High Quality Elagolix Sodium Powder CAS 832720-36-2

Elagolix sodium (ABT-620) is a small molecule, orally active gonadotropin-releasing hormone (GnRH) receptor antagonist. It has the ability to suppress estradiol (E2) concentrations in a dose-dependent manner.It was originally developed by Neurocrine Biosciences, then licensed to Abbott (now Abbvie) for worldwide co-development of this indication in 2010. AbbVie is applying to use elagolix for the treatment of endometriosis with associated pain. Elagolix is the first orally available GnRH antagonist, and as such may provide patients with relief from the painful symptoms of endometriosis while offering advantages over currently available injectable peptide-based treatments. The estimated patient population is over 170 million women worldwide.
Elagolix is an antagonist of the gonadotropin-releasing hormone receptor (GnRHR; Ki= 0.9 nM in a radioligand binding assay). It is selective for GnRHR over the cytochrome P450 (CYP) isoform CYP3A4 (IC50= 56 μM) as well as a panel of 100 receptors, ion channels, enzymes, and transporters (IC50s = >10 μM). Elagolix inhibits GnRH-induced inositol phosphate production in RBL-1 cells expressing human GnRHR (IC50= 1.5 nM).In vivo, elagolix (30 mg/kg) suppresses production of luteinizing hormone in castrated male cynomolgus macaques. Formulations containing elagolix have been used in the treatment of endometriosis.
Elagolix sodium is a small synthetic molecule chemically known as Sodium 4-({(1R)-2- [5-(2-fluoro-3-methoxyphenyl)-3-{[2-fluoro-6-(trifluoromethyl) phenyl]methyl}-4- methyl -2,6-dioxo-3,6-dihydropyrimidin-1(2H)-yl]-1-phenylethyl} amino)butanoate. The structure was confirmed by mass spectrometry, infrared spectroscopy, nuclear magnetic resonance.Elagolix sodium is isolated as a hygroscopic, amorphous white to off-white to light yellow powder.