Department of Pathology & Laboratory Medicine, University of Rochester Medical Center, Rochester, NY, USA.
Department of Urology, Yokohama City University Graduate School of Medicine, Yokohama, Japan.
Drug Des Devel Ther. 2023 Aug 4;17:2325-2333. doi: 10.2147/DDDT.S373546. eCollection 2023.
Androgen deprivation therapy, primarily via a gonadotropin-releasing hormone receptor agonist or antagonist together with or without an androgen receptor antagonist, remains the mainstay of medical treatment for advanced prostate cancer. Meanwhile, relugolix has been developed as the first orally active, non-peptide, selective antagonist for the gonadotropin-releasing hormone receptor. Previous randomized studies involving patients with prostate cancer have demonstrated comparable efficacy in androgen suppression between relugolix vs other gonadotropin-releasing hormone antagonists or agonists. This review summarizes available data on the design and development of relugolix and its therapeutic application, and discusses if relugolix represents a promising oral alternative to injectable androgen deprivation therapy. Based on current published evidence, further investigation is likely required to determine the actual clinical benefits of relugolix therapy against prostate cancer.
雄激素剥夺疗法（ADT）主要通过促性腺激素释放激素（GnRH）受体激动剂或拮抗剂联合或不联合雄激素受体拮抗剂来实现，仍然是治疗晚期前列腺癌的主要方法。同时，瑞戈非尼（relugolix）已被开发为首个具有口服活性的、非肽类的、促性腺激素释放激素受体的选择性拮抗剂。先前涉及前列腺癌患者的随机研究表明，瑞戈非尼与其他 GnRH 拮抗剂或激动剂在雄激素抑制方面具有相当的疗效。本综述总结了瑞戈非尼的设计、开发及其治疗应用的现有数据，并讨论了瑞戈非尼是否代表了一种有前途的口服雄激素剥夺疗法替代方案。基于目前已发表的证据，可能需要进一步研究来确定瑞戈非尼治疗前列腺癌的实际临床获益。
