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Antiprogestin Ru 486: A Contragestive Agent

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Contraception Research for Today and the Nineties

Part of the book series: Progress in Vaccinology ((VACCINOLOGY,volume 1))

Abstract

The steroidal derivative RU 486 [17β-hydroxy-11β-(4-dimethylaminophenyl l)-17α-(prop-1-ynyl)-estra-4,9-dien-3-one] is the first potent antiprogestin to be useful medically. Acting reversibly at the molecular level of receptor binding, RU 486 interrupts progesterone action, while allowing endocrine functions to return quickly to normal afterwards. However, target-ceil dynamics that depend on a continuity of progesterone action is irreversibly disrupted. In cycled women, RU 486 acts during the luteal phase in the endometrium, provoking bleeding and, via a decrease in luteinizing hormone (LH), resulting in a secondary luteolysis. In pregnant women it affects mainly the decidualized mucosa, increases myometrial contractility and maturation of the cervix, leading to termination of pregnancy, Luteolysis, brought on by secondary alteration or detachment of the trophoblast, is secondary to the decrease in human chorionic gonadotropin (HCG). Clinical studies thus far indicate that RU 486 can be a very efficient and safe contragestive agent, especially for the medical termination of early pregnancy and as a postcoital menses inducer or menstrual regulator. The failures observed when RU 486 is given alone may be overcome when efficient form(s) of RU 486 are administered and/or when uterotonics are used in combination with the RU 486. A small amount of prostaglandin, which by itself is inefficient, when given at the end of RU 486 treatment yields highly satisfactory results in women with up to 8 weeks of ammenorhea. Treatment with the antiprogestin RU 486 does not expose women to a hormonal drug continuously, and no significant systemic side effects have been observed, including those that seemed possible because of the compound’s antiglucocorticosteroid activity. Based upon physiological and molecular understanding of RU 486 actions, this antiprogestin may be a second generation agent to achieve safe and effective control of human fertility.

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Authors
  1. Etienne-Emile Baulieu
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Editors and Affiliations

  1. National Institute of Immunology, JNU Complex, Shahid Jeet Singh Marg, 110 067, New Delhi, India

    G. P. Talwar

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© 1988 Springer-Verlag New York Inc.

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Baulieu, EE. (1988). Antiprogestin Ru 486: A Contragestive Agent. In: Talwar, G.P. (eds) Contraception Research for Today and the Nineties. Progress in Vaccinology, vol 1. Springer, New York, NY. https://doi.org/10.1007/978-1-4612-3746-4_6

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  • DOI: https://doi.org/10.1007/978-1-4612-3746-4_6

  • Publisher Name: Springer, New York, NY

  • Print ISBN: 978-1-4612-8331-7

  • Online ISBN: 978-1-4612-3746-4

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