372
Views
24
CrossRef citations to date
0
Altmetric
Drug Evaluations

Pharmacokinetic evaluation of ulipristal acetate for uterine leiomyoma treatment

, MD, , MD, , MD, , PhD, , MD, , MD, , MD, , MD, , MD & , MD show all
Pages 901-908 | Published online: 10 Jun 2012

Bibliography

  • Buttram VC Jr, Reiter RC. Uterine leiomyomata: etiology, symptomatology, and management. Fertil Steril 1981;36:433-45
  • Stewart EA. Uterine fibroids. Lancet 2001;357:293-8
  • Garcia CR, Tureck RW. Submucosal leiomyomas and infertility. Fertil Steril 1984;42:16-19
  • Rice JP, Kay HH, Mahony BS. The clinical significance of uterine leiomyomas in pregnancy. Am J Obstet Gynecol 1989;160:1212-16
  • Kjerulff KH, Langenberg P, Seidman JD, Uterine leiomyomas: racial differences in severity, symptoms and age at diagnosis. J Reprod Med 1996;41:483-90
  • Cheng M-H, Chao H-T, Wang P-H. Medical treatment for uterine myomas. Taiwan J Obstet Gynecol 2008;47:18-23
  • Ross RK, Pike MC, Vessey MP, Risk factors for uterine fibroids: reduced risk associated with oral contraceptives. BMJ 1986;293:359-62
  • Parazzini F, La Vecchia C, Negri E, Epidemiologic characteristics of women with uterine fibroids: a case control study. Obstet Gynecol 1988;72:853-7
  • Filicori M, Hall DA, Loughlin JS, A conservative approach to the management of uterine leiomyoma: pituitary desensitization by a luteinizing hormone-releasing hormone analogue. Am J Obstet Gynecol 1983;147:726-7
  • Shaw RW. New approaches to the management of fibroids. Curr Opin Obstet Gynecol 1991;3:859-64
  • Stovall TG, Muneyyirci-Delale O, Summit RL Jr, Scialli AR. GnRH agonist and iron versus placebo and iron in the anemic patient before surgery for leiomyomas: a randomized controlled trial. Obstet Gynecol 1995;86:64-71
  • Paoletti AM, Serra GG, Cagnacci A, Spontaneous reversibility of bone loss induced by gonadotropin-releasing hormone analog treatment. Fertil Steril 1996;65:707-10
  • Sayed GH, Zakherah MS, El-Nashar SA, Shaaban MM. A randomized clinical trial of a levonorgestrel-releasing intrauterine system and a low-dose combined oral contraceptive for fibroid-related menorrhagia. Int J Gynaecol Obstet 2011;112:126-30
  • Soysal S, Soysal ME. The efficacy of levonorgestrel-releasing intrauterine device in selected cases of myoma-related menorrhagia: a prospective controlled trial. Gynecol Obstet Invest 2005;59:29-35
  • Starczewski A, Iwanicki M. Intrauterine therapy with levonorgestrel releasing IUD of women with hypermenorrhea secondary to uterine fibroids. Ginekol Pol 2000;71:1221-5
  • Wildemeersch D, Schacht E. The effect on menstrual blood loss in women with uterine fibroids of a novel ‘‘frameless'' intrauterine levonorgestrel releasing drug delivery system: a pilot study. Eur J Obstet Gynecol Reprod Biol 2002;102:74-9
  • Freed M, Spies JB. Uterine artery embolization for fibroids: a review of current outcomes. Semin Reprod Med 2010;28:235-41
  • Edwards RD, Moss JG, Lumsden M, Uterine-artery embolization versus surgery for symptomatic uterine fibroids. N Engl J Med 2007;356:360-70
  • Al Hilli MM, Stewart E. Magnetic resonance-guided focused ultrasound surgery. Semin Reprod Med 2010;28:242-9
  • Cermik D, Arici A, Taylor HS. Coordinated regulation of HOX gene expression in myometrium and uterine leiomyoma. Fertil Steril 2002;78:979-84
  • Kawaguchi K, Fujii S, Konishi I, Immunohistochemical analysis of oestrogen receptors, progesterone receptors and Ki-67 in leiomyoma and myometrium during the menstrual cycle and pregnancy. Virchows Arch A Pathol Anat Histopathol 1991;419:309-15
  • Mixson WT, Hammond DO. Response of fibromyomas to a progestin. Am J Obstet Gynecol 1961;82:754-60
  • Lamminen S, Rantala I, Helin H, Proliferative activity of human uterine leiomyoma cells as measured by automatic image analysis. Gynecol Obstet Invest 1992;34:111-14
  • Carr BR, Marshburn PB, Weatherall PT, An evaluation of the effect of gonadotropin releasing hormone analogs 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;76:1217-23
  • Friedman AJ, Daly M, Juneau-Norcross M, Long-term medical therapy for leiomyomata uteri: a prospective, randomized study of leuprolide acetate depot plus either oestrogen-progestin or progestin ‘add-back' for 2 years. Hum Reprod 1994;9:1618-25
  • Mangelsdorf DJ, Thummel C, Beato M, 1995; The nuclear receptor superfamily: the second decade. Cell 1995;83:835-9
  • Robinson-Rechavi M, Escriva Garcia H, Laudet V. The nuclear receptor superfamily. J Cell Sci 2003;116:585-6
  • Marelli G, Codegoni AM, Bizzi A. Estrogen and progesterone receptors in leiomyomas and normal uterine tissues during reproductive life. Acta Eur Fertil 1989;20:19-22
  • Sadan O, van Iddekinge B, van Gelderen CJ, Oestrogen and progesterone receptor concentrations in leiomyoma and normal myometrium. Ann Clin Biochem 1987;24(Pt 3):263-7
  • Nisolle M, Gillerot S, Casanas-Roux F, 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 gonadotropin releasing hormone agonist therapy. Hum Reprod 1999;14:2844-50
  • Viville B, Charnock-Jones DS, Sharkey AM, Distribution of the A and B forms of the progesterone receptor messenger ribonucleic acid and protein in uterine leiomyomata and adjacent myometrium. Hum Reprod 1997;12:815-22
  • Maruo T, Ohara N, Wang J, Matsuo H. Sex steroidal regulation of uterine leiomyoma growth and apoptosis. Hum Reprod Update 2004;10:207-20
  • Wardell SE, Edwards DP. Mechanisms controlling agonist and antagonist potential of selective progesterone receptor modulators (SPRMs). Semin Reprod Med 2005;23:9-21
  • Elger W, Bartley J, Schneider B, Endocrine pharmacological characterization of progesterone antagonists and progesteronereceptor modulators with respect to PR-agonist and antagonist activity. Steroids 2000;65:713-23
  • Spitz I. Progesterone antagonists and progesterone receptor modulators: an overview. Steroids 2003;68:981-93
  • Murphy AA, Kettel LM, Morales AJ, Regression of uterine leiomyomata in response to the antiprogesterone RU 486. J Clin Endocrinol Metab 1993;76:513-17
  • Fiscella K, Eisinger SH, Meldrum S, Effect of mifepristone for symptomatic leiomyomata on quality of life and uterine size: a randomized controlled trial. Obstet Gynecol 2006;108:1381-7
  • Carbonell Esteve JL, Acosta R, Heredia B, Mifepristone for the treatment of uterine leiomyomas: a randomized controlled trial. Obstet Gynecol 2008;112:1029-36
  • Neef G, Beier S, Elger W, New steroids with antiprogestational and antiglucocorticoid activities. Steroids 1984;44:349-72
  • Gagne D, Pons M, Crates de Paulet A. Analysis of the relation between receptor binding affinity and antagonist efficacy of antiglucocorticoids. J Steroid Biochem 1986;25:315-22
  • Busso N, Collart M, Vassalli JD, Belin D. Antagonist effect of RU486 on transcription of glucocorticoid-regulated genes. Exp Cell Res 1987;173:425-30
  • Gainer EE, Ulmann A. Pharmacologic properties of CDB(VA)-2914. Steroids 2003;68:1005-11
  • Attardi BJ, Burgenson J, Hild SA, Reel JR. 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;88:277-88
  • Passaro MD, Piquion J, Mullen N, Luteal phase dose-response relationships of the antiprogestin CDB-2914 in normally cycling women. Hum Reprod 2003;18:1820-7
  • Hild SA, Reel JR, Hoffman LH, Blye RP. CDB-2914: anti-progestational/anti-glucocorticoid profile and post-coital anti-fertility activity in rats and rabbits. Hum Reprod 2000;15:822-9
  • Attardi BJ, Hild SA, Reel JR, Blye RP. CDB-4124 [17alpha-acetoxy-11beta-(4-N,N-dimethylaminophenyl)-21-methoxy-19-norpregna-4,9-diene-3,20-dione]: a potent antiprogestin with antiovulatory and postcoital antifertility activity [abstract 1293]. Proceedings of the Program of the 82nd Annual Meeting of the Endocrine Society; Toronto, Canada; 2000
  • Attardi BJ, Burgenson J, Hild SA, CDB-4124 and its putative monodemethylated metabolite, CDB-4453, are potent antiprogestins with reduced antiglucocorticoid activity: in vitro comparison to mifepristone and CDB-2914. Mol Cell Endocrinol 2002;188:111-23
  • Wang J, Ohara N, Wang Z, A novel selective progesterone receptor modulator asoprisnil (J867) down-regulates the expression of EGF, IGF-I, TGFbeta3 and their receptors in cultured uterine leiomyoma cells. Hum Reprod 2006;21:1869-77
  • Xu Q, Ohara N, Chen W, 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;21:2408-16
  • Larner JM, Reel JR, Blye RP. Circulating concentrations of the antiprogestin CDB-2914 and mifepristone in the female rhesus monkey following various routes of administration. Hum Reprod 2000;15:1100-6
  • Blithe DL, Nieman LK, Blye RP, Development of the selective progesterone receptor modulator CDB-2914 for clinical indications. Steroids 2003;68:1013-17
  • Reel JR, Hild-Petito S, Blye RP. Antiovulatory and postcoital antifertility activity of the antiprogestin CDB-2914 when administered as single multiple or continuous doses to rats. Contraception 1998;58:129-36
  • Stratton P, Hartog B, Hajizadeh N, A single middle-follicular dose of CDB-2914, a new antiprogestin, inhibits folliculogenesis and endometrial differentiation in normally cycling women. Hum Reprod 2000;15:1092-9
  • Levens ED, Potlog-Nahari C, Armstrong AY, CDB-2914 for uterine leiomyomata treatment: a randomized controlled trial. Obstet Gynecol 2008;111:1129-36
  • Chabbert-Buffet N, Pintiaux-Kairis A, Bouchard P; on behalf of the 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;92:3582-9
  • Nieman LK, Blocker W, Nansel T, Efficacy and tolerability of CDB-2914 treatment for symptomatic uterine fibroids: a randomized double-blind, placebo-controlled, phase IIb study. Fertil Steril 2011;95:767-72; e1-2
  • Donnez J, Tatarchuk T, Bouchard P, for the PEARL I Study Group. Ulipristal acetate versus placebo for fibroid treatment before surgery. N Engl J Med 2012;366:409-20
  • Donnez J, Tomaszewski J, Vazquez F, for the PEARL II Study Group. Ulipristal acetate versus leuprolide acetate for uterine fibroids. N Engl J Med 2012;366:421-32
  • Higham JM, O'Brien PM, Shaw RW. Assessment of menstrual blood loss using a pictorial chart. Br J Obstet Gynaecol 1990;97:734-9
  • Lethaby A, Vollenhoven B, Sowter M. Pre-operative GnRH analogue therapy before hysterectomy of myomectomy for uterine fibroids. Cochrane Database Syst Rev 2001;CD000547
  • Stovall TG, Muneyyirci-Delale O, Summit RL Jr, Scialli AR. GnRH agonist and iron versus placebo and iron in the anemic patient before surgery for leiomyomas: a randomized controlled trial. Obstet Gynecol 1995;86:65-71
  • Mutter GL, Bergeron C, Deligdisch L, The spectrum of endometrial pathology induced by progesterone receptor modulators. Mod Pathol 2008;21:591-8
  • Bagaria M, Suneja A, Vaid NB, Low-dose mifepristone in treatment of uterine leiomyoma: a randomised double-blind placebo-controlled clinical trial. Aust NZ J Obstet Gynaecol 2009;49:77-83
  • Carbonell Esteve JL, Acosta R, Heredia B, Mifepristone for the treatment of uterine leiomyomas: a randomized controlled trial. Obstet Gynecol 2008;112:1029-36
  • Steinauer J, Pritts EA, Jackson R, Jacoby AF. Systematic review of mifepristone for the treatment of uterine leiomyomata. Obstet Gynecol 2004;103:1331-6

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.