Abstract: Gonadotropin-releasing hormone (GnRH) receptor agonists are still the most commonly used androgen deprivation treatment (ADT) drugs for prostate cancer in clinical practice. Currently, the GnRH receptor antagonists used for endocrine therapy for prostate cancer primarily include degarelix and relugolix (TAK-385). The former is administered by subcutaneous injection, while the latter is an oral drug. Compared to GnRH agonists, GnRH antagonists reduce serum testosterone levels more rapidly without an initial testosterone surge or subsequent microsurges. This review focuses on the mechanism of action of GnRH antagonists and agonists, the developmental history of GnRH antagonists, and emerging data from clinical studies of the two antagonists used as endocrine therapy for prostate cancer.

Keywords: gonadotropin-releasing hormone, prostate cancer, degarelix, relugolix


中文翻译：

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促性腺激素释放激素受体拮抗剂治疗前列腺癌的临床研究进展

摘要：促性腺激素释放激素（GnRH）受体激动剂仍是临床上最常用的前列腺癌雄激素剥夺治疗（ADT）药物。目前，用于前列腺癌内分泌治疗的GnRH受体拮抗剂主要包括地加瑞克和瑞卢戈利克（TAK-385）。前者为皮下注射给药，后者为口服给药。与 GnRH 激动剂相比，GnRH 拮抗剂可更迅速地降低血清睾酮水平，而不会出现最初的睾酮激增或随后的显微激增。本综述重点关注 GnRH 拮抗剂和激动剂的作用机制、GnRH 拮抗剂的发展历史，以及两种拮抗剂用于前列腺癌内分泌治疗的临床研究的新数据。

关键词： 促性腺激素释放激素, 前列腺癌, 地加瑞克, relugolix