Clinical Pharmacy, Faculty of Pharmacy, Ain Shams University, Cairo, Egypt.
Al-Galaa Military Hospital, Cairo, Egypt, Drug Research Center (DRC), Cairo, Egypt.
Expert Rev Clin Pharmacol. 2021 Apr;14(4):427-437. doi: 10.1080/17512433.2021.1900726. Epub 2021 Mar 15.
Uterine fibroids (UFs) are the most common benign tumor arising from myometrium of reproductive age women, with significant financial burden estimated in hundreds of billions of dollars. Unfortunately, there are limitations in available long-term treatment options. Thus, there is a large unmet need in the UF space for noninvasive therapeutics.
Authors reviewed the literature available for elagolix; an orally bioavailable, second-generation, non-peptide gonadotropin-releasing hormone (GnRH) antagonist recently approved by the US Food and Drug Administration (FDA) in combination with estradiol/norethindrone acetate for the management of heavy menstrual bleeding associated with UFs in premenopausal women.
The utility of new-generation oral GnRH-antagonists, such as elagolix, relugolix and linzagolix, is offering a new potential opportunity for the future therapy of UFs: elagolix has been the most studied drug of this class for treating benign gynecological diseases, including endometriosis and UFs, for which it has been US FDA-approved in 2018 and 2020, respectively.
子宫肌瘤(UFs)是育龄妇女的子宫平滑肌最常见的良性肿瘤,据估计其带来的经济负担高达数千亿美元。遗憾的是,目前可用的长期治疗方案存在局限性。因此,UF 领域对非侵入性治疗存在巨大的未满足需求。
作者对 Elagolix 的相关文献进行了回顾,Elagolix 是一种口服生物利用度高的第二代非肽类促性腺激素释放激素(GnRH)拮抗剂,最近获得美国食品和药物管理局(FDA)批准,与雌二醇/炔雌醇醋酸酯联合用于治疗与 UF 相关的绝经前妇女的重度月经过多。
新一代口服 GnRH 拮抗剂,如 Elagolix、Relugolix 和 Linzagolix,为 UF 的未来治疗提供了新的潜在机会:Elagolix 是该类药物中研究最多的治疗良性妇科疾病的药物,包括子宫内膜异位症和 UF,分别于 2018 年和 2020 年获得美国 FDA 批准。