GnRH拮抗剂在前列腺癌内分泌治疗中的临床应用和发展前景

晚期前列腺癌的一线治疗方案是内分泌治疗，即去除雄激素治疗。目前去除雄激素治疗最常用的药物是促性腺激素释放激素（GnRH）激动剂，但其初次使用时可能导致睾酮激增，维持用药时也存在睾酮波动的风险，需要联合应用抗雄激素药物来缓解病情的恶化。研究表明，GnRH拮抗剂也可应用于前列腺癌治疗，且其直接抑制受体活性，不存在诱发睾酮激增的风险。本文综述了GnRH激动剂和GnRH拮抗剂的作用机制、GnRH拮抗剂的发展历史及其在前列腺癌治疗中的临床应用，评价了GnRH拮抗剂的安全性和有效性，揭示了GnRH拮抗剂的临床价值和发展前景。
Hormone therapy (androgen deprivation therapy, ADT) is the first line treatment for advanced prostate cancer. Gonadotropin-releasing hormone (GnRH) agonist is commonly used for ADT, with the risk of flare-up effect at the first dose and testosterone fluctuation, which needs combination of anti-androgen drugs to alleviate the deterioration of the clinical condition. GnRH antagonists directly bind to GnRH receptor, blocking its activity, and they can be used in prostate cancer treatment, without testosterone flare-up effect. This review focused on functional mechanisms of GnRH agonists and antagonists, and history and clinical application of GnRH antagonists, so as to evaluate the clinical safety and effectiveness of GnRH antagonists and to discuss their clinical value and future prospects