554
Views
5
CrossRef citations to date
0
Altmetric
Drug Evaluation

Vilaprisan for treating uterine fibroids

ORCID Icon, ORCID Icon, ORCID Icon, ORCID Icon, ORCID Icon, ORCID Icon, ORCID Icon, ORCID Icon, ORCID Icon, ORCID Icon & ORCID Icon show all
Pages 497-505 | Received 05 Feb 2018, Accepted 26 Apr 2018, Published online: 07 May 2018

References

  • Bulun S. Uterine fibroids. N Engl J Med. 2013;369:1344–1365.
  • Catherino WH, Parrott E, Segars J. Proceedings from the national institute of child health and human development conference on the uterine fibroid research update workshop. Fertil Steril. 2011;95:9–12.
  • Donnez J, Jadoul P. What are the implications of myomas on fertility? A need for a debate? Hum Reprod. 2002;17:1424–1430.
  • Ben-Nagi J, Miell J, Mavrelos D, et al. Endometrial implantation factors in women with submucous uterine fibroids. Reprod Biomed Online. 2010;21:610–615.
  • Sunkara SK, Khairy M, El-Toukhy T, et al. The effect of intramural fibroids without uterine cavity involvement on the outcome of IVF treatment: a systematic review and meta-analysis. Hum Reprod. 2010;25:418–429.
  • Donnez J, Dolmans MM. Uterine fibroid management: from the present to the future. Hum Reprod Update. 2016;22:665–686.
  • Linder D, Gartler SM. Glucose-6-phosphate dehydrogenase mosaicism: utilization as a cell marker in the study of leiomyomas. Science. 1965;150:67–69.
  • Ono M, Qiang W, Serna VA, et al. Role of stem cells in human uterine leiomyoma growth. PLoS One 2012;7:e36935.
  • Tanwar PS, Lee HJ, Zhang L, et al. Constitutive activation of beta-catenin in uterine stroma and smooth muscle leads to the development of mesenchymal tumors in mice. Biol Reprod. 2009;81:545–552.
  • Arici A, Sozen I. Transforming growth factor-beta3 is expressed at high levels in leiomyoma where it stimulates fibronectin expression and cell proliferation. Fertil Steril. 2000;73:1006–1011.
  • Marsh EE, Bulun SE. Steroid hormones and leiomyomas. Obstet Gynecol Clin North Am. 2006;33:59–67.
  • Parsanezhad ME, Azmoon M, Alborzi S, et al. A randomized, controlled clinical trial comparing the effects of aromatase inhibitor (letrozole) and gonadotropin releasing hormone agonist (triptorelin) on uterine leiomyoma volume and hormonal status. Fertil Steril. 2010;93:192–198.
  • Ishikawa H, Ishi K, Serna VA, et al. Progesterone is essential for maintenance and growth of uterine leiomyoma. Endocrinology. 2010;151:2433–2442.
  • Lamminen S, Rantala I, Helin H, et al. Proliferative activity of human uterine leiomyoma cells as measured by automatic image analysis. Gynecol Obstet Invest. 1992;34:111–114.
  • Stewart EA. Clinical practice. Uterine fibroids. N Engl J Med. 2015;372:1646–1655.
  • Pérez-López FR, Ornat L, Ceausu I, et al. EMAS position statement: management of uterine fibroids. Maturitas. 2014;79:106–116.
  • Marret H, Fritel X, Ouldamer L, et al. Therapeutic management of uterine fibroid tumors: updated French guidelines. Eur J Obstet Gynecol Reprod Biol. 2012;165:156–164.
  • Mais V, Ajossa S, Guerriero S, et al. Laparoscopic versus abdominal myomectomy: a prospective, randomized trial to evaluate benefits in early outcome. Am J Obstet Gynecol. 1996;174:654–658.
  • Jin C, Hu Y, Chen XC, et al. Laparoscopic versus open myomectomy - a metaanalysis of randomized controlled trials. Eur J Obstet Gynecol Reprod Biol. 2009;145:14–21.
  • US Food and Drug Administration. Laparoscopic uterine power morcellation in hysterectomy and myomectomy, FDA safety communication. 2014 [cited 2016 Jul 4]. Available from: https://wayback.archive-it.org/7993/20170404182209/https:/www.fda.gov/MedicalDevices/Safety/AlertsandNotices/ucm424443.htm
  • Bosteels J, Weyers S, Kasius J, et al. Anti-adhesion therapy following operative hysteroscopy for treatment of female subfertility. Cochrane Database Syst Rev. 2015;11:CD011110.
  • Borah BJ, Nicholson WK, Bradley L, et al. The impact of uterine leiomyomas: a national survey of affected women. Am J Obstet Gynecol. 2013;209:319.e1-319.e20.
  • Qin J, Yang T, Kong F, et al. Oral contraceptive use and uterine leiomyoma risk: a meta-analysis based on cohort and case-control studies. Arch GynecolObstet. 2013;288:139–148.
  • Hoellen F, Griesinger G, Bohlmann MK. Therapeutic drugs in the treatment of symptomatic uterine fibroids. Expert Opin Pharmacother. 2013;14:2079–2085.
  • Duhan N, Madaan S, Sen J. Role of the aromatase inhibitor letrozole in the management of uterine leiomyomas in premenopausal women. Eur J Obstet Gynecol Reprod Biol. 2013;171:329–332.
  • Song H, Lu D, Navaratnam K, et al. Aromatase inhibitors for uterine fibroids. Cochrane Database Syst Rev. 2013;10:CD009505.
  • Donnez J, Schrurs B, Gillerot S, et al. Treatment of uterine fibroids with implants of gonadotropin-releasing hormone agonist: assessment by hysterography. Fertil Steril. 1989;51:947–950.
  • Lethaby A, Vollenhoven B, Sowter M. Pre-operative GnRH analogue therapy before hysterectomy or myomectomy for uterine fibroids. Cochrane Database Syst Rev. 2001;Issue 2. Art. No.: CD000547..
  • Gutmann JN, Corson SL. GnRH agonist therapy before myomectomy or hysterectomy. J Minim Invasive Gynecol. 2005;12:529–537.
  • Paoletti AM, Serra GG, Cagnacci A, et al. Spontaneous reversibility of bone loss induced by gonadotropin-releasing hormone analog treatment. Fertil Steril. 1996;65:707–710.
  • Lethaby AE, Vollenhoven BJ. An evidence-based approach to hormonal therapies for premenopausal women with fibroids. Best Pract Res Clin Obstet Gynaecol. 2008;22:307–331.
  • Bouchard P, Chabbert-Buffet N, Fauser BC. Selective progesterone receptor modulators in reproductive medicine: pharmacology, clinical efficacy and safety. Fertil Steril. 2011;96:1175–1189.
  • Singh SS, Belland L, Leyland N, et al. The past, present, and future of selective progesterone receptor modulators in the management of uterine fibroids. Am J Obstet Gynecol. 2017;S0002-9378:32697–32702.
  • Wagenfeld A, Saunders PT, Whitaker L, et al. Selective progesterone receptor modulators (SPRMs): progesterone receptor action, mode of action on the endometrium and treatment options in gynecological therapies. Expert Opin Ther Targets. 2016;20:1045–1054.
  • Xu Q, Ohara N, Liu J, et al. Progesterone receptor modulator CDB-2914 induces extracellular matrix metalloproteinase inducer in cultured human uterine leiomyoma cells. Mol Hum Reprod. 2008;14:181–191.
  • Murphy AA, Kettel LM, Morales AJ, et al. Regression of uterine leiomyomata in response to the antiprogesterone RU 486. J Clin Endocrinol Metab. 1993;76:513–517.
  • Eisinger SH, Meldrum S, Fiscella K, et al. Low-dose mifepristone for uterine leiomyomata. Obstet Gynecol. 2003;101:243–250.
  • Shen Q, Hua Y, Jiang W, et al. Effects of mifepristone on uterine leiomyoma in premenopausal women: a meta-analysis. Fertil Steril. 2013;100:1722–1726.
  • Tristan M, Orozco LJ, Steed A, et al. Mifepristone for uterine fibroids. Cochrane Database Syst Rev. 2012;8:CD007687.
  • EPAR summary for the public: Esmya (ulipristal acetate). European Medicines Agency. 2012 [cited 2018 Jan 10]. Available from: http://www.ema.europa.eu/ema/index.jsp?curl=pages/medicines/human/medicines/002041/human_med_001542.jsp&mid=WC0b01ac058001d124
  • Chwalisz K, Larsen L, Mattia-Goldberg C, et al. A randomized, controlled trial of asoprisnil, a novel selective progesterone receptor modulator, in women with uterine leiomyomata. Fertil Steril. 2007;87:1399–1412.
  • Wilkens J, Chwalisz K, Han C, et al. Effects of the selective progesterone receptor modulator asoprisnil on uterine artery blood flow, ovarian activity, and clinical symptoms in patients with uterine leiomyomata scheduled for hysterectomy. J Clin Endocrinol Metab. 2008;93:4664–4671.
  • Wiehle R, Goldberg J, Brodniewicz T, et al. Effects of a new progesterone receptor modulator, CDB-4124, on fibroid size and uterine bleeding. US Obstetr Gynaecol. 2008;3:17–20.
  • Donnez J, Tatarchuk TF, Bouchard P, et al. Ulipristal acetate versus placebo for fibroid treatment before surgery. N Engl J Med. 2012;366:409–420.
  • Donnez J, Tomaszewski J, Vazquez F, et al. Ulipristal acetate versus leuprolide acetate for uterine fibroids. N Engl J Med. 2012;366:421–432.
  • Biglia N, Carinelli S, Maiorana A, et al. Ulipristal acetate: a novel pharmacological approach for the treatment of uterine fibroids. Drug Des Dev Ther. 2014;8:285–292.
  • Donnez J, Donnez O, Matule D, et al. Long-term medical management of uterine fibroids with ulipristal acetate. Fertil Steril. 2016;105:165–173.
  • Fauser BC, Donnez J, Bouchard P, et al. Safety after extended repeated use of ulipristal acetate for uterine fibroids. PLoS One 2017;12:e0173523.
  • Mutter GL, Bergeron C, Deligdisch L, et al. The spectrum of endometrial pathology induced by progesterone receptor modulators. Mod Pathol. 2008;21:591–598.
  • Williams AR, Bergeron C, Barlow DH, et al. Endometrial morphology after treatment of uterine fibroids with the selective progesterone receptor modulator, ulipristal acetate. Int J Gynecol Pathol. 2012;31:556–569.
  • Bouchard P, Chabbert-Buffet N. The history and use of the progesterone receptor modulator ulipristal acetate for heavy menstrual bleeding with uterine fibroids. Best Pract Res Clin Obstet Gynaecol. 2017;40:105–110.
  • National Center for Biotechnology Information. PubChem compound database. CID=50915138. 2011 [cited 2018 Jan 24]. Available from: https://pubchem.ncbi.nlm.nih.gov/compound/50915138
  • Wagenfeld A, Bone W, Schwede W, et al. BAY 1002670: a novel, highly potent and selective progesterone receptor modulator for gynaecological therapies. Hum Reprod. 2013;28:2253–2264.
  • Schütt B, Kaiser A, Schultze-Mosgau M-H, et al. Pharmacodynamics and safety of the novel selective progesterone receptor modulator vilaprisan: a double-blind, randomized, placebo-controlled phase 1 trial in healthy women. Hum Reprod. 2016;31:1703–1712.
  • Schultze-Mosgau M-H, Schuett B, Hafner F-T, et al. Pharmacokinetics and safety of the selective progesterone receptor modulator vilaprisan in healthy postmenopausal women. Int J Clin Pharmacol Ther. 2017;55:16–24.
  • Schultze-Mosgau MH, Höchel J, Prien O, et al. Characterization of the pharmacokinetics of vilaprisan: bioavailability, excretion, biotransformation, and drug-drug interaction potential. Clin Pharmacokinet 2018. doi: 10.1007/s40262-017-0607-4.
  • Schütt B, Schultze-Mosgau MH, Draeger C, et al. Effect of the novel selective progesterone receptor modulator vilaprisan on ovarian activity in healthy women. J Clin Pharmacol. 2018;58:228–239.
  • Bradley L, Ren X, Groettrup-Wolfers E, et al. Results of the asteroid (assess safety and efficacy of vilaprisan in patients with uterine fibroids) 1 study: A phase 2, placebo-controlled dose finding study. Fertil Steril. 2016;106:e95–e96.
  • Seitz C, Bumbuliene Ž, Costa AR, et al. Rationale and design of ASTEROID 2, a randomized, placebo- and active comparator-controlled study to assess the efficacy and safety of vilaprisan in patients with uterine fibroids. Contemp Clin Trials. 2017;55:56–62.
  • Bayer starts phase III study program with vilaprisan in the treatment of symptomatic uterine fibroids. Germany: Investor news. Leverkusen. 2017 [cited 2018 Jan 28]. Available from: https://www.investor.bayer.de/en/nc/news/investor-news/investor-news/bayer-starts-phase-iii-study-program-with-vilaprisan-in-the-treatment-of-symptomatic-uterine-fibroid/
  • Zimmermann A, Bernuit D, Gerlinger C, et al. Prevalence, symptoms and management of uterine fibroids: an international internet-based survey of 21,746 women. BMC Womens Health 2012 Mar 26;12:6.
  • Ludwig H, Strasser K. Symptomatology of anemia. Semin Oncol. 2001;28(2 Suppl 8):7–14.
  • Turkoski BB. Tired blood. Part 2. Orthop Nur. 2003;22:363–368.
  • Attardi BJ, Burgenson J, Hild SA, et al. 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. J Steroid Biochem Mol Biol. 2004;88:277–288.
  • Archer DF, Stewart EA, Jain RI, et al. Elagolix for the management of heavy menstrual bleeding associated with uterine fibroids: results from a phase 2a proof-of-concept study. Fertil Steril. 2017;108:152–60.e4.

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.