促性腺激素释放激素拮抗剂研究进展

Research progress of Gonadotropin-releasing Hormone Antagonists

促性腺激素释放激素(GnRH)拮抗剂是对GnRH的分子结构进行人为改造继而合成出的一种Gn RH类似物,这种Gn RH类似物在人体吸收后被酶裂解的速度变慢,半衰期延长,临床用药更为安全。其发挥作用的方式主要是竞争性地结合促性腺激素释放激素受体(GnRHR),从而快速有效地切断信号的传递,目前临床上广泛地应用于各种性激素类疾病。例如子宫内膜异位症、前列腺癌、子宫肌瘤以及体外受精-胚胎移植(IVF-ET)方案。Gn RHA研究进展较缓慢,本文将对最新上市或处于临床研究的GnRHA进行综述。

Gonadotropin-releasing hormone(GnRH) antagonist is a GnRH analogue synthesized by artificial modification of the molecular structure of GnRH.This GnRH analogue, after being absorbed by human body, has a slower rate of enzyme lysis and a longer half-life, making it safer for clinical use. It acts by competitively binding to the gonadotropin-releasing hormone receptor(GnRHR) to quickly and effectively cut off signal transmission. It is widely used in various sex hormone diseases in clinical practice at present. Examples include endometriosis, prostate cancer, uterine fibroids, and in vitro fertilization-embryo transfer(IVF-ET) regimens. GnRHA research progress is slow, this paper will review the latest GnRHA on the market or in clinical studies.