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Synthesis of [H‐3]‐ and [C‐14]‐labeled elagolix
Author(s) -
Soli Eric D.,
Surber Bruce W.,
Reed Aimee D.
Publication year - 2021
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.3908
Subject(s) - luteinizing hormone , hormone , chemistry , hormone receptor , follicle stimulating hormone , uterine fibroids , medicine , endocrinology , pharmacology , gynecology , biochemistry , cancer , breast cancer
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 [ 3 H]elagolix for preclinical metabolism studies and [ 14 C]elagolix for environmental risk assessment studies.