Androgen receptor antagonists for prostate cancer therapy

    1. Frank Claessens1
    1. 1Laboratory of Molecular Endocrinology, Department of Cellular and Molecular Medicine, Katholieke Universiteit Leuven, Herestraat 49, B-3000 Leuven, Belgium
      2Urology, Department of Development and Regeneration, University Hospitals Leuven, Herestraat 49, 3000 Leuven, Belgium
      3Laboratory for Structural Bioinformatics, Center for Life Science Technologies, RIKEN, Yokohama, Japan
    1. Correspondence should be addressed to F Claessens; Email: frank.claessens{at}


    Androgen deprivation is the mainstay therapy for metastatic prostate cancer (PCa). Another way of suppressing androgen receptor (AR) signaling is via AR antagonists or antiandrogens. Despite being frequently prescribed in clinical practice, there is conflicting evidence concerning the role of AR antagonists in the management of PCa. In the castration-resistant settings of PCa, docetaxel has been the only treatment option for decades. With recent evidence that castration-resistant PCa is far from AR-independent, there has been an increasing interest in developing new AR antagonists. This review gives a concise overview of the clinically available antiandrogens and the experimental AR antagonists that tackle androgen action with a different approach.

    • Revision received 21 February 2014
    • Accepted 13 March 2014
    • Made available online as an Accepted Preprint 17 March 2014
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