Journal ArticleDOI
Efficacy and safety of the farnesoid X receptor agonist obeticholic acid in patients with type 2 diabetes and nonalcoholic fatty liver disease.
Sunder Mudaliar,Robert R. Henry,Arun J. Sanyal,Linda Morrow,Hanns-Ulrich Marschall,Mark Kipnes,Luciano Adorini,Cathi Sciacca,Paul Clopton,E. Castelloe,Paul Dillon,Mark Pruzanski,David Shapiro +12 more
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TLDR
Administration of 25 or 50 mg OCA for 6 weeks was well tolerated, increased insulin sensitivity, and reduced markers of liver inflammation and fibrosis in patients with type 2 diabetes mellitus and nonalcoholic fatty liver disease.About:
This article is published in Gastroenterology.The article was published on 2013-09-01. It has received 794 citations till now. The article focuses on the topics: Insulin resistance & Nonalcoholic fatty liver disease.read more
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Novel Pharmacotherapy Options for NASH
TL;DR: The need for specific pharmacotherapy is now acknowledged by practitioners, the pharmaceutical industry, and regulators and is largely expected by patients, and there is a clear move away from products developed second hand for NASH or from generic, non-specific hepatoprotectors toward molecules developed and tested specifically forNASH.
Journal ArticleDOI
Modeling and Experimental Studies of Obeticholic Acid Exposure and the Impact of Cirrhosis Stage.
Jeffrey E. Edwards,Carl LaCerte,T. Peyret,Nathalie H. Gosselin,J.F. Marier,AF Hofmann,David Shapiro +6 more
TL;DR: There was good agreement between predicted and observed increases in systemic OCA exposure in subjects with mild, moderate, and severe hepatic impairment, which were 1.4‐, 8‐, and 13‐fold relative to healthy volunteers.
Journal ArticleDOI
The intrahepatic expression levels of bile acid transporters are inversely correlated with the histological progression of nonalcoholic fatty liver disease
Kazuya Okushin,Takeya Tsutsumi,Kenichiro Enooku,Hidetaka Fujinaga,Akira Kado,Junji Shibahara,Masashi Fukayama,Kyoji Moriya,Hiroshi Yotsuyanagi,Kazuhiko Koike +9 more
TL;DR: The expression levels of the BA export transporter BSEP were inversely correlated with NAS in NAFLD patients, suggesting down-regulation may cause excessive BA levels in hepatocytes, leading to cell injury.
Journal ArticleDOI
Activation of FXR protects against renal fibrosis via suppressing Smad3 expression.
Kai Zhao,Jialin He,Yan Zhang,Zhizhen Xu,Haojun Xiong,Rujun Gong,Song Li,Shan Chen,Fengtian He +8 more
TL;DR: It is found that the level of FXR was negatively correlated with that of Smad3 and fibronectin (a marker of fibrosis) in human fibrotic kidneys, and FXR/Smad3 pathway may be a novel target for the treatment of renal fibrosis.
Journal ArticleDOI
Farnesoid X receptor agonist INT-767 attenuates liver steatosis and inflammation in rat model of nonalcoholic steatohepatitis.
Ying-Bin Hu,Xin-Yu Liu,Wei Zhan +2 more
TL;DR: INT-767 robustly restores the lipid, glucose metabolism to normal level, attenuates insulin resistance through upregulating FXR level and reverting the dysregulation of its target genes in liver metabolism, and attenuates the pro-inflammatory response by suppression of TNF-α and NF-κB signaling pathway.
References
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Journal ArticleDOI
Diagnosis and Classification of Diabetes Mellitus
TL;DR: The chronic hyperglycemia of diabetes is associated with long-term damage, dys-function, and failure of differentorgans, especially the eyes, kidneys, nerves, heart, and blood vessels.
Journal ArticleDOI
Glucose clamp technique: a method for quantifying insulin secretion and resistance.
TL;DR: Methods for the quantification of beta-cell sensitivity to glucose (hyperglycemic clamp technique) and of tissue sensitivity to insulin (euglycemic insulin clamp technique] are described.
Journal ArticleDOI
Fibroblast growth factor 15 functions as an enterohepatic signal to regulate bile acid homeostasis
Takeshi Inagaki,Mihwa Choi,Antonio Moschetta,Li Peng,Carolyn L. Cummins,Jeffrey G. McDonald,Guizhen Luo,Stacey A. Jones,Bryan Goodwin,James A. Richardson,Robert D. Gerard,Joyce J. Repa,David J. Mangelsdorf,Steven A. Kliewer +13 more
TL;DR: It is demonstrated that fibroblast growth factor 15 signals from intestine to liver to repress the gene encoding cholesterol 7alpha-hydroxylase (CYP7A1), which catalyzes the first and rate-limiting step in the classical bile acid synthetic pathway.
Journal ArticleDOI
Gut microbiota regulates bile acid metabolism by reducing the levels of tauro-beta-muricholic acid, a naturally occurring FXR antagonist.
Sama I. Sayin,Annika Wahlström,Jenny Felin,Sirkku Jäntti,Hanns-Ulrich Marschall,Krister Bamberg,Bo Angelin,Tuulia Hyötyläinen,Matej Orešič,Fredrik Bäckhed,Fredrik Bäckhed +10 more
TL;DR: It is suggested that the gut microbiota not only regulates secondary bile acids metabolism but also inhibits bile acid synthesis in the liver by alleviating FXR inhibition in the ileum.
Journal ArticleDOI
Role of Bile Acids and Bile Acid Receptors in Metabolic Regulation
TL;DR: Results suggest that modulation of FXR activity and BA metabolism may open new attractive pharmacological approaches for the treatment of the metabolic syndrome and type 2 diabetes.
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Farnesoid X nuclear receptor ligand obeticholic acid for non-cirrhotic, non-alcoholic steatohepatitis (FLINT): a multicentre, randomised, placebo-controlled trial
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 J. McCullough,Norah A. Terrault,Jeanne M. Clark,James Tonascia,Elizabeth M. Brunt,David E. Kleiner,Edward Doo +17 more