Department of Medicine & Surgery, Duke Cancer Institute, Duke University, Durham, NC 27710, USA.
The Institute of Cancer Research & Royal Marsden NHS Foundation Trust, London, UK.
Future Oncol. 2021 Nov;17(33):4431-4446. doi: 10.2217/fon-2021-0575. Epub 2021 Aug 19.
Androgen deprivation therapy using gonadotropin-releasing hormone (GnRH) analogues is standard treatment for intermediate and advanced prostate cancer. GnRH agonist therapy results in an initial testosterone flare, and increased metabolic and cardiovascular risks. The GnRH antagonist relugolix is able to reduce serum testosterone levels in men with prostate cancer without inducing testosterone flare. In the HERO Phase III trial, relugolix was superior to leuprolide acetate at rapidly reducing testosterone and continuously suppressing testosterone, with faster post-treatment recovery of testosterone levels. Relugolix was associated with a 54% lower incidence of major adverse cardiovascular events than leuprolide acetate. As the first oral GnRH antagonist approved for the treatment of advanced prostate cancer, relugolix offers a new treatment option.
促性腺激素释放激素（GnRH）类似物的雄激素剥夺疗法是治疗中晚期前列腺癌的标准方法。 GnRH 激动剂治疗会导致初始睾酮激增，并增加代谢和心血管风险。 GnRH 拮抗剂瑞戈非尼能够降低前列腺癌男性的血清睾酮水平，而不会引起睾酮激增。在 HERO III 期试验中，瑞戈非尼在快速降低睾酮和持续抑制睾酮方面优于醋酸亮丙瑞林，并且在治疗后更快地恢复睾酮水平。与醋酸亮丙瑞林相比，瑞戈非尼与主要不良心血管事件的发生率降低 54%相关。作为首个批准用于治疗晚期前列腺癌的口服 GnRH 拮抗剂，瑞戈非尼提供了一种新的治疗选择。
