Elagolix, also known as NBI56418 and ABT-620, is a Gonadotropin-Releasing Hormone (GnRH) Antagonist. Elagolix inhibits gonadatropin releasing hormone (GnRH) receptors in the pituitary gland and ultimately reduces circulating sex hormone levels. Elagolix is believed to have its effect by altering the level of pituitary GnRH suppression and, as a result, titrating circulating estrogen levels.
Chen, Chen; Wu, Dongpei; Guo, Zhiqiang; Xie, Qiu; Reinhart, Greg J.; Madan, Ajay; Wen, Jenny; Chen, Takung; Huang, Charles Q.; Chen, Mi; Chen, Yongsheng; Tucci, Fabio C.; Rowbottom, Martin; Pontillo, Joseph; Zhu, Yun-Fei; Wade, Warren; Saunders, John; Bozigian, Haig; Struthers, R. Scott. Discovery of Sodium R-(+)-4-{2-[5-(2-Fluoro-3-methoxyphenyl)-3-(2-fluoro-6-[trifluoromethyl]benzyl)-4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl]-1-phenylethylamino}butyrate (Elagolix), a Potent and Orally Available Nonpeptide Antagonist of the Human Gonadotropin-Releasing Hormone Receptor. Journal of Medicinal Chemistry. Volume 51. Issue 23. Pages 7478-7485. Journal. (2008).
Bartos, Petr; Hylse, Ondrej. Process for preparing elagolix. Assignee Synthon B.V., Neth. WO 2019115019. (2019).
Sulake, Rohidas Shivaji; Shinde, Sagar Raosaheb; Siyan, Rajinder Singh; Bhise, Nandu Baban; Singh, Girij Pal. Process for the preparation of elagolix and pharmaceutically acceptable salts thereof. Assignee Lupin Limited, India. WO 2018198086. (2018).
