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Non-steroidal steroid receptor modulators.

Pedro H H Hermkens1, Sarah Kamp, Scott Lusher

  • 1NV Organon, Molenstraat 110, PO Box 20, 5340 BH Oss, The Netherlands. pedro.hermkens@organon.com

Idrugs : the Investigational Drugs Journal
|July 6, 2006
PubMed
Summary
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Non-steroidal ligands for estrogen and androgen receptors show therapeutic promise. Developing similar compounds for other steroid receptors faces challenges in demonstrating benefits and achieving functional selectivity.

Area of Science:

  • Endocrinology and Pharmacology
  • Drug Discovery and Development

Background:

  • Non-steroidal ligands for estrogen receptors (ERs) and androgen receptors (ARs) have proven therapeutic potential.
  • Recent efforts have focused on developing non-steroidal ligands for other classic steroid receptors.

Purpose of the Study:

  • To review the progress and challenges in developing non-steroidal ligands for classic steroid receptors.
  • To highlight the ongoing difficulties in achieving functional selectivity for these novel compounds.

Main Methods:

  • Literature review of non-steroidal ligand development for steroid receptors.
  • Analysis of current clinical development status and challenges.

Main Results:

  • Non-steroidal ligands for ERs and ARs have been successfully developed and launched.

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  • Compounds for glucocorticoid, mineralocorticoid, and progesterone receptors are in early development, with benefits over steroidal counterparts yet to be proven.
  • No new non-steroidal ER or AR ligands have been launched in the past decade.

    • Conclusions:

    • The development of non-steroidal ligands for steroid receptors is an active area of research.
    • Demonstrating clear advantages over existing steroidal drugs and achieving functional selectivity remain significant hurdles.