Obeticholic Acid (INT747; 6-ECDCA) is a novel derivative of cholic acid which acts as a potent and selective FXR agonist displaying anticholeretic activity in an in vivo rat model of cholestasis. It inhibits vascular smooth muscle cell inflammation and migration as well as promotes adipocyte differentiation and regulates adipose cell function in vivo.
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He XL, Wang LT, Gu XZ, Xiao JX, Qiu WW. A facile synthesis of ursodeoxycholic acid and obeticholic acid from cholic acid. Steroids. 2018 Dec;140:173-178. doi: 10.1016/j.steroids.2018.10.009. Epub 2018 Oct 31. PubMed PMID: 30389306.
Pellicciari, Roberto. Preparation of 6α-alkyl-chenodeoxycholic acid derivatives as farnesoid X receptor agonist. WO 2002072598.
Steiner, Andre; Waenerlund Poulsen, Heidi; Jolibois, Emilie; Rewolinski, Melissa; Gross, Ralf; Sharp, Emma; Dubas-Fisher, Fiona; Eberlin, Alex. Preparation and uses of obeticholic acid. US 20130345188. (Assignee Intercept Pharmaceuticals, Inc., USA)
Weymouth-Wilson, Alexander; Komsta, Zofia; Boydell, James; Wallis, Laura; Otter, Carl; Davies, Ieuan; Clarkson, Rob. Preparation of 6α-alkyl-6,7-dione steroids as intermediates for the production of FXR receptor modulators. WO 2016079520. (Assignee Dextra Laboratories Limited, UK)
Coutable, Ludovic. Preparation of obeticholic acid from 3α-hydroxy-7-keto-5β-cholanic acid comprising continuous flow process steps. EP 3287467. (Assignee Ratiopharm GmbH, Germany)
Siripragada, Mahender Rao; Tomer, Sanjiv; Patel, Nilav; Shah, Sudhir; Reddy, Sudharshan; Sharma, Dhaval. An improved process for preparation of obeticholic acid. WO 2018220513. (Assignee Alembic Pharmaceuticals Limited, India)
