Therapeutic Strategies to Target the Androgen Receptor

J Med Chem. 2022 Jul 14;65(13):8772-8797. doi: 10.1021/acs.jmedchem.2c00716. Epub 2022 Jul 5.


The androgen receptor (AR) plays a key role in the maintenance of muscle and bone and the support of male sexual-related functions, as well as in the progression of prostate cancer. Accordingly, AR-targeted therapies have been developed for the treatment of related human diseases and conditions. AR agonists are an important class of drugs in the treatment of bone loss and muscle atrophy. AR antagonists have also been developed for the treatment of prostate cancer, including metastatic castration-resistant prostate cancer (mCRPC). Additionally, selective AR degraders (SARDs) have been reported. More recently, heterobifunctional degrader molecules of AR have been developed, and four such compounds are now in clinical development for the treatment of human prostate cancer. This review attempts to summarize the different types of compounds designed to target AR and the current frontiers of research on this important therapeutic target.

Publication types

  • Review
  • Research Support, Non-U.S. Gov't
  • Research Support, N.I.H., Extramural

MeSH terms

  • Androgen Antagonists
  • Androgen Receptor Antagonists / pharmacology
  • Androgen Receptor Antagonists / therapeutic use
  • Humans
  • Male
  • Prostatic Neoplasms, Castration-Resistant* / drug therapy
  • Receptors, Androgen*


  • Androgen Antagonists
  • Androgen Receptor Antagonists
  • Receptors, Androgen