Relugolix for the treatment of uterine fibroids
Relugolix for the treatment of uterine fibroids
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DOI：
10.1358/dot.2019.55.8.3020179
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发表时间：
2019-08-01
期刊：
影响因子：
1.8
通讯作者：
Ferrero, S.
中科院分区：
文献类型：
--
作者：
Barra, F.;Seca, M.;Ferrero, S.
子宫平滑肌瘤是最常见的妇科良性肿瘤，影响20-40%的女性。有几种治疗方案可用于治疗这些患者。过去几年，治疗子宫肌瘤的药物治疗在很大程度上增加了，特别是对于拒绝、推迟或不适合手术的女性。近年来，促性腺激素释放激素（GnRH）拮抗剂（GnRH-ants）的临床研究不断涌现。这类药物对脑下垂体的GnRH受体发挥纯粹的竞争性拮抗活性，立即停止促性腺激素和性类固醇的释放。Relugolix是一种口服活性非肽类GnRH-ant，最近在日本获得上市许可，用于治疗子宫肌瘤相关症状。目前，美国和欧洲正在进行几项III期临床试验，以评估这种分子在这种环境中的作用。
Uterine leiomyomas represent the most common form of benign gynecological tumors affecting 20-40% of women during their life. Several therapeutic options are available for treating these patients. The use of medical treatment for myomas has largely grown in the last years, in particular for women who would refuse, postpone or are not candidates for surgery. In the last years, the clinical investigation of gonadotropin-releasing hormone (GnRH) antagonists (GnRH-ants) has emerged. This class of drugs exerts pure competitive antagonistic activity on the GnRH receptor at the pituitary gland, producing an immediate stop in the release of gonadotropins and sex steroids. Relugolix is an orally active nonpeptide GnRH-ant, recently licensed for marketing in Japan for the treatment of symptoms related to uterine myomas. Currently, several phase III clinical trials are ongoing to evaluate this molecule in this setting in the U.S. and Europe.