Literature DB >> 27406083

Obeticholic Acid: First Global Approval.

A Markham1, Susan J Keam2.   

Abstract

Obeticholic acid (Ocaliva(TM)) is a farnesoid-X receptor (FXR) agonist that is being developed by Intercept Pharmaceuticals for the treatment of various liver diseases, and has recently been granted accelerated approval in the USA for the treatment of primary biliary cholangitis in combination with ursodeoxycholic acid in adults with an inadequate response to ursodeoxycholic acid, or as monotherapy in adults unable to tolerate ursodeoxycholic acid. The drug is in preregistration for this indication in the EU. This article summarizes the milestones in the development of obeticholic acid leading to this first approval for primary biliary cholangitis.

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Year:  2016        PMID： 27406083     DOI： 10.1007/s40265-016-0616-x

Source DB:  PubMed          Journal:  Drugs        ISSN： 0012-6667            Impact factor:   9.546


  5 in total

1.  Farnesoid X nuclear receptor ligand obeticholic acid for non-cirrhotic, non-alcoholic steatohepatitis (FLINT): a multicentre, randomised, placebo-controlled trial.

Authors:  Brent A Neuschwander-Tetri; Rohit Loomba; Arun J Sanyal; Joel E Lavine; Mark L Van Natta; Manal F Abdelmalek; Naga Chalasani; Srinivasan Dasarathy; Anna Mae Diehl; Bilal Hameed; Kris V Kowdley; Arthur McCullough; Norah Terrault; Jeanne M Clark; James Tonascia; Elizabeth M Brunt; David E Kleiner; Edward Doo
Journal:  Lancet       Date:  2014-11-07       Impact factor: 79.321

2.  The response of patients with bile acid diarrhoea to the farnesoid X receptor agonist obeticholic acid.

Authors:  J R F Walters; I M Johnston; J D Nolan; C Vassie; M E Pruzanski; D A Shapiro
Journal:  Aliment Pharmacol Ther       Date:  2014-10-20       Impact factor: 8.171

3.  6alpha-ethyl-chenodeoxycholic acid (6-ECDCA), a potent and selective FXR agonist endowed with anticholestatic activity.

Authors:  Roberto Pellicciari; Stefano Fiorucci; Emidio Camaioni; Carlo Clerici; Gabriele Costantino; Patrick R Maloney; Antonio Morelli; Derek J Parks; Timothy M Willson
Journal:  J Med Chem       Date:  2002-08-15       Impact factor: 7.446

4.  Efficacy and safety of the farnesoid X receptor agonist obeticholic acid in patients with type 2 diabetes and nonalcoholic fatty liver disease.

Authors:  Sunder Mudaliar; Robert R Henry; Arun J Sanyal; Linda Morrow; Hanns-Ulrich Marschall; Mark Kipnes; Luciano Adorini; Cathi I Sciacca; Paul Clopton; Erin Castelloe; Paul Dillon; Mark Pruzanski; David Shapiro
Journal:  Gastroenterology       Date:  2013-05-30       Impact factor: 22.682

5.  Efficacy of obeticholic acid in patients with primary biliary cirrhosis and inadequate response to ursodeoxycholic acid.

Authors:  Gideon M Hirschfield; Andrew Mason; Velimir Luketic; Keith Lindor; Stuart C Gordon; Marlyn Mayo; Kris V Kowdley; Catherine Vincent; Henry C Bodhenheimer; Albert Parés; Michael Trauner; Hanns-Ulrich Marschall; Luciano Adorini; Cathi Sciacca; Tessa Beecher-Jones; Erin Castelloe; Olaf Böhm; David Shapiro
Journal:  Gastroenterology       Date:  2014-12-11       Impact factor: 22.682
  5 in total
  22 in total

1.  Discovery of new FXR agonists based on 6-ECDCA binding properties by virtual screening and molecular docking.

Authors:  Antonella Giancristofaro; Arménio J M Barbosa; Alessandra Ammazzalorso; Pasquale Amoia; Barbara De Filippis; Marialuigia Fantacuzzi; Letizia Giampietro; Cristina Maccallini; Rosa Amoroso
Journal:  Medchemcomm       Date:  2018-07-04       Impact factor: 3.597

2.  Weak Microbial Metabolites: a Treasure Trove for Using Biomimicry to Discover and Optimize Drugs.

Authors:  Zdenek Dvorak; Max Klapholz; Thomas P Burris; Benjamin P Willing; Antimo Gioiello; Roberto Pellicciari; Francesco Galli; John March; Stephen J O'Keefe; R Balfour Sartor; Chang H Kim; Maayan Levy; Sridhar Mani
Journal:  Mol Pharmacol       Date:  2020-08-06       Impact factor: 4.436

Review 3.  Nutrient-sensing nuclear receptors PPARα and FXR control liver energy balance.

Authors:  Geoffrey A Preidis; Kang Ho Kim; David D Moore
Journal:  J Clin Invest       Date:  2017-03-13       Impact factor: 14.808

4.  Cenicriviroc, a cytokine receptor antagonist, potentiates all-trans retinoic acid in reducing liver injury in cholestatic rodents.

Authors:  Dongke Yu; Shi-Ying Cai; Albert Mennone; Pamela Vig; James L Boyer
Journal:  Liver Int       Date:  2018-02-13       Impact factor: 5.828

5.  Farnesoid X Receptor Agonists Obeticholic Acid and Chenodeoxycholic Acid Increase Bile Acid Efflux in Sandwich-Cultured Human Hepatocytes: Functional Evidence and Mechanisms.

Authors:  Cen Guo; Carl LaCerte; Jeffrey E Edwards; Kenneth R Brouwer; Kim L R Brouwer
Journal:  J Pharmacol Exp Ther       Date:  2018-02-27       Impact factor: 4.030

Review 6.  The role of farnesoid X receptor in metabolic diseases, and gastrointestinal and liver cancer.

Authors:  Lulu Sun; Jie Cai; Frank J Gonzalez
Journal:  Nat Rev Gastroenterol Hepatol       Date:  2021-02-10       Impact factor: 46.802

7.  Bioequivalence and Pharmacokinetic Profiles of Generic and Branded Obeticholic Acid in Healthy Chinese Subjects Under Fasting and Fed Conditions.

Authors:  Meng-Na Wang; Hai-Tao Yu; Ya-Qian Li; Yun Zeng; Shuang Yang; Guo-Ping Yang; Qi Pei; Jie Huang
Journal:  Drug Des Devel Ther       Date:  2021-01-14       Impact factor: 4.162

8.  Potential of therapeutic bile acids in the treatment of neonatal Hyperbilirubinemia.

Authors:  Lori W E van der Schoor; Henkjan J Verkade; Anna Bertolini; Sanne de Wit; Elvira Mennillo; Eva Rettenmeier; André A Weber; Rick Havinga; Petra Valášková; Jana Jašprová; Dicky Struik; Vincent W Bloks; Shujuan Chen; Andrea B Schreuder; Libor Vítek; Robert H Tukey; Johan W Jonker
Journal:  Sci Rep       Date:  2021-05-27       Impact factor: 4.379

9.  Kinsenoside Alleviates 17α-Ethinylestradiol-Induced Cholestatic Liver Injury in Rats by Inhibiting Inflammatory Responses and Regulating FXR-Mediated Bile Acid Homeostasis.

Authors:  Jiaxiong Ming; Qianqian Xu; Limin Gao; Yanfang Deng; Jie Yin; Qun Zhou; Qingyi Tong; Yonghui Zhang
Journal:  Pharmaceuticals (Basel)       Date:  2021-05-11

Review 10.  Recent advances in the diagnosis and treatment of primary biliary cholangitis.

Authors:  Ying-Qiu Huang
Journal:  World J Hepatol       Date:  2016-11-28
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