Novel, potent anti-androgens of therapeutic potential: recent advances and promising developments

Future Med Chem. 2010 Apr;2(4):667-80. doi: 10.4155/fmc.10.14.


The beneficial effect of androgen ablation has been well established in prostate cancer therapy. Despite the initial response, patients typically relapse with a more aggressive form described as castration-resistant prostate cancer (CRCP), driven by continued androgen receptor (AR) signaling. This review details the current state of anti-androgen therapy, mainly for CRPC, with major emphasis on the most potent and promising compounds under development. Anti-androgen failure has been linked to elevated AR expression, increased expression of coactivator proteins, AR mutations, ligand-independent AR activation and persistent intraprostatic androgens. MDV3100, BMS-641988 and VN/124-1 were developed to overcome these mechanisms. In CRCP, prostate cancer cells still rely on intracellular androgens and, to a greater extent, on active AR for growth and survival. Therefore, potent anti-androgens that efficiently disrupt the functions (signaling) of AR are envisioned to be effective drugs for all types of prostate cancers.

Publication types

  • Review

MeSH terms

  • Androgen Antagonists / chemical synthesis
  • Androgen Antagonists / chemistry*
  • Androgen Antagonists / therapeutic use*
  • Humans
  • Male
  • Molecular Structure
  • Prostatic Neoplasms / drug therapy*
  • Receptors, Androgen / genetics
  • Receptors, Androgen / metabolism
  • Signal Transduction / physiology


  • AR protein, human
  • Androgen Antagonists
  • Receptors, Androgen