Synthesis of [H-3] and [C-14] Labeled Elagolix†.

Abstract

Gonadotropin-releasing hormone (GnRH) receptor antagonists are an important class of compounds designed to block the pituitary gland from synthesizing follicle stimulating hormone and luteinizing hormone for the treatment of sex hormone dependent disorders. Elagolix (Orilissa™, ABT-620) is currently approved for the treatment of pain associated with endometriosis1 and ORIAHNN™ (elagolix, estradiol and norethindrone acetate) is approved for management of heavy menstrual bleeding due to uterine fibroids in pre-menopausal women.2 In order to support the development of elagolix, we prepared [3 H]elagolix for preclinical metabolism studies and [14 C]elagolix for environmental risk assessment studies.