Relugolix GnRH (LHRH) receptor antagonist Treatment of uterine fibroids Treatment of endometriosis-related pain Treatment of prostate cancer

摘要

Relugolix (TAK-385) is a gonadotropin-releasing hormone (GnRH) antagonist. It is under development and investigation by Myovant Sciences and Takeda for the treatment of endometriosis, uterine fibroids and prostate cancer. Relugolix is a nonpeptide, orally active small-molecule compound that was recently approved in Japan for the treatment of uterine fibroids. Additionally, it is in phase ill trials for endometriosis and prostate cancer. Inhibition of anterior pituitary GnRH receptors results in reduction of the circulating gonadotropins luteinizing hormone and follicle-stimulating hormone, leading to the suppression of estrogen production in women and testosterone production in men. Considering its oral activity and the cost effectiveness compared to injectable GnRH antagonists, as well as the ability to bypass the initial flare effect of traditional GnRH agonists such as leuprolide acetate, relugolix has been actively explored in several ongoing clinical trials as a promising therapeutic opportunity against hormone-dependent diseases.