Literature DB >> 22176795

Effects of a novel estrogen-free, progesterone receptor modulator contraceptive vaginal ring on inhibition of ovulation, bleeding patterns and endometrium in normal women.

Vivian Brache1, Regine Sitruk-Ware, Alistair Williams, Diana Blithe, Horacio Croxatto, Narender Kumar, Sushma Kumar, Yun-Yen Tsong, Irving Sivin, Anita Nath, Heather Sussman, Leila Cochon, Maria Jose Miranda, Verónica Reyes, Anibal Faundes, Daniel Mishell.   

Abstract

BACKGROUND: Progesterone receptor modulators (PRMs) delivered by contraceptive vaginal rings provide an opportunity for development of an estrogen-free contraceptive that does not require daily oral intake of steroids. The objective of this proof-of-concept study was to determine whether continuous delivery of 600-800 mcg of ulipristal acetate (UPA) from a contraceptive vaginal ring could achieve 80% to 90% inhibition of ovulation. STUDY
DESIGN: This was a prospective, controlled, open-labeled, multicenter international trial to examine the effectiveness and safety of this prototype vaginal ring. Thirty-nine healthy women, 21-40 years old and not at risk of pregnancy, were enrolled at three clinic sites. Volunteers participated in a control cycle, a 12-week treatment period and a post-treatment cycle. Pharmacodynamic effects on follicular function and inhibition of ovulation, effects on endometrium, bleeding patterns and serum UPA levels were evaluated.
RESULTS: Mean UPA levels during treatment were nearly constant, approximately 5.1 ng/mL throughout the study. Ovulation was documented in 32% of 111 "4-week treatment cycles." A correlation was observed between serum UPA and degree of inhibition of ovarian activity. There was no evidence of hyperplasia of endometrium, but PRM-associated endometrial changes were frequently observed (41%).
CONCLUSION: In this study, the minimum effective contraceptive dose was not established. Further studies are required testing higher doses of UPA to attain ovulation suppression in a higher percentage of subjects.
Copyright © 2012 Elsevier Inc. All rights reserved.

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Year:  2011        PMID: 22176795      PMCID: PMC3405946          DOI: 10.1016/j.contraception.2011.10.003

Source DB:  PubMed          Journal:  Contraception        ISSN: 0010-7824            Impact factor:   3.375


  33 in total

Review 1.  Family planning: the unfinished agenda.

Authors:  John Cleland; Stan Bernstein; Alex Ezeh; Anibal Faundes; Anna Glasier; Jolene Innis
Journal:  Lancet       Date:  2006-11-18       Impact factor: 79.321

2.  Serum Nestorone and ethinyl estradiol levels, and ovulation inhibition in women using three different dosage combinations of a Nestorone progestogen-ethinyl estradiol contraceptive vaginal ring on a bleeding-signaled regimen.

Authors:  Ian S Fraser; Edith Weisberg; Vivian Brache; Francisco Alvarez; Rebeca Massai; Daniel R Mishell; Dan Apter; Judi Gale; Yun Yen Tsong; Irving Sivin
Journal:  Contraception       Date:  2005-07       Impact factor: 3.375

3.  A novel estrogen-free oral contraceptive pill for women: multicentre, double-blind, randomized controlled trial of mifepristone and progestogen-only pill (levonorgestrel).

Authors:  F Lakha; P C Ho; Z M Van der Spuy; K Dada; R Elton; A F Glasier; H O D Critchley; A R W Williams; D T Baird
Journal:  Hum Reprod       Date:  2007-07-03       Impact factor: 6.918

4.  The spectrum of endometrial pathology induced by progesterone receptor modulators.

Authors:  George L Mutter; Christine Bergeron; Liane Deligdisch; Alex Ferenczy; Mick Glant; Maria Merino; Alistair R W Williams; Diana L Blithe
Journal:  Mod Pathol       Date:  2008-02-08       Impact factor: 7.842

Review 5.  Progesterone receptor antagonists and the endometrial antiproliferative effect.

Authors:  Robert M Brenner; Ov D Slayden
Journal:  Semin Reprod Med       Date:  2005-02       Impact factor: 1.303

6.  A novel pathway involving progesterone receptor, endothelin-2, and endothelin receptor B controls ovulation in mice.

Authors:  Gopinath S Palanisamy; Yong-Pil Cheon; Jaeyeon Kim; Athilakshmi Kannan; Quanxi Li; Marcey Sato; Srinivasa R Mantena; Regine L Sitruk-Ware; Milan K Bagchi; Indrani C Bagchi
Journal:  Mol Endocrinol       Date:  2006-08-03

7.  The effects of 1-month administration of asoprisnil (J867), a selective progesterone receptor modulator, in healthy premenopausal women.

Authors:  Kristof Chwalisz; Walter Elger; Therese Stickler; Cynthia Mattia-Goldberg; Lois Larsen
Journal:  Hum Reprod       Date:  2005-01-21       Impact factor: 6.918

8.  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.

Authors:  Nathalie Chabbert-Buffet; Axelle Pintiaux-Kairis; Philippe Bouchard
Journal:  J Clin Endocrinol Metab       Date:  2007-06-19       Impact factor: 5.958

9.  Ulipristal acetate taken 48-120 hours after intercourse for emergency contraception.

Authors:  Paul Fine; Henri Mathé; Savita Ginde; Vanessa Cullins; Johanna Morfesis; Erin Gainer
Journal:  Obstet Gynecol       Date:  2010-02       Impact factor: 7.661

10.  Progesterone receptor modulators and the endometrium: changes and consequences.

Authors:  Frances McFarland Horne; Diana L Blithe
Journal:  Hum Reprod Update       Date:  2007-07-14       Impact factor: 15.610

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  8 in total

Review 1.  Drug delivery for the treatment of endometriosis and uterine fibroids.

Authors:  David R Friend
Journal:  Drug Deliv Transl Res       Date:  2017-12       Impact factor: 4.617

Review 2.  Contraception technology: past, present and future.

Authors:  Regine Sitruk-Ware; Anita Nath; Daniel R Mishell
Journal:  Contraception       Date:  2012-09-17       Impact factor: 3.375

Review 3.  Pipeline for contraceptive development.

Authors:  Diana L Blithe
Journal:  Fertil Steril       Date:  2016-08-11       Impact factor: 7.329

Review 4.  Vaginal ring delivery of selective progesterone receptor modulators for contraception.

Authors:  Jeffrey T Jensen
Journal:  Contraception       Date:  2012-10-04       Impact factor: 3.375

5.  A randomized study on pharmacodynamic effects of vaginal rings delivering the progesterone receptor modulator ulipristal acetate: research for a novel estrogen-free, method of contraception.

Authors:  YongMei Huang; Jeffrey T Jensen; Vivian Brache; Leila Cochon; Alistair Williams; Maria-José Miranda; Horacio Croxatto; Narender Kumar; Heather Sussman; Elena Hoskin; Marlena Plagianos; Kevin Roberts; Ruth Merkatz; Diana Blithe; Regine Sitruk-Ware
Journal:  Contraception       Date:  2014-08-12       Impact factor: 3.375

6.  The optimization of an intravaginal ring releasing progesterone using a mathematical model.

Authors:  Ignacio M Helbling; Juan C D Ibarra; Julio A Luna
Journal:  Pharm Res       Date:  2013-10-18       Impact factor: 4.200

Review 7.  Priority strategies for India's family planning programme.

Authors:  Saroj Pachauri
Journal:  Indian J Med Res       Date:  2014-11       Impact factor: 2.375

8.  Cervical and systemic concentrations of long acting hormonal contraceptive (LARC) progestins depend on delivery method: Implications for the study of HIV transmission.

Authors:  Lyndsey R Buckner; Erma Z Drobnis; Molly S Augustine; Lynette K Rogers; Jill Akers; Patricia D Mott; Thomas J Hope; Alison J Quayle; Danny J Schust
Journal:  PLoS One       Date:  2019-05-16       Impact factor: 3.240

  8 in total

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