Testosterone Surge: Rationale for Gonadotropin-Releasing Hormone Blockers?

Gonadotropin-releasing hormone (GnRH) agonists currently form the mainstay of management of advanced prostate cancer. They effectively suppress serum testosterone levels, which in turn inhibits tumor growth. However, the initial response to GnRH agonists is a transient increase in the serum testosterone levels. Known as a testosterone surge, this can lead to a worsening of symptoms and can adversely affect survival. Therefore, much interest exists in the development of a new class of drugs—GnRH antagonists—which produce immediate suppression of luteinizing hormone and testosterone without a testosterone surge. The most promising GnRH antagonist to date is degarelix.