Selective progesterone receptor modulators: an update

Expert Opin Pharmacother. 2014 Jul;15(10):1403-15. doi: 10.1517/14656566.2014.914494. Epub 2014 Apr 30.

Abstract

Introduction: Several selective progesterone receptor modulators (SPRMs) show promise in several areas of medicine and this work has been summarized by us in 2008.

Areas covered: Since the publication of our reviews, several developments have taken place in the field of reproductive medicine. The first is emergency contraception (EC). Two SPRMs are clinically utilized today: mifepristone (MFP) and ulipristal acetate (UPA). MFP is available for EC in up to 120 h following unprotected intercourse. A dose of 10 mg is significantly more effective than levonorgestrel (LNG). In a metanalysis of the use of UPA versus LNG up to 72 h after unprotected intercourse, failure rates of 1.4 versus 2.2% were reported. The second is contraception. A daily dose of 2 mg MFP can block ovulation and several MFP regimens are being tested, including a vaginal ring releasing MFP. The third is the preoperative administration in women harboring leiomyomas, where clinical testing of several SPRM has shown that they can decrease uterine leiomyomas' size and substantially reduce uterine bleeding. SPRM can induce unusual, specific endometrial appearances. Many believe that these changes should not cause concern, but the issue remains controversial.

Expert opinion: SPRMs are very effective in EC and for the preoperative treatment of uterine leiomyomas.

Keywords: adenomyosis; asoprisnil; contraception; emergency contraception; endometriosis; mifepristone; proellex; selective progesterone receptor modulators; ulipristal acetate; uterine leiomyomas.

Publication types

  • Review

MeSH terms

  • Adenomyosis / drug therapy
  • Animals
  • Clinical Trials as Topic
  • Contraception, Postcoital / methods
  • Contraceptive Agents, Female / therapeutic use*
  • Contraceptives, Postcoital / therapeutic use
  • Endometriosis / drug therapy
  • Estrenes / therapeutic use
  • Female
  • Hormone Antagonists / therapeutic use
  • Humans
  • Leiomyoma / drug therapy
  • Levonorgestrel / therapeutic use
  • Mifepristone / therapeutic use
  • Norpregnadienes / therapeutic use
  • Oximes / therapeutic use
  • Receptors, Progesterone / metabolism*
  • Uterine Neoplasms / drug therapy

Substances

  • Contraceptive Agents, Female
  • Contraceptives, Postcoital
  • Estrenes
  • Hormone Antagonists
  • Norpregnadienes
  • Oximes
  • Receptors, Progesterone
  • Mifepristone
  • Levonorgestrel
  • asoprisnil
  • ulipristal acetate