MedKoo product information:

Elagolix

Elagolix is a novel, first-in-class oral gonadotropin-releasing hormone (GnRH) antagonist, which has recently completed a phase IIb study in endometriosis. In addition to endometriosis, elagolix will be evaluated for the treatment of uterine fibroids.

On 16. June 2010, Abbott (NYSE: ABT) and Neurocrine Biosciences, Inc. (Nasdaq: NBIX)  announced that they have entered into a collaboration agreement to develop and commercialize elagolix for the treatment of endometriosis-related pain. Source:

According a recent news published in May 2010,  Neurocrine Biosciences, Inc. announced statistically significant and clinically meaningful top-line efficacy results from its Phase II Daisy PETAL study (901 study) using its proprietary, orally-active nonpeptide Gonadotropin-Releasing Hormone (GnRH) receptor antagonist, elagolix, in patients with endometriosis.  “The Daisy PETAL study was successful, all primary and secondary efficacy endpoints were met, and provided exactly the information we need to move this program forward,” said Chris O’Brien, M.D., Chief Medical Officer at Neurocrine. “We now have confirmation that the daily scales for menstrual and non-menstrual pelvic pain, developed with extensive input from the FDA and patients, function well in a clinical trial setting. These daily endpoints reflect the way women with endometriosis experience their symptoms and also demonstrate improvement with elagolix.”

Current developer:    Neurocrine Biosciences, Inc, Abbott.

1: Tomillero A, Moral MA. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2009 Oct;31(8):541-57. PubMed PMID: 19967103.

2: Struthers RS, Nicholls AJ, Grundy J, Chen T, Jimenez R, Yen SS, Bozigian HP. Suppression of gonadotropins and estradiol in premenopausal women by oral administration of the nonpeptide gonadotropin-releasing hormone antagonist elagolix. J Clin Endocrinol Metab. 2009 Feb;94(2):545-51. Epub 2008 Nov 25. PubMed PMID: 19033369; PubMed Central PMCID: PMC2646513.

3: Chen C, Wu D, Guo Z, Xie Q, Reinhart GJ, Madan A, Wen J, Chen T, Huang CQ, Chen M, Chen Y, Tucci FC, Rowbottom M, Pontillo J, Zhu YF, Wade W, Saunders J, Bozigian H, Struthers RS. 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. J Med Chem. 2008 Dec 11;51(23):7478-85.  PubMed PMID: 19006286.