治疗子宫内膜异位症新药——elagolix
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摘要
Elagolix是艾伯维和Neurovrine Biosciences联合开发的口服短效促性腺激素释放激素受体(GnRH)拮抗剂,其通过与脑垂体中的GnRH受体竞争结合、降低血液循环中的性腺激素水平发挥疗效。2018年7月23日,elagolix获批用于治疗子宫内膜异位,成为美国食品药品监督管理局首个批准用于治疗子宫内膜异位症的新药。另外,其在子宫肌瘤适应证的Ⅲ期临床研究也值得期待。本文就elagolix的基本信息、作用机制和临床试验情况作一概述。
Elagolix is an oral short acting GnRH receptor antagonist developed by AbbVie and Neurovrine Biosciences. Elagolix reduces the level of gonadotropin in blood circulation by competitive binding with GnRH receptor. On July 23, 2018, elagolix was approved for the treatment of endometriosis, becoming the first FDA approved new drug for the treatment of endometriosis. In addition, the phase Ⅲ clinical study on the indications of uterine leiomyoma is also worth looking forward to. The basic information, mechanism and clinical trials of elagolix were reviewed.
Elagolix is an oral short acting GnRH receptor antagonist developed by AbbVie and Neurovrine Biosciences. Elagolix reduces the level of gonadotropin in blood circulation by competitive binding with GnRH receptor. On July 23, 2018, elagolix was approved for the treatment of endometriosis, becoming the first FDA approved new drug for the treatment of endometriosis. In addition, the phase Ⅲ clinical study on the indications of uterine leiomyoma is also worth looking forward to. The basic information, mechanism and clinical trials of elagolix were reviewed.
引文
[1]田玉玲.B超和CT在诊断子宫肌瘤中的作用对比[J].中外医学研究,2012,3(31):5.
[2]艾伯维公布Elagolix子宫肌瘤临床3期扩大研究积极结果[EB/OL].(2018-08-23)[2018-09-18]. https://news. bioon.com/article/6726308. html.
[3] Struthers R S,Nicholls A J,Grundy J,et al. Suppression of gonadotropins and estradiol in premenopausal women by oral administration of the nonpeptide gonadotropin-releasing hormone antagonist elagolix[J]. J Clin Endocrinol Metab,2009,94(2):545-551.
[4] Ng J, Chwalisz K, Charter D C, et al. Dose-dependent suppression of gonadotropins and ovarian hormones by elagolix in healthy premenopausal women[J]. J Clin Endocrinol Metab, 2017,102(5):1683-1691.
[5] Diamond M P,Carr B,Dmowski W P,et al. Elagolix treatment for endometriosis-associated pain:results from a phase 2, randomized, double-blind, placebo-controlled study[J]. Reprod Sci,2014,21(3):363-371.
[6] Carr B, Giudice L,Dmowski W P,et al. Elagolix, an oral GnRH antagonist for endometriosis associated pain:a randomized controlled study[J]. J Endometr Pelvic Pain Disord, 2013,5(3):105-115.
[7] Carr B,Dmowski W P, O'Brien C, et al. Elagolix, an oral GnRH antagonist, versus subcutaneous depot medroxyprogesterone acetate for the treatment of endometriosis:effects on bone mineral density[J]. Reprod Sci,2014,21(11):1341-1351.
[8] Taylor H S, Giudice L C,Lessey B A,et al. Treatment of endometriosis-associated pain with elagolix, an oral GnRH antagonist[J]. N Engl J Med,2017,377(1):28-40.
[9] ClinicalTrials. Elagolix[EB/OL].(2017-12-17)[2018-08-28].https://www. clinicaltrials. gov/.
[2]艾伯维公布Elagolix子宫肌瘤临床3期扩大研究积极结果[EB/OL].(2018-08-23)[2018-09-18]. https://news. bioon.com/article/6726308. html.
[3] Struthers R S,Nicholls A J,Grundy J,et al. Suppression of gonadotropins and estradiol in premenopausal women by oral administration of the nonpeptide gonadotropin-releasing hormone antagonist elagolix[J]. J Clin Endocrinol Metab,2009,94(2):545-551.
[4] Ng J, Chwalisz K, Charter D C, et al. Dose-dependent suppression of gonadotropins and ovarian hormones by elagolix in healthy premenopausal women[J]. J Clin Endocrinol Metab, 2017,102(5):1683-1691.
[5] Diamond M P,Carr B,Dmowski W P,et al. Elagolix treatment for endometriosis-associated pain:results from a phase 2, randomized, double-blind, placebo-controlled study[J]. Reprod Sci,2014,21(3):363-371.
[6] Carr B, Giudice L,Dmowski W P,et al. Elagolix, an oral GnRH antagonist for endometriosis associated pain:a randomized controlled study[J]. J Endometr Pelvic Pain Disord, 2013,5(3):105-115.
[7] Carr B,Dmowski W P, O'Brien C, et al. Elagolix, an oral GnRH antagonist, versus subcutaneous depot medroxyprogesterone acetate for the treatment of endometriosis:effects on bone mineral density[J]. Reprod Sci,2014,21(11):1341-1351.
[8] Taylor H S, Giudice L C,Lessey B A,et al. Treatment of endometriosis-associated pain with elagolix, an oral GnRH antagonist[J]. N Engl J Med,2017,377(1):28-40.
[9] ClinicalTrials. Elagolix[EB/OL].(2017-12-17)[2018-08-28].https://www. clinicaltrials. gov/.