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Selektive Progesteronrezeptormodulatoren

Wirkmechanismen und klinische Einsatzmöglichkeiten

Selective progesterone receptor modulators

Mechanisms of action and possible clinical applications

  • Arzneimitteltherapie
  • Published:
Gynäkologische Endokrinologie Aims and scope

Zusammenfassung

Hintergrund

Selektive Progesteronrezeptormodulatoren (SPRM) sind eine Substanzgruppe mit vielfältigen potenziellen Anwendungsmöglichkeiten auf dem Gebiet der gynäkologischen Endokrinologie.

Material und Methoden

Anhand der vorliegenden Literatur wird der Wissensstand zu den Wirkmechanismen der SPRM zusammengefasst. Zudem werden die möglichen Indikationen diskutiert.

Ergebnisse

Die Effekte von Progesteron werden durch den Progesteronrezeptor (PR) vermittelt. SPRM wirken agonistisch und/oder antagonistisch an den Isoformen des PR. Die Isoformen funktionieren primär als ligandenaktivierte Transkriptionsfaktoren. Mögliche Indikationen der SPRM-Gabe sind die Kontrazeption, Notfallkontrazeption, Endometriosetherapie und Behandlung von Uterusmyomen. Klinisch zugelassen sind derzeit Ulipristalacetat (UPA) und Mifepriston (MFP). MFP und UPA können als effektives Notfallkontrazeptivum verschrieben werden, wobei der genaue Wirkmechanismus noch nicht abschließend geklärt ist. UPA ist zudem eine Therapieoption für prämenopausale Frauen mit symptomatischen Uterusmyomen. Relativ wenige Fortschritte gibt es in der Entwicklung von SPRM zur Kontrazeption. Bisher liegen nur wenige Daten für die Indikation im Sinne der Langzeitkontrazeption vor.

Schlussfolgerungen

Haupteinsatzgebiete der SPRM sind die Notfallkontrazeption und die präoperative Behandlung von Uterusmyomen. Forschungsbemühungen bezüglich des Einsatzes von SPRM sind derzeit auf die Langzeitkontrazeption gerichtet. Hier ist insbesondere der UPA-freisetzende Vaginalring ein möglicher Ansatz.

Abstract

Background

Selective progesterone receptor modulators (SPRM) are a group of substances with a multitude of potential applications in the field of gynecological endocrinology.

Material and methods

The state of knowledge on the mechanisms of action of SPRMs is summarized based on the currently available literature. In addition, the possible indications are discussed.

Results

The effects of progesterone are mediated by progesterone receptors (PR) and SPRMs have agonistic as well as antagonistic effects on the isoforms of PR. The isoforms primarily function as ligand-activated transcription factors. Possible indications are contraception, postcoital contraception, endometriosis therapy and treatment of uterine leiomyomas. Currently approved for clinical use are ulipristal acetate (UPA) and mifepristone (MFP), which can be prescribed as an effective postcoital contraceptive but the exact mechanism of action is not yet fully clarified. Additionally, UPA is a therapy option for premenopausal women with symptomatic uterine leiomyomas. There has been relatively little progress in the development of SPRMs for contraception. So far the amount of data currently available on the indications in the sense of long-term contraception are scarce.

Conclusion

The main fields of application of SPRMs are postcoital contraception and preoperative treatment of uterine leiomyomas. Future research efforts concerning the use of SPRMs are currently centered on the field of long-term contraception. Of particular interest is the vaginal ring delivery of UPA.

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Authors and Affiliations

  1. Klinik und Lehrstuhl für Frauenheilkunde und Geburtshilfe, Universität Regensburg
, Caritas-Krankenhaus St. Josef, Landshuter Str. 65, 93053, Regensburg, Deutschland

    Christina Selgrad &  Olaf Ortmann

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  1. Christina Selgrad
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  2. Olaf Ortmann
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Correspondence to Olaf Ortmann.

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Interessenkonflikt

C. Selgrad und O. Ortmann geben an, dass kein Interessenkonflikt besteht.

Dieser Beitrag beinhaltet keine Studien an Menschen oder Tieren.

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M. Birkhäuser, Basel

A.O. Mueck, Tübingen

O. Ortmann, Regensburg

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Selgrad, C., Ortmann, O. Selektive Progesteronrezeptormodulatoren. Gynäkologische Endokrinologie 14, 44–48 (2016). https://doi.org/10.1007/s10304-015-0050-2

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  • DOI: https://doi.org/10.1007/s10304-015-0050-2

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