832720-36-2

Application：Elagolix (INN, USAN) (former developmental code names NBI-56418, ABT-620) is a highly potent, selective, orally-active, short-duration, non-peptide antagonist of the gonadotropin-releasing hormone receptor (GnRHR) (KD = 54 pM) that is under development for clinical use by Neurocrine Biosciences and AbbVie. As of 2015, it is in phase III clinical trials for the treatment of endometriosis and uterine leiomyoma. The drug was also under investigation for the treatment of prostate cancer and benign prostatic hyperplasia, but development for these indications was ultimately not pursued. Elagolix is regarded as the frontrunner of a new class of GnRH inhibitors that have been denoted as second-generation, due to their non-peptide nature and oral bioavailability.
Because of the relatively short half-life of elagolix, the actions of gonadotropin-releasing hormone (GnRH) are not fully blocked throughout the day. For this reason, gonadotropin and sex hormone levels are only partially suppressed, and the degree of suppression can be dose-dependently adjusted as desired. Moreover, if elagolix is discontinued, its effects are rapidly reversible. Due to the suppression of estrogen levels by elagolix being incomplete, effects on bone mineral density are minimal, which is in contrast to first-generation GnRH inhibitors. Moreover, the incidence and severity of menopausal side effects such as hot flashes are also reduced relative to first-generation GnRH inhibitors.