Degarelix: a novel gonadotropin-releasing hormone blocker for the treatment of prostate cancer.

Androgen deprivation therapy with gonadotropin releasing-hormone (GnRH) receptor agonists provides the mainstay of endocrine treatment for advanced prostate cancer. Although effective, GnRH agonists induce an initial testosterone surge, which can cause painful and potentially dangerous clinical flare. Degarelix is a novel GnRH receptor blocker that provides immediate, profound and sustained testosterone reduction, without an initial surge. In a Phase III trial, degarelix and leuprolide showed similar long-term efficacy in maintaining testosterone levels of 0.5 ng/ml or less over 1 year, and induced significantly faster testosterone and prostate-specific antigen suppression. Degarelix was well tolerated; the most common side effects were mild/moderate injection-site reactions and hot flashes. Findings to date suggest that degarelix may make an important contribution to the treatment of prostate cancer.