Synthesis of [H ‐3]‐ and [C‐14]‐labeled elagolix

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 (ABT‐620) is currently approved for the treatment of pain associated with endometriosis and as a combination with estradiol and norethindrone acetate is approved for management of heavy menstrual bleeding due to uterine fibroids. In order to support the development of elagolix, we prepared [3H]elagolix for preclinical metabolism studies and [14C]elagolix for environmental risk assessment studies. 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 (ABT‐620) is currently approved for the treatment of pain associated with endometriosis and as a combination with estradiol and norethindrone acetate is approved for management of heavy menstrual bleeding due to uterine fibroids. In order to support the development of elagolix, we prepared [3H]elagolix for preclinical metabolism studies and [14C]elagolix for environmental risk assessment studies.
Source: Journal of Labelled Compounds and Radiopharmaceuticals - Category: Biochemistry Authors: Tags: RESEARCH ARTICLE Source Type: research