gynecol Endocrinol 2005; 20: 80–83
  • Murphy A A, Morales A J, Kettel L M, Yen S S. Regression of uterine leiomyomata to the antiprogesterone RU486: dose-response effect. Fertil Steril 1995; 64: 187–190
  • Ohara N, Morikawa A, Chen W, Wang J, DeManno D A, Chwalisz K, Maruo T. Comparative effects of SPRM asoprisnil (J867) on proliferation, apoptosis, and the expression of growth factors in cultured uterine leiomyoma cells and normal myometrial cells. Reprod Sci 2007; 14(8 Suppl)20–27
  • Xu Q, Ohara N, Chen W, Liu J, Sasaki H, Morikawa A, Sitruk-Ware R, Johansson E D, Maruo T. Progesterone receptor modulator CDB-2914 down-regulates vascular endothelial growth factor, adrenomedullin and their receptors and modulates progesterone receptor content in cultured human uterine leiomyoma cells. Hum Reprod 2006; 21: 2408–2416
  • Steinauer J, Pritts E A, Jackson R, Jacoby A F. Systematic review of mifepristone for the treatment of uterine leiomyomata. Obstet Gynecol 2004; 103: 1331–1336, (review)
  • Chwalisz K, Perez M C, Demanno D, Winkel C, Schubert G, Elger W. Selective progesterone receptor modulator development and use in the treatment of leiomyomata and endometriosis. Endocr Rev 2005; 26: 423–438, (review). Erratum in: Endocr Rev 2005;26:703
  • Giudice L C, Kao L C. Endometriosis. Lancet 2004; 364: 1789–1799, (review)
  • Kyama C M, Mihalyi A, Simsa P, Mwenda J M, Tomassetti C, Meuleman C, D'Hooghe T M. Non-steroidal targets in the diagnosis and treatment of endometriosis. Curr Med Chem 2008; 15: 1006–1017, (review)
  • Rodgers A K, Falcone T. Treatment strategies for endometriosis. Expert Opin Pharmacother 2008; 9: 243–255, (review)
  • Han S, Sidell N. RU486-induced growth inhibition of human endometrial cells involves the nuclear factor-κ B signaling pathway. J Clin Endocrinol Metab 2003; 88: 713–719
  • Kettel L M, Murphy A A, Morales A J, Ulmann A, Baulieu E E, Yen S S. Treatment of endometriosis with the anti-progesterone mifepristone (RU486). Fertil Steril 1996; 65: 23–28
  • Elger W, Bartley J, Schneider B, Kaufmann G, Schubert G, Chwalisz K. Endocrine pharmacological characterization of progesterone antagonists and progesterone receptor modulators with respect to PR-agonistic and antagonistic activity. Steroids 2000; 65: 713–723, (review)
  • Mutter G L, Bergeron C, Deligdisch L, Ferenczy A, Glant M, Merino M, Williams A R, Blithe D L. The spectrum of endometrial pathology induced by progesterone receptor modulators. Mod Pathol 2008; 21: 591–598

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.