促性腺激素釋放激素(GnRH)拮抗劑是在促性腺激素釋放激素的基礎(chǔ)上經(jīng)過(guò)人工改造,使其在體內(nèi)不易被酶裂解,穩(wěn)定性增強(qiáng),半衰期延長(zhǎng)的一種藥物,臨床應(yīng)用更安全。其主要通過(guò)快速競(jìng)爭(zhēng)性地與GnRH受體結(jié)合阻斷信號(hào)的傳遞,從而達(dá)到臨床治療目的。艾伯維公司與Neurocrine Biosciences公司共同開(kāi)發(fā)的elagolix是一種口服GnRH拮抗劑,通過(guò)抑制腦垂體促性腺釋放激素受體,最終降低血循環(huán)中的性腺激素水平來(lái)治療子宮內(nèi)膜異位癥,目前處于臨床Ⅲ期,計(jì)劃在2017年提交其治療子宮內(nèi)膜異位癥的新藥申請(qǐng)。

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.