Role of 5α-Reductase Inhibitors in Prostate Cancer Prevention and Treatment

Although testosterone is the most abundant serum androgen, dihydrotestosterone is the main prostatic androgen. Testosterone is converted to dihydrotestosterone by the enzyme 5 alpha-reductase (5 alpha-R). Dihydrotestosterone plays an important role in several human diseases, including benign prostate enlargement and prostate cancer. The observation that males born with 5 alpha-R 2 deficiency have never been reported to develop prostate cancer stimulated interest in development of 5 alpha-R inhibitors. Thus far, 2 5 alpha-R inhibitors are approved for clinical use. Several trials evaluated the use of 5 alpha-R inhibitors in prostate cancer prevention and treatment and will be reviewed in this article. UROLOGY 79: 1197-1205, 2012. (c) 2012 Elsevier Inc.