促性腺激素释放激素(GnRH)拮抗剂是在促性腺激素释放激素的基础上经过人工改造,使其在体内不易被酶裂解,稳定性增强,半衰期延长的一种药物,临床应用更安全。其主要通过快速竞争性地与GnRH受体结合阻断信号的传递,从而达到临床治疗目的。艾伯维公司与Neurocrine Biosciences公司共同开发的elagolix是一种口服GnRH拮抗剂,通过抑制脑垂体促性腺释放激素受体,最终降低血循环中的性腺激素水平来治疗子宫内膜异位症,目前处于临床Ⅲ期,计划在2017年提交其治疗子宫内膜异位症的新药申请。

Gonadotropin-releasing hormone (GnRH) antagonist is a drug which is not easily be cleaved in the body by artificial modification on the basis of the GnRH. Its stability is enhanced, and the half-life is prolonged. As a result, the clinical application of GnRH antagonist is safer. It blocks the transmission of signal mainly by binding with GnRH receptor rapidly and competitively, thereby reaching the purpose of clinical treatment. Elagolix is an oral GnRH antagonist, which is developed by AbbVie Company and Neurocrine Biosciences Company. It can inhibit pituitary gonadotropin-releasing hormone receptor, and ultimately reduce the sex hormone levels in blood circulation to treat endometriosis. It is currently in phase Ⅲ clinical studies, and has been planed to submit a new drug application in treatment of endometriosis in 2017.