1,143
Views
23
CrossRef citations to date
0
Altmetric
Drug Evaluations

GFT505 for the treatment of nonalcoholic steatohepatitis and type 2 diabetes

&

Bibliography

  • UK Prospective Diabetes Study Group. UK prospective diabetes study 16. Overview of 6 years’ therapy of type II diabetes: a progressive disease. Diabetes 1995;44:1249–58
  • Inzucchi SE, Bergenstal RM, Buse JB, et al. Management of hyperglycaemia in type 2 diabetes : a patient-centered approach. Position statement of the American Diabetes Association (ADA) and the European Association for the Study of Diabetes (EASD). Diabetologia 2012;55:1577–96
  • Tiv M, Viel JF, Mauny F, et al. Medication adherence in type 2 diabetes: the ENTRED study 2007, a French Population-Based Study. PLoS One 2012;7(3):e32412
  • Martin BC, Warram JH, Krolewski AS, et al. Role of glucose and insulin resistance in development of type 2 diabetes mellitus: results of a 25-year follow-up study. Lancet 1992;340:925–9
  • Saltiel AR, Kahn CR. Insulin signalling and the regulation of glucose and lipid metabolism. Nature 2001;414:799–806
  • Smith BW, Adams LA. Nonalcholic fatty liver disease and diabetes mellitus: pathogenesis and treatment. Nat Rev Endocrinol 2011;7:456–65
  • Chalasani N, Younossi Z, Lavine JE, et al. The diagnosis and management of non-alcoholic fatty liver disease: practice guideline by the american association for the study of liver diseases, american college of gastroenterology, and the american gastroenterological association. Hepatology 2012;55:2005–23
  • Ratziu V, Bellentani S, Cortez-Pinto S, et al. A position statement on NAFLD/NASH based on the EASL special conference. J Hepatol 2010;53:372–84
  • Hamaguchi M, Kojima T, Takeda N, et al. The metabolic syndrome as a predictor of nonalcoholic fatty liver disease. Ann Intern Med 2005;143:722–8
  • Postic C, Girard J. Contribution of de novo acid synthesis to hepatic steatosis and insulin resistance: lessons from genetically engineered mice. J Clin Invest 2008;118:829–38
  • Zhan Y, An W. Roles of liver innate immune cells in nonalcoholic fatty liver disease. World J Gastroenterol 2010;16:4652–60
  • Cariou B, Charbonnel B, Staels B. Thiazolidinediones and PPARgamma agonists: time for a reassessment. Trends Endocrinol Metab 2012;23:205–15
  • Phielix E, Szendroedi J, Roden M. The role of metformin and thiazolidinediones in the regulation of hepatic glucose metabolism and its clinical impact. Trends Pharmacol Sci 2011;32:607–16
  • Viollet B, Guigas B, Sanz Garcia N, et al. Cellular and molecular mechanisms of metformin: an overview. Clin Sci (London) 2012;122:253–70
  • Juurinen L, Kotronen A, Graner M, et al. Rosiglitazone reduces liver fat and insulin requirements and improves hepatic insulin sensitivity and glycemic control in patients with type 2 diabetes requiring high insulin doses. J Clin Endocrinol Metab 2008;93:118–24
  • Miyazaki Y, Mahankali A, Matsuda M, et al. Effect of pioglitazone on abdominal fat distribution and insulin sensitivity in type 2 diabetic patients. J Clin Endocrinol Metab 2002;87:2784–91
  • Belfort R, Harrison SA, Brown K, et al. A placebo-controlled trial of piogliotazone in subjects with nonalcoholic steatohepatitis. N Engl J Med 2006;355:2297–22307
  • Boettcher E, Csako G, Pucino F, et al. Meta-analysis : pioglitazone improves liver histology and fibrosis in patients with non-alcoholic steatohepatitis. Aliment Pharmacol Ther 2012;35:66–75
  • Colca JR, McDonald WG, Kletzien RF. Mitochondrial target of thiazolidinediones. Diabetes Obes Metab 2014. [Epub ahead of print]
  • Colca JR, VanderLugt JT, Adams WJ, et al. Clinical proof-of-concept study with MSDC-0160, a prototype mTOT-modulating insulin sensitizing. Clin Pharmacol Ther 2013;93:352–9
  • Intercept Pharmaceuticals, Inc. Press release. 2014. Available from: http://ir.interceptpharma.com/releasedetail.cfm?ReleaseID=818725
  • Mudaliar S, Henry RR, Sanyal AJ, et al. Efficacy andsafety of the farnesoid X receptor agonist obeticholic acid in patients with type 2 diabetes and nonalcoholic fatty liver disease. Gastroenterology 2013;145:574–82
  • Lalloyer F, Staels B. Fibrates, glitazones, and peroxisome proliferator-activated receptors. Arterioscler Thromb Vasc Biol 2010;30:894–9
  • Lefebvre P, Chinetti G, Fruchart JC, et al. Sorting out the roles of PPAR alpha in energy metabolism and vascular homeostasis. J Clin Invest 2006;116:571–80
  • Tanaka T, Yamamoto J, Iwasaki S, et al. Activation of peroxisome proliferator-activated receptor delta induces fatty acid beta-oxidation in skeletal muscle and attenuates metabolic syndrome. Proc Natl Acad Sci USA 2003;100:15924–9
  • Lee CH, Olson P, Hevener A, et al. PPARdelta regulates glucose metabolism and insulin sensitivity. Proc Natl Acad Sci USA 2006;103:3444–9
  • Sprecher DL, Massien C, Pearce G, et al. Triglyceride: high density lipoprotein cholesterol effects in healthy subjects administered a peroxisome proliferator activated receptor delta agonist. Arterioscler Thromb Vasc Biol 2007;27:359–65
  • Riserus U, Sprecher D, Johnson T, et al. Activation of peroxisome proliferator-activated receptor (PPAR) delta promotes reversal of multiple metabolic abnormalities reduces oxidative stress, and increases fatty acid oxidation in moderately obese men. Diabetes 2008;57:332–9
  • Cariou B, Hanf R, Lambert-Porcheron S, et al. Dual peroxisome proliferator-activated receptor alpha/ delta agonist GFT505 improves hepatic and peripheral insulin sensitivity in abdominally obese subjects. Diabetes Care 2013;36:2923–30
  • Lalloyer F, Wouters K, Baron M, et al. Peroxisome proliferator-activated receptor-alpha gene level differently affects lipid metabolism and inflammation in apolipoprotein E2 knock-in mice. Arterioscler Thromb Vasc Biol 2011;31:1573–9
  • Staels B, Rubenstrunk A, Noël B, et al. Hepatoprotective effects of the dual peroxisome proliferator-activated receptor alpha/delta agonist, GFT505, in rodent models of nonalcoholic fatty liver disease/nonalcoholic steatohepatitis. Hepatology 2013;58:1941–52
  • Hanf R, Millatt L, Cariou B, et al. The dual peroxisome proliferator-activated receptor alpha/delta agonist GFT505 exerts anti-diabetic effects in db/db mice without peroxisome proliferator-activated receptor gamma-associated cardiac adverse events. Diab Vasc Dis Res 2014; In press
  • Stienstra R, Mandard S, Patsouris D, et al. Peroxisome proliferator-activated receptor alpha protects against obesity-induced hepatic inflammation. Endocrinology 2007;148:2753–63
  • Tailleux A, Wouters K, Staels B. Roles of PPARs in NAFLD: potential therapeutic targets. Biochim Biophys Acta 2012;1821:809–18
  • Iwaisako K, Haimerl M, Paik YH, et al. Protection from liver fibrosis by a peroxisome proliferator-activated receptor delta agonist. Proc Natl Acad Sci USA 2012;109:E1369–76
  • Cariou B, Zaïr Y, Staels B, et al. Effects of the new dual PPAR alpha / delta agonist GFT505 on lipid and glucose homeostasis in abdominally obese patients with combined dyslipidemia or impaired glucose metabolism. Diabetes Care 2011;34:2008–14
  • Shulman GI. Cellular mechanisms of insulin resistance. J Clin Invest 2000;106:171–7
  • Stefan N, Häring HU. The roles of hepatokines in metabolism. Nat Rev Endocrinol 2013;9:144–52
  • Liu S, Brown JD, Stanya KJ, et al. A diurnal serum lipid integrates hepatic lipogenesis and peripheral fatty acid use. Nature 2013;502:550–4
  • Genfit. Press release. 2014. Available from: http://www.genfit.com/wp-content/uploads/2014/06/2014-06-27-PR-GENFIT-DSMB.pdf
  • Genfit. Press release. 2014. Available from: http://www.genfit.com/wp-content/uploads/2014/03/2012.02.08_PR-GENFIT_EN.pdf
  • Staels B, Maes M, Zambon A. Fibrates and future PPARalpha agonists in the treatment of cardiovascular disease. Nat Clin Pract Cardiovasc Med 2008;5:542–5
  • Fievet C, Fruchart JC, Staels B. PPAR alpha and PPAR gamma dual agonists for the treatment of type 2 diabetes and the metabolic syndrome. Curr Opin Pharmacol 2006;6:606–14
  • Lincoff AM, Tardiff JC, Schwartz GG, et al. Effect of aleglitazar on cardiovascular outcomes after acute coronary syndrome in patients with type 2 diabetes mellitus:the AleCardio randomized clinical trial. JAMA 2014;311:1515–12
  • Ting RD, Keech AC, Drury PL, et al. Benefits and safety of long-term fenofibrate therapy in people with type 2 diabetes and renal impairment : the FIELD study. Diabetes Care 2012;35:218–25
  • Udanis SM, Bakris GL. Do fibrates truly preserve kidney function ? Nat Rev Endocrinol 2011;7:130–1
  • Mackenzie LS, Lione L. Harnessing the benefits of PPAR beta//delta agonists. Life Sci 2013;93:963–7
  • Belfort R, Berria R, Cornell J, Cusi K. Fenofibrate reduces systemic inflammation markers independent of its effects on lipid and glucose metabolism in patients with the metabolic syndrome. J Clin Endocrinol Metab 2010;95:829–36
  • Fabbrini E, Mohammed BS, Korenblat KM, et al. Effect of fenofibrate and niacin on intrahepatic triglyceride content, very low-density lipoprotein kinetics, and insulin action in obese subjects with non alcoholic fatty liver disease. J Clin Endocrinol Metab 2010;95:829–36
  • Bajaj M, Suraamornkul S, Hardies LJ, et al. Effects of peroxisome proliferator-activated receptor (PPAR)- alpha and PPAR- gamma agonists on glucose and lipid metabolism in patients with type 2 diabetes mellitus. Diabetologia 2007;50:1723–31
  • Chen Y, Hu Y, Lin M, et al. Therapeutic effects of PPAR alpha agonists on diabetic retinopathy in type 1 diabetes models. Diabetes 2013;62:261–72
  • ACCORD study group, ACCORD Eye study group. Chew EY, Ambrosius WT, Davis MD, et al. Effects of medical therapies on retinopathy progression in type 2 diabetes. N Engl J Med 2010;363:233–44

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.