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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。
The first-line treatment for advanced prostate cancer is endocrine therapy, which removes androgen therapy. Currently the most commonly used drug to remove androgen therapy is the gonadotropin-releasing hormone (GnRH) agonist, but its initial use may lead to testosterone surge, there is also the risk of testosterone fluctuations in the maintenance of medication, the need for combined anti-androgen drugs to alleviate The deterioration of the condition. Studies have shown that GnRH antagonists can also be used in the treatment of prostate cancer, and its direct inhibition of receptor activity, there is no risk of inducing testosterone surge. This review summarizes the mechanisms of action of GnRH agonists and GnRH antagonists, the history of GnRH antagonists and their clinical utility in the treatment of prostate cancer, and evaluates the safety and efficacy of GnRH antagonists, revealing the clinical utility of GnRH antagonists Value and development prospects.