Special Issue on New Drugs in the Management of Advanced Prostate Cancer: Original ArticlesNovel Concepts in Androgen Receptor BlockadeHsieh, Andrew C. MD*; Ryan, Charles J. MD*Author Information From the *The Urologic Oncology Program, UCSF Comprehensive Cancer Center, University of California-San Francisco, San Francisco, CA. Reprints: Charles J. Ryan, MD, Urologic Oncology Program, UCSF Comprehensive Cancer Center, 1600 Divisadero 3rd Floor, San Francisco, CA 94143. E-mail: email@example.com. The Cancer Journal: January 2008 - Volume 14 - Issue 1 - p 11-14 doi: 10.1097/PPO.0b013e318161d13e Buy Metrics Abstract Androgen receptor blockade is a cornerstone of treatment for prostate cancer. Despite castrate levels of testosterone, activation of the androgen receptor remains an important mediator of disease progression in the androgen “independent” state. Thus, maximal blockade of androgen receptor signaling is a continual goal in the management of castration-resistant prostate cancer. In this review we will discuss how various aspects of androgen receptor signaling are being targeted for therapeutic development in castration-resistant prostate cancer. These include direct androgen receptor inhibitors, inhibitors of adrenal androgen synthesis, and a dual 5α-reductase isoenzyme inhibitor. © 2008 Lippincott Williams & Wilkins, Inc.