Leyland Nicholas, Estes Stephanie J, Lessey Bruce A, Advincula Arnold P, Taylor Hugh S
Department of Obstetrics and Gynecology, McMaster University, Hamilton, Ontario, Canada.
Department of Obstetrics and Gynecology, Penn State Health, Hershey, Pennsylvania, USA.
J Womens Health (Larchmt). 2021 Apr;30(4):569-578. doi: 10.1089/jwh.2019.8096. Epub 2020 Sep 22.
Pain associated with endometriosis is a considerable burden for women, permeating all aspects of their lives, from their ability to perform daily activities to their quality of life. Although there are many options for endometriosis-associated pain management, they are often limited by insufficient efficacy, inconvenient routes of administration, and/or intolerable side effects. Elagolix, a nonpeptide, small-molecule gonadotropin-releasing hormone (GnRH) receptor antagonist, is the first new oral therapy to be approved for the treatment of endometriosis-associated pain in the United States in more than a decade. Modulation of estradiol with elagolix is dose dependent and ranges from partial to full suppression. Clinical evidence has shown that elagolix at both approved doses (150 mg once daily and 200 mg twice daily) is effective for reducing symptoms of pelvic pain (dysmenorrhea, nonmenstrual pelvic pain, and dyspareunia), improving quality of life, and decreasing use of rescue analgesics (nonsteroidal anti-inflammatory drugs and/or opioids). The availability of two dosing options allows for individualization of treatment based on baseline clinical factors and response to therapy. Elagolix is well tolerated, with less pronounced hypoestrogenic effects compared with GnRH agonists. This review provides an overview of elagolix, highlighting currently available treatment options and the application of this new treatment for women with endometriosis-associated pain.
子宫内膜异位症相关疼痛给女性带来了相当大的负担，渗透到她们生活的方方面面，从日常活动能力到生活质量。尽管有多种治疗子宫内膜异位症相关疼痛的方法，但这些方法往往受到疗效不足、给药途径不便和/或难以忍受的副作用的限制。Elagolix是一种非肽类小分子促性腺激素释放激素（GnRH）受体拮抗剂，是十多年来在美国首个被批准用于治疗子宫内膜异位症相关疼痛的新型口服疗法。Elagolix对雌二醇的调节呈剂量依赖性，范围从部分抑制到完全抑制。临床证据表明，两种批准剂量（每日一次150mg和每日两次200mg）的Elagolix均能有效减轻盆腔疼痛症状（痛经、非经期盆腔疼痛和性交困难），改善生活质量，并减少急救镇痛药（非甾体抗炎药和/或阿片类药物）的使用。两种给药方案的可用性使得能够根据基线临床因素和治疗反应进行个体化治疗。Elagolix耐受性良好，与GnRH激动剂相比，雌激素缺乏效应不那么明显。本综述概述了Elagolix，重点介绍了目前可用的治疗方案以及这种新疗法在患有子宫内膜异位症相关疼痛的女性中的应用。
