The Sustained Effects of a Dual GIP/GLP-1 Receptor Agonist, NNC0090-2746, in Patients with Type 2 Diabetes

Cell Metabolism - Tập 26 - Trang 343-352.e2 - 2017
Juan Pablo Frias1, Edward J. Bastyr2, Louis Vignati3, Matthias H. Tschöp4,5,6, Christophe Schmitt7, Klara Owen8, Rune Haubo Christensen8, Richard D. DiMarchi9
1National Research Institute, Los Angeles, CA 90057, USA
2Division of Endocrinology & Metabolism, Indiana University School of Medicine, Indianapolis, IN 46202, USA
3Former scientific advisor to MB2 LLC, Carmel, IN 46032, USA
4Institute for Diabetes and Obesity, Helmholtz Diabetes Center at Helmholtz Zentrum München, German Research Center for Environmental Health (GmbH), Neuherberg 85764, Germany
5Division of Metabolic Diseases, Department of Medicine, Technische Universität München, Munich 80333, Germany
6German Center for Diabetes Research (DZD), Neuherberg, 85764, Germany
7F. Hoffmann-La Roche AG, Basel 4070, Switzerland
8Novo Nordisk A/S, Søborg 2860, Denmark
9Novo Nordisk Research Center Indianapolis, Indianapolis, IN, 46241, USA

Tài liệu tham khảo

Aaboe, 2015, Restoration of the insulinotropic effect of glucose-dependent insulinotropic polypeptide contributes to the antidiabetic effect of dipeptidyl peptidase-4 inhibitors, Diabetes Obes. Metab., 17, 74, 10.1111/dom.12395 Baggio, 2007, Biology of incretins: GLP-1 and GIP, Gastroenterology, 132, 2131, 10.1053/j.gastro.2007.03.054 Campbell, 2013, Pharmacology, physiology, and mechanisms of incretin hormone action, Cell Metab., 17, 819, 10.1016/j.cmet.2013.04.008 Campbell, 2016, TCF1 links GIPR signaling to the control of beta cell function and survival, Nat. Med., 22, 84, 10.1038/nm.3997 Chia, 2009, Exogenous glucose-dependent insulinotropic polypeptide worsens post prandial hyperglycemia in type 2 diabetes, Diabetes, 58, 1342, 10.2337/db08-0958 Davies, 2015, Efficacy of liraglutide for weight loss among patients with type 2 diabetes: the SCALE diabetes randomized clinical trial, JAMA, 314, 687, 10.1001/jama.2015.9676 Dungan, 2014, Once-weekly dulaglutide versus once-daily liraglutide in metformin-treated patients with type 2 diabetes (AWARD-6): a randomised, open-label, phase 3, non-inferiority trial, Lancet, 384, 1349, 10.1016/S0140-6736(14)60976-4 Dupre, 1973, Stimulation of insulin secretion by gastric inhibitory polypeptide in man, J. Clin. Endocrinol. Metab., 37, 826, 10.1210/jcem-37-5-826 Finan, 2013, Unimolecular dual incretins maximize metabolic benefits in rodents, monkeys, and humans, Sci. Transl. Med., 5, 209ra151, 10.1126/scitranslmed.3007218 Fineman, 2012, Clinical relevance of anti-exenatide antibodies: safety, efficacy and cross-reactivity with long-term treatment, Diabetes Obes. Metab., 14, 546, 10.1111/j.1463-1326.2012.01561.x Gault, 2002, Characterization of the cellular and metabolic effects of a novel enzyme-resistant antagonist of glucose-dependent insulinotropic polypeptide, Biochem. Biophys. Res. Commun., 290, 1420, 10.1006/bbrc.2002.6364 Gault, 2005, Chemical ablation of gastric inhibitory polypeptide receptor action by daily (Pro3)GIP administration improves glucose tolerance and ameliorates insulin resistance and abnormalities of islet structure in obesity-related diabetes, Diabetes, 54, 2436, 10.2337/diabetes.54.8.2436 Gutniak, 1992, Antidiabetogenic effect of glucagon-like peptide-1 (7-36)amide in normal subjects and patients with diabetes mellitus, N. Engl. J. Med., 326, 1316, 10.1056/NEJM199205143262003 Hermansen, 2013, Liraglutide suppresses postprandial triglyceride and apolipoprotein B48 elevations after a fat-rich meal in patients with type 2 diabetes: a randomized, double-blind, placebo-controlled, cross-over trial, Diabetes Obes. Metab., 15, 1040, 10.1111/dom.12133 Højberg, 2009, Four weeks of near-normalisation of blood glucose improves the insulin response to glucagon-like peptide-1 and glucose-dependent insulinotropic polypeptide in patients with type 2 diabetes, Diabetologia, 52, 199, 10.1007/s00125-008-1195-5 Irwin, 2004, Effects of short-term chemical ablation of the GIP receptor on insulin secretion, islet morphology and glucose homeostasis in mice, Biol. Chem., 385, 845, 10.1515/BC.2004.110 Klonoff, 2008, Exenatide effects on diabetes, obesity, cardiovascular risk factors and hepatic biomarkers in patients with type 2 diabetes treated for at least 3 years, Curr. Med. Res. Opin., 24, 275, 10.1185/030079908X253870 Knop, 2007, The insulinotropic effect of GIP is impaired in patients with chronic pancreatitis and secondary diabetes mellitus as compared to patients with chronic pancreatitis and normal glucose tolerance, Regul. Pept., 144, 123, 10.1016/j.regpep.2007.07.002 Knop, 2007, Reduced incretin effect in type 2 diabetes: cause or consequence of the diabetic state?, Diabetes, 56, 1951, 10.2337/db07-0100 Kreymann, 1987, Glucagon-like peptide-1 7-36: a physiological incretin in man, Lancet, 2, 1300, 10.1016/S0140-6736(87)91194-9 le Roux, 2017, 3 years of liraglutide versus placebo for type 2 diabetes risk reduction and weight management in individuals with prediabetes: a randomised, double-blind trial, Lancet, 389, 1399, 10.1016/S0140-6736(17)30069-7 Lorenz, 2013, Recent progress and future options in the development of GLP-1 receptor agonists for the treatment of diabesity, Bioorg. Med. Chem. Lett., 23, 4011, 10.1016/j.bmcl.2013.05.022 Maffei, 1995, Leptin levels in human and rodent: measurement of plasma leptin and ob RNA in obese and weight-reduced subjects, Nat. Med., 1, 1155, 10.1038/nm1195-1155 McClean, 2007, GIP receptor antagonism reverses obesity, insulin resistance, and associated metabolic disturbances induced in mice by prolonged consumption of high-fat diet, Am. J. Physiol. Endocrinol. Metab., 293, E1746, 10.1152/ajpendo.00460.2007 McIntyre, 1964, New interpretation of oral glucose tolerance, Lancet, 2, 20, 10.1016/S0140-6736(64)90011-X Mentis, 2011, GIP does not potentiate the antidiabetic effects of GLP-1 in hyperglycemic patients with type 2 diabetes, Diabetes, 60, 1270, 10.2337/db10-1332 Milicevic, 2016, Low incidence of anti-drug antibodies in patients with type 2 diabetes treated with once-weekly glucagon-like peptide-1 receptor agonist dulaglutide, Diabetes Obes. Metab., 18, 533, 10.1111/dom.12640 Miyawaki, 2002, Inhibition of gastric inhibitory polypeptide signaling prevents obesity, Nat. Med., 8, 738, 10.1038/nm727 Møller, 2016, Glucose-dependent insulinotropic polypeptide is associated with lower low-density lipoprotein but unhealthy fat distribution, independent of insulin: the ADDITION-PRO study, J. Clin. Endocrinol. Metab., 101, 485, 10.1210/jc.2015-3133 Nauck, 2016, The incretin effect in healthy individuals and those with type 2 diabetes: physiology, pathophysiology, and response to therapeutic interventions, Lancet Diabetes Endocrinol., 4, 525, 10.1016/S2213-8587(15)00482-9 Nauck, 1986, Incretin effects of increasing glucose loads in man calculated from venous insulin and C-peptide responses, J. Clin. Endocrinol. Metab., 63, 492, 10.1210/jcem-63-2-492 Nauck, 1993, Preserved incretin activity of glucagon-like peptide 1 [7-36 amide] but not of synthetic human gastric inhibitory polypeptide in patients with type-2 diabetes mellitus, J. Clin. Invest., 91, 301, 10.1172/JCI116186 Nauck, 1996, Effects of subcutaneous glucagon-like peptide 1 (GLP-1 [7-36 amide]) in patients with NIDDM, Diabetologia, 39, 1546, 10.1007/s001250050613 Nauck, 2009, Efficacy and safety comparison of liraglutide, glimepiride, and placebo, all in combination with metformin, in type 2 diabetes: the LEAD (liraglutide effect and action in diabetes)-2 study, Diabetes Care, 32, 84, 10.2337/dc08-1355 Nauck, 2013, Long-term efficacy and safety comparison of liraglutide, glimepiride and placebo, all in combination with metformin in type 2 diabetes: 2-year results from the LEAD-2 study, Diabetes Obes. Metab., 15, 204, 10.1111/dom.12012 Neff, 2010, Emerging role of GLP-1 receptor agonists in the treatment of obesity, Diabetes Metab. Syndr. Obes., 3, 263, 10.2147/DMSO.S6816 Ng, 2014, Global, regional, and national prevalence of overweight and obesity in children and adults during 1980-2013: a systematic analysis for the Global Burden of Disease Study 2013, Lancet, 384, 766, 10.1016/S0140-6736(14)60460-8 Plutzky, 2009, Reductions in lipids and CV risk markers in patients with type 2 diabetes treated with liraglutide: a meta-analysis, Can. J. Diabetes, 33, 209, 10.1016/S1499-2671(09)33072-5 Portron, 2017, Pharmacodynamics, pharmacokinetics, safety and tolerability of the novel dual GIP/GLP-1 agonist (RG7697) after single subcutaneous administration in healthy subjects, Diabetes Obes. Metab., 10.1111/dom.13025 Reusch, 2014, Diabetes Obes. Metab., 16, 1257, 10.1111/dom.12382 Rosenbaum, 1997, Effects of weight change on plasma leptin concentrations and energy expenditure, J. Clin. Endocrinol. Metab., 82, 3647 Schmitt, 2017, Pharmacodynamics, pharmacokinetics and safety of multiple ascending doses of the novel dual GIP/GLP-1 agonist RG7697 in patients with type 2 diabetes mellitus, Diabetes Obes. Metab., 10.1111/dom.13024 Tschöp, 2016, Unimolecular polypharmacy for treatment of diabetes and obesity, Cell Metab., 24, 51, 10.1016/j.cmet.2016.06.021 Vilsbøll, 2002, Defective amplification of the late phase insulin response to glucose by GIP in obese type II diabetic patients, Diabetologia, 45, 1111, 10.1007/s00125-002-0878-6 World Health Organization (2016). Global Report on Diabetes. Available at: http://apps.who.int/iris/bitstream/10665/204871/1/9789241565257_eng.pdf. Accessed July 4, 2017. Wysham, 2014, Efficacy and safety of dulaglutide added onto pioglitazone and metformin versus exenatide in type 2 diabetes in a randomized controlled trial (AWARD-1), Diabetes Care, 37, 2159, 10.2337/dc13-2760 Xu, 2007, Downregulation of GLP-1 and GIP receptor expression by hyperglycemia: possible contribution to impaired incretin effects in diabetes, Diabetes, 56, 1551, 10.2337/db06-1033