ELAGOLIX

Description: Elagolix (formerly known as NBI56418 and ABT-620; trade name: Orilissa) is a potent, specific, orally bioavailable, non-peptide antagonist of the gonadotropin-releasing hormone receptor (GnRHR) with KD of 54 pM. On 7/23/2018, Elagolix was approved by FDA for the management of moderate to severe pain associated with endometriosis. Elagolix is a short-acting GnRH antagonist that produces a dose-dependent suppression of ovarian estrogen production, that is, from partial suppression at lower doses to full suppression at higher doses. 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.

References: Reprod Sci. 2014 Nov; 21(11):1341-51.

Related CAS#:832720-36-2 (sodium salt)