sufugolix

Sufugolix is a non-peptide, orally active, small molecule drug that acts as a highly potent and selective antagonist of the gonadotropin-releasing hormone receptor (GnRHR), also known as the luteinizing hormone-releasing hormone (LHRH) receptor. It was developed by Takeda for the treatment of endometriosis and uterine leiomyoma (fibroids). Sufugolix reached phase II clinical trials for both indications but development was discontinued in favor of relugolix, which demonstrated a more favorable pharmacological profile. Mechanistically, sufugolix is distinct from other GnRHR antagonists in that it functions as a non-competitive or insurmountable/trapping antagonist rather than a competitive antagonist. The drug suppresses gonadotropin and sex hormone levels rapidly and reversibly upon oral administration[1][4][5][6].

Other names

sufugolixSufugolix [INN:BAN]