Recent developments in antiandrogens and selective androgen receptor modulators

Bernard Haendler1, Arwed Cleve

  • 1TRG Oncology, Global Drug Discovery, Bayer HealthCare, D-13342 Berlin, Germany. bernard.haendler@bayer.com

Insights

Androgens like testosterone are vital for male traits and influence diseases such as prostate cancer. Understanding androgen receptor (AR) signaling is key to developing better treatments for various conditions.

Area of Science:

  • Endocrinology
  • Molecular Biology
  • Oncology

Background:

  • Androgens, including testosterone and dihydrotestosterone, are crucial for male sexual development and characteristics.
  • The androgen receptor (AR) is a transcription factor that mediates androgen action and is implicated in prostate and breast cancers.

Purpose of the Study:

  • To explore the role of androgen receptor (AR) signaling in various physiological and pathological conditions.
  • To highlight the therapeutic potential of targeting AR in diseases beyond cancer, such as hypogonadism, frailty, cachexia, and polycystic ovary syndrome.

Main Methods:

  • Review of existing literature on AR function and AR-targeting drugs.
  • Analysis of the mechanisms underlying normal and aberrant AR signaling pathways.

Main Results:

  • AR plays a critical role in both normal development and diseases like prostate cancer.
  • AR targeting shows promise for treating conditions including hypogonadism, frailty, cachexia, and PCOS.

Conclusions:

  • Despite numerous AR ligands developed over 40 years, improved compounds are needed for better efficacy and fewer side effects.
  • Further understanding of AR signaling mechanisms is essential for developing next-generation AR-targeting therapeutics.

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