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Target Oncol. 2023 Mar;18(2):295-302. doi: 10.1007/s11523-022-00944-4. Epub 2023 Jan 18.
Relugolix (Orgovyx), an orally active nonpeptide gonadotropin-releasing hormone (GnRH) receptor antagonist that provides rapid testosterone suppression, is indicated in the USA for the treatment of advanced prostate cancer and in the EU for advanced hormone-sensitive prostate cancer. In the pivotal phase III HERO trial in men with advanced prostate cancer, once-daily oral relugolix (with a loading dose on day 1) led to a sustained castration rate over 48 weeks of treatment of > 90%, a rate that was non-inferior to that provided by intramuscular leuprolide depot every 3 months (with an exploratory analysis further indicating the superiority of relugolix over leuprolide). Relugolix was generally well tolerated, having an adverse event profile that is consistent with testosterone suppression. Furthermore, there is evidence that relugolix may be associated with a lower risk of major adverse cardiac events compared with leuprolide. With the ability to provide the rapid testosterone suppression (with no initial surge in testosterone upon treatment initiation) combined with the benefits of oral administration and potentially improved cardiac safety, relugolix presents a valuable treatment option for men with advanced prostate cancer where androgen deprivation therapy is indicated.
瑞戈非尼（Orgovyx），一种口服活性非肽促性腺激素释放激素（GnRH）受体拮抗剂，可迅速抑制睾酮，在美国被批准用于治疗晚期前列腺癌，在欧盟被批准用于治疗晚期激素敏感型前列腺癌。在晚期前列腺癌的关键 III 期 HERO 试验中，每日一次口服瑞戈非尼（第 1 天给予负荷剂量）可在 48 周的治疗中持续维持 >90%的去势率，该去势率与每 3 个月肌内注射亮丙瑞林（进行探索性分析表明瑞戈非尼优于亮丙瑞林）的去势率相当。瑞戈非尼总体耐受性良好，其不良事件谱与睾酮抑制一致。此外，有证据表明与亮丙瑞林相比，瑞戈非尼可能与较低的主要不良心脏事件风险相关。瑞戈非尼具有快速抑制睾酮的能力（治疗开始时没有睾酮初始激增），加上口服给药的益处和潜在改善的心脏安全性，为需要雄激素剥夺治疗的晚期前列腺癌患者提供了一种有价值的治疗选择。
