Literature DB >> 25193534

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.

YongMei Huang1, Jeffrey T Jensen2, Vivian Brache3, Leila Cochon3, Alistair Williams4, Maria-José Miranda5, Horacio Croxatto6, Narender Kumar1, Heather Sussman1, Elena Hoskin1, Marlena Plagianos1, Kevin Roberts1, Ruth Merkatz1, Diana Blithe7, Regine Sitruk-Ware8.   

Abstract

OBJECTIVE: To determine whether a 3-month contraceptive vaginal ring (CVR) delivering ulipristal acetate (UPA) can inhibit ovulation in 90% of cycles. STUDY
DESIGN: This was a randomized dose-finding parallel group clinical trial. Fifty-five healthy women with normal ovulation at baseline were randomized to receive a low-dose (1500 μg/day) or a high-dose (2500 μg/day) UPA-CVR for two consecutive 12-week treatment periods, followed by a recovery cycle. A subgroup of women received levonorgestrel (LNG) 1.5 mg orally twice (at the end of both 12-week ring periods) or once (at the end of the 24-week treatment). The primary outcome was ovulation suppression assessed by transvaginal ultrasound and hormone levels. Secondary outcomes included endometrial safety and bleeding patterns.
RESULTS: All subjects showed normal ovulation at baseline and recovery. Ovulation suppression was seen in 81.8% (95% CI: 73.3%, 88.5%) and 86.1% (95% CI: 78.1%, 92%) of treatment cycles with low and high-dose, respectively. Benign progesterone receptor modulator associated endometrial changes (PAEC) were seen during treatment; 78.8% at week 24, but resolved at recovery cycle. A few cases of heavy bleeding occurred near the end of the 24-week treatment, but a single dose of LNG every 12 weeks reduced the increase in endometrial thickness during the second treatment period and prevented excessive bleeding.
CONCLUSION: The 3-month UPA-CVR may become an effective long-acting, user-controlled estrogen-free contraceptive. The greatest suppression of ovulation was seen with the 2500-μg/day ring. IMPLICATIONS: The 3-month CVR delivering UPA 2500 μg/day can become an effective user-controlled estrogen-free contraceptive method. Benign PAEC during treatment returns to normal after discontinuation. The prevention of occasional excessive withdrawal bleeding, either by a progestin or by using higher UPA levels to increase follicle suppression may permit prolonged treatment.
Copyright © 2014 Elsevier Inc. All rights reserved.

Entities:  

Keywords:  Contraception; Endometrium; Pharmacodynamics; Ulipristal acetate; Vaginal ring

Mesh:

Substances:

Year:  2014        PMID: 25193534      PMCID: PMC4253673          DOI: 10.1016/j.contraception.2014.08.006

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


  21 in total

1.  Immunocytochemical assessment of mitotic activity with an antibody to phosphorylated histone H3 in the macaque and human endometrium.

Authors:  Robert M Brenner; Ov D Slayden; William H Rodgers; Hilary O D Critchley; Rebecca Carroll; Xiao Jing Nie; Kuni Mah
Journal:  Hum Reprod       Date:  2003-06       Impact factor: 6.918

2.  In vitro antiprogestational/antiglucocorticoid activity and progestin and glucocorticoid receptor binding of the putative metabolites and synthetic derivatives of CDB-2914, CDB-4124, and mifepristone.

Authors:  Barbara J Attardi; Janet Burgenson; Sheri A Hild; Jerry R Reel
Journal:  J Steroid Biochem Mol Biol       Date:  2004-03       Impact factor: 4.292

3.  Ulipristal acetate does not impact human normal breast tissue.

Authors:  Laudine Communal; Myriam Vilasco; Justine Hugon-Rodin; Aurélie Courtin; Najat Mourra; Najiba Lahlou; Sylvie Dumont; Marc Chaouat; Patricia Forgez; Anne Gompel
Journal:  Hum Reprod       Date:  2012-06-26       Impact factor: 6.918

4.  Endometrial morphology after treatment of uterine fibroids with the selective progesterone receptor modulator, ulipristal acetate.

Authors:  Alistair R W Williams; Christine Bergeron; David H Barlow; Alex Ferenczy
Journal:  Int J Gynecol Pathol       Date:  2012-11       Impact factor: 2.762

5.  Pharmacokinetic study of different dosing regimens of levonorgestrel for emergency contraception in healthy women.

Authors:  Elof Johansson; Vivian Brache; Frank Alvarez; Anibal Faundes; Leila Cochon; Sirpa Ranta; Mark Lovern; Narender Kumar
Journal:  Hum Reprod       Date:  2002-06       Impact factor: 6.918

6.  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

7.  Pharmacologic properties of CDB(VA)-2914.

Authors:  Erin E Gainer; André Ulmann
Journal:  Steroids       Date:  2003-11       Impact factor: 2.668

Review 8.  Vaginal ring delivery of selective progesterone receptor modulators for contraception.

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

Review 9.  Emergency contraception -- mechanisms of action.

Authors:  Kristina Gemzell-Danielsson; Cecilia Berger; Lalitkumar P G L
Journal:  Contraception       Date:  2012-10-29       Impact factor: 3.375

10.  Effect of long-term treatment with low-dose mifepristone on the endometrium.

Authors:  D T Baird; A Brown; H O D Critchley; A R Williams; S Lin; L Cheng
Journal:  Hum Reprod       Date:  2003-01       Impact factor: 6.918

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  4 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.  Pipeline for contraceptive development.

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

3.  Impact of the menstrual cycle and ethinyl estradiol/etonogestrel contraceptive vaginal ring on granulysin and other mucosal immune mediators.

Authors:  Sean M Hughes; Urvashi Pandey; Christine Johnston; Jeanne Marrazzo; Florian Hladik; Elizabeth Micks
Journal:  Am J Reprod Immunol       Date:  2021-03-16       Impact factor: 3.777

Review 4.  90 YEARS OF PROGESTERONE: Selective progesterone receptor modulators in gynaecological therapies.

Authors:  H O D Critchley; R R Chodankar
Journal:  J Mol Endocrinol       Date:  2020-07       Impact factor: 5.098

  4 in total

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