Barra F, Scala C, Ferrero S
Academic Unit of Obstetrics and Gynaecology, IRCCS Ospedale Policlinico San Martino, Genoa, Italy; Department of Neurosciences, Rehabilitation, Ophthalmology, Genetics, Maternal and Child Health (DiNOGMI), University of Genoa, Genoa, Italy.
Drugs Today (Barc). 2019 Apr;55(4):237-246. doi: 10.1358/dot.2019.55.4.2930713.
First-line medical therapies for treating pain associated with endometriosis mainly consist in combined oral contraceptives and progestins. However, some women, having persistence of symptoms, may require further therapeutic options. Among these, gonadotropin-releasing hormone (GnRH) agonists (GnRH-as) have been widely employed in the last 30 years, despite being characterized by an unfavorable safety profile. Currently, new alternative investigational options are being investigated to treat this benign chronic disease. GnRH antagonists (GnRH-ants) are innovative hormonal drugs that do not induce flare-up effects and present also a limited onset of hypoestrogenic symptoms; in fact, their pharmacological mechanism of action, which consists in pure antagonistic activity, differs from that of traditional GnRH-as. In July 2018, the U.S. Food and Drug Administration (FDA) approved elagolix sodium for the management of moderate to severe pain associated with endometriosis, after the drug showed promising efficacy and safety results in previous phase III trials. This monograph aims to provide a complete overview of the pharmacokinetics, clinical efficacy and safety of this GnRH-ant for treat¬ing patients with endometriosis.
治疗子宫内膜异位症相关疼痛的一线药物治疗主要包括复方口服避孕药和孕激素。然而，一些症状持续存在的女性可能需要更多的治疗选择。其中，促性腺激素释放激素（GnRH）激动剂（GnRH-as）在过去30年中被广泛应用，尽管其安全性并不理想。目前，正在研究新的替代研究性治疗方案来治疗这种良性慢性疾病。GnRH拮抗剂（GnRH-ants）是一种新型激素类药物，不会引发“flare-up”效应，且低雌激素症状的发作也有限；事实上，其纯拮抗活性的药理作用机制与传统的GnRH-as不同。2018年7月，美国食品药品监督管理局（FDA）批准了艾拉戈利钠用于治疗与子宫内膜异位症相关的中度至重度疼痛，此前该药物在III期试验中显示出了有前景的疗效和安全性结果。本专题文章旨在全面概述这种GnRH拮抗剂在治疗子宫内膜异位症患者时的药代动力学、临床疗效和安全性。
