van Poppel Hendrik, Nilsson Sten
Department of Urology, University Hospital Gasthuisberg, Leuven, Belgium.
Urology. 2008 Jun;71(6):1001-6. doi: 10.1016/j.urology.2007.12.070. Epub 2008 Apr 14.
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.
促性腺激素释放激素（GnRH）激动剂目前是晚期前列腺癌治疗的主要手段。它们能有效抑制血清睾酮水平，进而抑制肿瘤生长。然而，对GnRH激动剂的初始反应是血清睾酮水平短暂升高。这种现象被称为睾酮激增，可能导致症状恶化并对生存产生不利影响。因此，人们对开发一类新型药物——GnRH拮抗剂——非常感兴趣，这类药物能立即抑制促黄体生成素和睾酮，且不会出现睾酮激增。迄今为止，最有前景的GnRH拮抗剂是地加瑞克。
