Skip to main content
SpringerLink
Log in

Proven and Potential Clinical Applications of Mifpristone (RU486)

  • Published:
Reviews in Endocrine and Metabolic Disorders Aims and scope Submit manuscript

This is a preview of subscription content, log in via an institution to check access.

Access this article

Log in via an institution

Price excludes VAT (USA)
Tax calculation will be finalised during checkout.

Instant access to the full article PDF.

Institutional subscriptions

References

  1. Philibert D, Deraedt R, Teutsch G. RU38486: A potent antiglucortoid in vivo. In: 8th International Congress of Pharmacology. Tokyo, Japan, 1981.

  2. Philibert D. RU38486: An original multifaceted antihormone in vivo. In: Agarwal M. eds. Adrenal Steroid Antagonism. Berlin: Walter de Gruyter 1984; 77-101.

    Google Scholar 

  3. Baulieu E. Contragestion and other clinical applications of RU486, an antiprogesterone at the receptor. Science 1989;245:1351-1357.

    Google Scholar 

  4. Spitz IM, Bardin CW. Mifepristone (RU486)-a modulator of progestin and glucocortocoid action. N Engl J Med 1993;329(6):404-412.

    Google Scholar 

  5. Spitz IM, Croxatto HB, Robbins A. Antiprogestins: Mechanism of action and contraceptive potential. Annu Rev Pharmacol Toxicol 1996;36:47-81.

    Google Scholar 

  6. Spitz IM. Preface: Progestins, progesterone receptor modulators and progesterone antagonist. Steroids 2000;65(10/11):543-544.

    Google Scholar 

  7. Elger W, Bartley J, Schneider B, Kaufmann G, Schubert G, Chwalisz K. Endocrine pharmacological characterization of progesterone antagonistic and progesterone receptor modulators with respect to PR-agonistic and antagonistic activity. Steroids 2000;65(10/11):713-723.

    Google Scholar 

  8. Chwalisz K, Brenner RM, Fuhrmann U, Hess-Stumpp H, Elger W. Antiproliferative effects of progesterone antagonists and progesterone receptor modulators on the endometrium. Steroids 2000;65(10/11):741-751.

    Google Scholar 

  9. Spitz IM, Chwalisz K. Progesterone receptor modulators in women's health. Steroids 2000;65(10/11):807-816.

    Google Scholar 

  10. Garfield RE, Blennershassett MG, Miller SM. Control of myometrial contractility: Role and regulation of gap junctions. Oxf Rev Reprod Biol 1988;10:436-490.

    Google Scholar 

  11. Bygdeman M, Swahn ML. Progesterone receptor blockage. Effecy on uterine contractility and early pregnancy. Contraception 1985;32(1):45-51.

    Google Scholar 

  12. Cheng L, Kelly RW, Thong KJ, Hume R, Baird DT. The effect of mifepristone (RU486) on the immunohistochemical distribution of prostaglandin E and its metabolite in decidual and chorionic tissue in early pregnancy. J Clin Endocrinol Metab 1993;77(3):873-877.

    Google Scholar 

  13. Cheng L, Kelly RW, Thong KJ, Hume R, Baird DT. The effects of mifepristone (RU486) on prostaglandin dehydrogenase in decidual and chorionic tissue in early pregnancy. Hum Reprod 1993;8(5):705-709.

    Google Scholar 

  14. Gravanis A, Schaison G, George M, de Brux J, Satyaswaroop PG, Baulieu EE, Robel P. Endometrial and pituitary responses to the steroidal antiprogestin RU486 in postmenopausal women. J Clin Endocrinol Metab 1985;60(1):156-163.

    Google Scholar 

  15. Hodgen GD, van Uem JF, Chillik CF, Danforth DR, Wolf JP, Neulen J, Williams RF, Chwalisz K. Non-competitive anti-oestrogenic activity of progesterone antagonists in primate models. Hum Reprod 1994;9(Suppl. 1):77-81.

    Google Scholar 

  16. Slayden OD, Zelinski Wooten MB, Chwalisz K, Stouffer RL, Brenner RM. Chronic treatment of cycling rhesus monkeys with low doses of the antiprogestin ZK 137316: morphometric assessment of the uterus and oviduct. Hum Reprod 1998;13(2):269-277.

    Google Scholar 

  17. Chwalisz K, Stockemann K, Fritzemeier KH, Fuhrmann U. Modulation of oestrogenic effects by progesterone antagonists on the rat uterus. Hum Reprod Update 1998;4(5):570-583.

    Google Scholar 

  18. Newfield RS, Spitz IM, Isacson C, New MI. Long-term mifepristone (RU486) therapy resulting in massive benign endometrial hyperplasia. Clin Endocrinol (Oxf) 2001;54(3):399-404.

    Google Scholar 

  19. Grunberg SM, Rankin C, Townsen J, Ahamadi L. Phase III double blind randomized placebo-controlled study of mifepristone (RU) for the treatment of unresectable meningioma. Proceeding of ASCO, Thirty-Seventh Annual Meeting 2001;20:56a.

    Google Scholar 

  20. Herrmann W, Wyss R, Riondel A, Philibert D, Teutsch G, Sakiz E, Baulieu EE. Effet d'un steroide antiprogesterone chezla femme: interruption du cycle menstrual et de la grossesse au debut. CR Acad Sc Paris 1982;294:933-938.

    Google Scholar 

  21. Bygdeman M, Danielsson KG, Marions L, Swahn ML. Contraceptive use of antiprogestin. Eur J Contracept Reprod Health Care 1999;4(2):103-107.

    Google Scholar 

  22. Batista MC, Cartledge TP, Zellmer AW, Nieman LK, Loriaux DL, Merriam GR. The antiprogestin RU486 delays the midcycle gonadotropin surge and ovulation in gonadotropin-releasing hormone-induced cycles. Fertil Steril 1994;62(1):28-34.

    Google Scholar 

  23. Shoupe D, Mishell DR, Jr., Lahteenmaki P, Heikinheimo O, Birgerson L, Madkour H, Spitz IM. Effects of the antiprogesterone RU486 in normal women. I. Single-dose administration in the midluteal phase. Am J Obstet Gynecol 1987;157(6):1415-20.

    Google Scholar 

  24. Christin-Maitre S, Bouchard P, Spitz IM. Medical termination of pregnancy. New Engl J Med 2000;342(13):946-956.

    Google Scholar 

  25. Spitz IM, Bardin CW. Clinical pharmacology of RU486-an antiprogestin and antiglucocorticoid. Contraception 1993;48(5):403-444.

    Google Scholar 

  26. Couzinet B, Le Strat N, Ulmann A, Baulieu EE, Schaison G. Termination of early pregnancy by the progesterone antagonist RU486 (Mifepristone). N Engl J Med 1986;315(25):1565-1570.

    Google Scholar 

  27. Wold Health Organization Task Force on Post-ovulatory Methods of Fertility Regulation. Termination of pregnancy with reduced doses of mifepristone. BMJ 1993;307(6903):532-537.

    Google Scholar 

  28. Robbins A, Spitz IM. Mifepristone: clinical pharmacology. Clin Obstet Gynecol 1996;39(2):436-450.

    Google Scholar 

  29. Prasad RN, Choolani M. Termination of early human pregnancy with either 50 mg or 200 mg single oral dose of mifepristone (RU486) in combination with either 0.5 mg or 1.0 mg vaginal gemeprost. Aust N Z J Obstet Gynaecol 1996;36(1):20-23.

    Google Scholar 

  30. Spitz IM, Bardin CW, Benton L, Robbins A. Early pregnancy termination with mifepristone and misoprostol in the United States. N Engl J Med 1998;338(18):1241-1247.

    Google Scholar 

  31. Aubeny E, Peyron R, Larquier Turpin C, Renault M, Targosz V, Silvestre L, et al. Termination of early pregnancy (up to 63 days of amenorrhea) with mifepristone and increasing doses of misoprostol. Int J Fertil 1995;40 (Suppl. 2):85-91.

    Google Scholar 

  32. World Health Organization Task Force on Post-ovulatory Methods of Fertility Regulation. Comparison of two doses of mifepristone in combination with misoprostol for early medical abortion: a randomized trial. Brit J Obstet Gynecol 2000;107:524-530.

    Google Scholar 

  33. Ashok PW, Penney GC, Flett GM, Templeton A. An effective regimen for early medical abortion: a report of 2000 consecutive cases. Hum Reprod 1998;13(10):2962-2965.

    Google Scholar 

  34. el Rafaey H, Rajasekar D, Abdalla M, Calder L, Templeton A. Induction of abortion with mifepristone (RU486) and oral or vaginal misoprostol. N Engl J Med 1995;332(15):983-987.

    Google Scholar 

  35. Baird DT, Suckharoen N, Thong KJ. Randomized trial of misoprostol and cervagem in combination with a reduced dose of mifepristone for induction of abortion. Hum Reprod 1995;10(6):1521-1527.

    Google Scholar 

  36. Urquhart D, Templeton A, Shinwei F, Chapman M, Hawkins K, McGarry J, Rodger M, Baird D, Bjornsson S. The efficacy and tolerance of mifepristone and prostaglandin in termination of pregnancy of less than 63 days gestation; UK multicentre study?final results. Contraception 1997;55:1-5.

    Google Scholar 

  37. Schaff EA, Fielding SL, Westhoff C, Ellertson C, Eisinger SH, Stadalius LS, Fuller L. Vaginal misoprostal administered 1, 2, or 3 days after mifepristone for early medical abortion: A randomized trial. JAMA 2000;284(15):1948-1953.

    Google Scholar 

  38. Creinin MD, Schwartz JL, Pymar HC, Fink W. Efficacy of mifepristone followed on the same day by misoprostol for early termination of pregnancy: report of a randomized trial. BJOG 2001;108(5):469-473.

    Google Scholar 

  39. Rodger MW, Baird DT. Blood loss following induction of early abortion using mifepristone (RU486) and a prostaglandin analogue (gemeprost). Contraception 1989;40(4):439-447.

    Google Scholar 

  40. Cohn M, Stewart P. Pretreatment of the primigravid uterine cervix with mifepristone 30 h prior to termination of pregnancy: a double blind study. Br J Obstet Gynaecol 1991;98(8):778-782.

    Google Scholar 

  41. Urquhart DR, Templeton AA. Mifepristone (RU486) for cervical priming prior to surgically induced abortion in the late first trimester. Contraception 1990;42(2):191-199.

    Google Scholar 

  42. Urquhart DR, Templeton AA. The use of mifepristone prior to prostaglandin-induced mid-trimester abortion. Hum Reprod 1990;5(7):883-886.

    Google Scholar 

  43. Ashok PW, Templeton AA. Nonsurgical mid-trimester termination of pregnancy: a reviewof 500 consecutive cases. Br J Obstet Gynaecol 1999;106(7):706-710.

    Google Scholar 

  44. Cabrol D, Dubois C, Cronje H, Gonnet JM, Guillot M, Maria B, Moodley J, Oury JF, Thoulon JM, Treisser A. Induction of labor with mifepristone (RU486) in intrauterine fetal death. Am J Obstet Gynecol 1990;163(2):540-542.

    Google Scholar 

  45. Elliott CL, Brennand JE, Calder AA. The effects of mifepristone on cervical ripening and labor induction in primigravidae. Obstet Gynecol 1998;92(5):804-809.

    Google Scholar 

  46. Frydman R, Lelaidier C, Baton Mleux C, Fernandez H, Vial M, Bourget P. Labor induction in women at term with mifepristone (RU486): a double-blind, randomized, placebo-controlled study. Obstet Gynecol 1992;80(6):972-975.

    Google Scholar 

  47. Hill NC, Selinger M, Ferguson J, MacKenzie IZ. The placental transfer of mifepristone (RU486) during the second trimester and its influence upon maternal and fetal steroid concentrations. Br J Obstet Gynaecol 1990;97(5):406-411.

    Google Scholar 

  48. Kettel LM, Murphy AA, Morales AJ, Rivier J, Vale W, Yen SS. Rapid regression of uterine leiomyomas in response to daily administration of gonadotropin-releasing hormone antagonist [see comments]. Fertil Steril 1993;60(4):642-646.

    Google Scholar 

  49. Kettel LM, Murphy AA, Morales AJ, Ulmann A, Baulieu EE, Yen SS. Treatment of endometriosis with the antiprogesterone mifepristone (RU486). Fertil Steril 1996;65(1):23-28.

    Google Scholar 

  50. Kettel LM, Murphy AA, Morales AJ, Yen SS. Preliminary report on the treatment of endometriosis with low-dose mifepristone (RU486). Am J Obstet Gynecol 1998;178(6):1151-1156.

    Google Scholar 

  51. Yen SSC. Use of antiprogestins in the management of endometriosis and leiomyoma. In: Donaldson, MS, Dorflinger, L, Brown, SS, Benet, LZ eds. Clinical Applications of Mifepristone (RU496) and other Antiprogestins. Washington DC: National Academy Press, 1993;189-209.

    Google Scholar 

  52. Murphy AA, Castelano PZ. RU486: pharmacology and potential use in the treatment of endometriosis and leiomyomata uteri. Curr Opin Obstet Gynecol 1994;6(3):269-278.

    Google Scholar 

  53. Yang Y, Zheng S, Li K. Treatment of Uterine Leimyoma by two different doses of mifepristone. Chin J Obstet Gynecol 1996;31(10):624-626.

    Google Scholar 

  54. Spitz IM, Van Look PF, Coelingh Bennink HJ. The use of progesterone antagonists and progesterone receptor modulators in contraception. Steroids 2000;65(10/11):817-824.

    Google Scholar 

  55. Croxatto HB, Salvatierra AM, Croxatto HD, Fuentealba B. Effects of continuous treatment with low dose mifepristone throughout one menstrual cycle. Hum Reprod 1993;8(2):201-207.

    Google Scholar 

  56. Cameron ST, Critchley HO, Thong KJ, Buckley CH, Williams AR, Baird DR. Effects of daily low dose mifepristone on endometrial maturation and proliferation. Hum Reprod 1996;11(11):2518-2526.

    Google Scholar 

  57. Brown A, Mayo A, Smith KB, Cheng L, Lin S, Baird DT. Daily low dose mifepristone has contraceptive potential by suppressing ovulation and menstruation: a study over 4 months in Edinburgh and Shanghai. Int Jnl Obstets Gynec 2000;70(Suppl. 1):22.

    Google Scholar 

  58. Marions L, Danielsson KG, Swahn ML, Bygdeman M. Contraceptive efficacy of low doses of mifepristone. Fertil Steril 1998;70(5):813-816.

    Google Scholar 

  59. Marions L, Viski S, Gemzell-Danielsson K, Resch BA, Swahn ML, Bygdeman M, Kovacs L. Contraceptive efficacy of daily administration of 0.5 mg mifepristone. Hum Reprod 1994;14(11):2788-2790.

    Google Scholar 

  60. Gemzell Danielsson K, Swahn ML, Svalander P, Bygdeman M. Early luteal phase treatment with mifepristone (RU486) for fertily regulation. Hum Reprod 1993;8(6):870-873.

    Google Scholar 

  61. Swahn ML, Bygdeman M, Chen JK, Gemzell Danielsson K, Song S, Yang QY, Yang PJ, Qian ML, Chang WF. Once-a-month treatment with a combination of mifepristone and the prostaglandin analogue misoprostol. Hum Reprod 1999;14(2):485-488.

    Google Scholar 

  62. World Health Organization Task Force on Post-Ovulatory Methods of Fertility Regulation. Menstrual regulation by mifepristone plus prostaglandin: Results from a multicentre trial. Hum Reprod 1995;10(2):308-314.

    Google Scholar 

  63. World Health Organization Task Force on Postovulatory Methods of Fertility Regulation. Comparison of three single doses of mifepristone as emergency contraception: a randomized trial. Lancet 1999;353(9154):697-702.

    Google Scholar 

  64. Messinis IE, Krishnan M, Kazem R, Khadilkar S, Templeton AA. Effect of mifepristone on folliculogenesis in women treated with recombinant FSH. Clin Endocrinol Oxf 1997;46(3):309-314.

    Google Scholar 

  65. Hegele Hartung C, Mootz U, Beier HM. Luteal control of endometrial receptivity and its modification by progesterone antagonists. Endocrinology 1992;131(5):2446-2460.

    Google Scholar 

  66. Paulson RJ, Sauer MV, Lobo RA. Potential enhancement of endometrial receptivity in cycles using controlled ovarian hyperstimulation with antiprogestins: a hypothesis. Fertil Steril 1997;67(2):321-325.

    Google Scholar 

  67. Nieman LK, Chrousos GP, Kellner C, Spitz IM, Nisula BC, Cutler GB, et al. Successful treatment of Cushing;s syndrome with the glucocorticoid antagonist RU486. J Clin Endocrinol Metab 1985;61(3):536-540.

    Google Scholar 

  68. Regelson W, Loria R, Kalimi M. Beyond 'abortion': RU-486 and the needs of the crisis constituency. JAMA 1990;264(8):1026-1027.

    Google Scholar 

  69. Klijn JG, Setyono Han B, Foekens JA. Progesterone antagonists and progesterone receptor modulators in the treatment of breast cancer. Steroids 2000;65(10-11):825-830.

    Google Scholar 

  70. Grunberg SM, Weiss MH, Spitz IM, Ahamadi J, Sadun A, Russell CA, et al. Treatment of unresectable meningiomas with the antiprogesterone agent mifepristone. J Neurosurg 1991;74:861-864.

    Google Scholar 

  71. Takiyama Y, Tanaka H, Takiyama Y, Makino I. The effects of hydrocortisone and RU486 (Mifepristone) on iodide uptake in porcine thyroid cells in primary culture. Endocrinology 1994:1972-1979.

  72. Gonzalez CH, Marques Dias MJ, Kim CA, Sugayama SM, Da Paz JA, Huson SM, Holmes LB. Congenital abnormalities in Brazilian children associated with misoprostol misuse in first trimester of pregnancy. Lancet 1998;351(9116):1624-1627.

    Google Scholar 

  73. Gonzalez CH, Vargas FR, Perez AB, Kim CA, Brunoni D, Marques Dias MJ, Leone CR, Correa Neto J, Llerena Junior JC, de Almeida JC. Limb deficiency with or without Mobius sequence in seven Brazilian children associated with misoprostol use in the first trimester of pregnancy. Am J Med Genet 193;47(1):59-64.

  74. Fonseca W, Alencar AJ, Mota FS, Coelho HL. Misoprostol and congenital malformations. Lancet 1991;338(8758):56.

    Google Scholar 

  75. Coelingh Bennink HJT. The Jerusalem Declaration. Steroids 2000;65:839-840.

    Google Scholar 

Download references

Author information

Authors and Affiliations

  1. Institute of Hormone Research, Shaare Zedek Medical Center, PO Box 3235, Jerusalem, 91031, Israel

    Irving M. Spitz

Authors
  1. Irving M. Spitz
    View author publications

    You can also search for this author in PubMed Google Scholar

Corresponding author

Correspondence to Irving M. Spitz.

Rights and permissions

Reprints and permissions

About this article

Cite this article

Spitz, I.M. Proven and Potential Clinical Applications of Mifpristone (RU486). Rev Endocr Metab Disord 3, 267–275 (2002). https://doi.org/10.1023/A:1020032711706

Download citation

  • Issue Date:

  • DOI: https://doi.org/10.1023/A:1020032711706

Search

Navigation