Incretin-based therapies for type 2 diabetes mellitus (original) (raw)

• Kreymann, B., Williams, G., Ghatei, M. A. & Bloom, S. R. Glucagon-like peptide-17–36: a physiological incretin in man. Lancet 2, 1300–1304 (1987).
  Article CAS Google Scholar
• Deacon, C. F. Therapeutic strategies based on glucagon-like peptide 1. Diabetes 53, 2181–2189 (2004).
  Article CAS Google Scholar
• Drucker, D. J. The biology of incretin hormones. Cell. Metab. 3, 153–165 (2006).
  Article CAS Google Scholar
• Drucker, D. J. & Nauck, M. A. The incretin system: glucagon-like peptide-1 receptor agonists and dipeptidyl peptidase-4 inhibitors in type 2 diabetes. Lancet 368, 1696–1705 (2006).
  Article CAS Google Scholar
• Deacon, C. F., Johnsen, A. H. & Holst, J. J. Degradation of glucagon-like peptide-1 by human plasma in vitro yields an _N_-terminally truncated peptide that is a major endogenous metabolite in vivo . J. Clin. Endocrinol. Metab. 80, 952–957 (1995).
  CAS PubMed Google Scholar
• Kieffer, T. J., McIntosh, C. H. & Pederson, R. A. Degradation of glucose-dependent insulinotropic polypeptide and truncated glucagon-like peptide 1 in vitro and in vivo by dipeptidyl peptidase IV. Endocrinology 136, 3585–3596 (1995).
  Article CAS Google Scholar
• Cervera, A. et al. Mechanism of action of exenatide to reduce postprandial hyperglycemia in type 2 diabetes. Am. J. Physiol. Endocrinol. Metab. 294, E846–E852 (2008).
  Article CAS Google Scholar
• Nauck, M. A. et al. Preserved incretin activity of glucagon-like peptide 17–36 amide but not of synthetic human gastric inhibitory polypeptide in patients with type-2 diabetes mellitus. J. Clin. Invest. 91, 301–307 (1993).
  Article CAS Google Scholar
• Højberg, P. V. et al. 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, 199–207 (2008).
  Article Google Scholar
• Zander, M., Madsbad, S., Madsen, J. L. & Holst, J. J. Effect of 6-week course of glucagon-like peptide 1 on glycaemic control, insulin sensitivity, and β-cell function in type 2 diabetes: a parallel-group study. Lancet 359, 824–830 (2002).
  Article CAS Google Scholar
• Buse, J. B. et al. Effects of exenatide (exendin-4) on glycemic control over 30 weeks in sulfonylurea-treated patients with type 2 diabetes. Diabetes Care 27, 2628–2635 (2004).
  Article CAS Google Scholar
• DeFronzo, R. A. et al. Effects of exenatide (exendin-4) on glycemic control and weight over 30 weeks in metformin-treated patients with type 2 diabetes. Diabetes Care 28, 1092–1100 (2005).
  Article CAS Google Scholar
• Kendall, D. M. et al. Effects of exenatide (exendin-4) on glycemic control over 30 weeks in patients with type 2 diabetes treated with metformin and a sulfonylurea. Diabetes Care 28, 1083–1091 (2005).
  Article CAS Google Scholar
• Zinman, B. et al. The effect of adding exenatide to a thiazolidinedione in suboptimally controlled type 2 diabetes: a randomized trial. Ann. Intern. Med. 146, 477–485 (2007).
  Article Google Scholar
• Heine, R. J. et al. Exenatide versus insulin glargine in patients with suboptimally controlled type 2 diabetes: a randomized trial. Ann. Intern. Med. 143, 559–569 (2005).
  Article CAS Google Scholar
• Nauck, M. A. et al. A comparison of twice-daily exenatide and biphasic insulin aspart in patients with type 2 diabetes who were suboptimally controlled with sulfonylurea and metformin: a non-inferiority study. Diabetologia 50, 259–267 (2007).
  Article CAS Google Scholar
• Bunck, M. C. et al. β-cell function and glycemic control following one year exenatide therapy, and after 12 week wash out, in patients with type 2 diabetes. Presented at the 68th Annual Meeting of the American Diabetes Association, 2008 June 6–10, San Francisco, US (2008).
  Google Scholar
• Vilsbøll, T. et al. Liraglutide, a long-acting human GLP-1 analog, given as monotherapy significantly improves glycemic control and lowers body weight without risk of hypoglycemia in patients with type 2 diabetes mellitus. Diabetes Care 6, 160–610 (2007).
  Google Scholar
• Seino, Y., Rasmussen, M. F., Zdravkovic, M. & Kaku, K. Dose-dependent improvement in glycemia with once-daily liraglutide without hypoglycemia or weight gain: a double-blind, randomized, controlled trial in Japanese patients with type 2 diabetes. Diabetes Res. Clin. Pract. 81, 161–168 (2008).
  Article CAS Google Scholar
• Zinman, B. et al. Efficacy and safety of the human GLP-1 analog liraglutide in combination with metformin and TZD in patients with type 2 diabetes mellitus (LEAD-4 Met + TZD). Presented at the 44 th Annual Meeting of the European Association for the Study of Diabetes, 2008 September 7–11, Rome, Italy (2008).
  Google Scholar
• Garber, A. et al. Liraglutide versus glimepiride monotherapy for type 2 diabetes (LEAD-3 Mono): a randomised, 52-week, phase III, double-blind, parallel-treatment trial. Lancet 373, 473–481 (2009).
  Article CAS Google Scholar
• Marre, M. et al. Liraglutide, a once-daily human GLP-1 analogue, added to a sulphonylurea over 26 weeks produces greater improvements in glycaemic and weight control compared with adding rosiglitazone or placebo in subjects with type 2 diabetes (LEAD-1 SU). Diabetic Medicine 14 Jan doi:10.1111/j.1464–54912009.02666.x (2009).
• Nauck, M. et al. Efficacy and safety comparison of liraglutide, glimepiride, and placebo, all in combination with metformin in type 2 diabetes mellitus (LEAD-2 Met). Diabetes Care 32, 84–90 (2008).
  Article Google Scholar
• Russell-Jones, D. et al. Significantly better glycemic control and weight reduction with liraglutide, a once-daily human GLP-1 analog, compared with insulin glargine: all as add-on to metformin and a sulfonylurea in type 2 diabetes. Presented at the 68th Annual meeting of the American Diabetes Association, 6–10 June 2008, San Francisco, USA (2008).
  Google Scholar
• Blonde, L. et al. Liragluide: superiror glycemia control vs exenatide when added to metformin and/or SU in type 2 diabetes. Presented at the Annual meeting of the Canadian Diabetes Association, 16 October 2008, Montreal, Quebec, Canada (2008).
  Google Scholar
• Ratner, R. E. et al. A dose-finding study of the new GLP-1 agonist AVE0010 in type 2 diabetes insufficiently controlled with metformin. Presented at the 68th Annual meeting of the American Diabetes Association, 2008 June 6–10, San Francisco, USA (2008).
  Google Scholar
• Kim, D, et al. Effects of once-weekly dosing of a long-acting release formulation of exenatide on glucose control and body weight in subjects with type 2 diabetes. Diabetes Care 30, 1487–1493 (2007).
  Article CAS Google Scholar
• Drucker, D. J. et al. Exenatide once weekly versus twice daily for the treatment of type 2 diabetes: a randomised, open-label, non-inferiority study. Lancet 372, 1240–1250 (2008).
  Article CAS Google Scholar
• Baggio, L. L. et al. A recombinant human glucagon-like peptide (GLP)-1-albumin protein (albugon) mimics peptidergic activation of GLP-1 receptor-dependent pathways coupled with satiety, gastrointestinal motility, and glucose homeostasis. Diabetes 53, 2492–2500 (2004).
  Article CAS Google Scholar
• Bloom, M. et al. Albugon fusion protein; a long-acting analog of GLP-1 that provides lasting anti-diabetic effect in animals. Presented at the 63 rd Annual Meeting of the American Diabetes Association, 2003 June, New Orleans, LO, USA (2003).
  Google Scholar
• Matthews, J. E. et al. Pharmacodynamics, pharmacokinetics, safety and tolerability of albiglutide, a long-acting GLP-1 mimetic, in patients with type 2 diabetes. J. Clin. Endocrinol. Metab. 93, 4810–4817 (2008).
  Article CAS Google Scholar
• Balena, R. et al. Eight weeks of treatment with the long acting, human GLP-1 analogue R1583 improves glycemic control and lowers body weight in subjects with type 2 diabetes mellitus (T2DM) treated with metformin: a double-blind placebo-controlled phase 2 Study. Presented at the 68th Annual Meeting of the American Diabetes Association, 2008 June 6–10, San Francisco, US (2008).
  Google Scholar
• Ratner, R. et al. safety and tolerability of high doses of the long acting, human GLP-1 analogue R1583 in diabetic subjects treated with metformin: a double-blind, placebo-controlled phase 2 study. Presented at the 68th Annual Meeting of the American Diabetes Association, 2008 June 6–10, San Francisco, USA (2008).
  Google Scholar
• Baggio, L. L. et al. The long-acting albumin-exendin-4 GLP-1R agonist CJC-1134 engages central and peripheral mechanisms regulating glucose homeostasis. Gastroenterology 134, 1137–1147 (2008).
  Article CAS Google Scholar
• Ahmad, S. R. & Swann, J. Exenatide and rare adverse events. N. Engl. J. Med. 358, 1970–1972 (2008).
  CAS PubMed Google Scholar
• Raufman, J.-P. et al. Truncated glucagon-like peptide-1 interacts with exendin receptors on disperced acini from guinea pig pancreas. Identification of a mammalian homologue of the reptilian peptide exendin-4. J. Biol. Chem. 267, 21432–21437 (1992).
  CAS PubMed Google Scholar
• Hansotia, T. et al. Double incretin receptor knockout (DIRKO) mice reveal an essential role for the enteroinsular axis in transducing the glucoregulatory actions of DPP-IV inhibitors. Diabetes 53, 1326–1335 (2004).
  Article CAS Google Scholar
• Aschner, P. et al. Effect of the dipeptidyl peptidase-4 inhibitor sitagliptin as monotherapy on glycemic control in patients with type 2 diabetes. Diabetes Care 29, 2632–2637 (2006).
  Article CAS Google Scholar
• Charbonnel, B. et al. Efficacy and safety of the dipeptidyl peptidase-4 inhibitor sitagliptin added to ongoing metformin therapy in patients with type 2 diabetes inadequately controlled with metformin alone. Diabetes Care 29, 2638–2643 (2006).
  Article CAS Google Scholar
• Rosenstock, J. et al. Efficacy and safety of the dipeptidyl peptidase-4 inhibitor sitagliptin added to ongoing pioglitazone therapy in patients with type 2 diabetes: a 24-week, multicenter, randomized, double-blind, placebo-controlled, parallel-group study. Clin. Ther. 28, 1556–1568 (2006).
  Article CAS Google Scholar
• Goldstein, B. J. et al. Effect of initial combination therapy with sitagliptin, a dipeptidyl peptidase-4 inhibitor, and metformin on glycemic control in patients with type 2 diabetes. Diabetes Care 30, 1979–1987 (2007).
  Article CAS Google Scholar
• Scott, R. et al. Efficacy and safety of sitagliptin when added to ongoing metformin therapy in patients with type 2 diabetes. Diabetes Obes. Metab. 10, 959–969 (2008).
  Article CAS Google Scholar
• Raz, I. et al. Efficacy and safety of sitagliptin added to ongoing metformin therapy in patients with type 2 diabetes. Curr. Med. Res. Opin. 24, 537–550 (2008).
  Article CAS Google Scholar
• Pi-Sunyer, F. X. et al. Efficacy and tolerability of vildagliptin monotherapy in drug-naive patients with type 2 diabetes. Diabetes Res. Clin. Pract. 76, 132–138 (2007).
  Article CAS Google Scholar
• Rosenstock, J. et al. Comparison of vildagliptin and rosiglitazone monotherapy in patients with type 2 diabetes: a 24-week, double-blind, randomized trial. Diabetes Care 30, 217–223 (2007).
  Article CAS Google Scholar
• Bolli, G. et al. Efficacy and tolerability of vildagliptin vs. pioglitazone when added to metformin: a 24-week, randomized, double-blind study. Diabetes Obes. Metab. 10, 82–90 (2008).
  CAS PubMed Google Scholar
• Lankas, G. R. et al. Dipeptidyl peptidase IV inhibition for the treatment of type 2 diabetes: potential importance of selectivity over dipeptidyl peptidases 8 and 9. Diabetes 54, 2988–2994 (2005).
  Article CAS Google Scholar
• Chan, J. C. et al. Safety and efficacy of sitagliptin in patients with type 2 diabetes and chronic renal insufficiency. Diabetes Obes. Metab. 10, 545–555 (2008).
  Article CAS Google Scholar
• Defronzo, R. A. et al. Efficacy and safety of the dipeptidyl peptidase-4 inhibitor alogliptin in patients with type 2 diabetes mellitus and inadequate glycemic control: a randomized, double-blind, placebo-controlled study. Diabetes Care 31, 2315–2317 (2008).
  Article CAS Google Scholar
• Nauck, M. A. et al. Efficacy and safety of adding the dipeptidyl peptidase-4 inhibitor alogliptin to metformin therapy in patients with type 2 diabetes inadequately controlled with metformin monotherapy: a multicentre, randomised, double-blind, placebo-controlled study. Int. J. Clin. Pract. 63, 46–55 (2009).
  Article CAS Google Scholar
• Fonseca, V. et al. Addition of vildagliptin to insulin improves glycaemic control in type 2 diabetes. Diabetologia 50, 1148–1155 (2007).
  Article CAS Google Scholar
• Garcia-Soria, G. et al. The dipeptidyl peptidase-4 inhibitor PHX1149 improves blood glucose control in patients with type 2 diabetes mellitus. Diabetes Obes. Metab. 10, 293–300 (2008).
  Article CAS Google Scholar
• Ghofaili, K. A. et al. Effect of exenatide on β cell function after islet transplantation in type 1 diabetes. Transplantation 83, 24–28 (2007).
  Article Google Scholar
• Froud, T. et al. The use of exenatide in islet transplant recipients with chronic allograft dysfunction: safety, efficacy, and metabolic effects. Transplantation 86, 36–45 (2008).
  Article Google Scholar
• Inzucchi, S. E. & McGuire, D. K. New drugs for the treatment of diabetes: part II: incretin-based therapy and beyond. Circulation 117, 574–584 (2008).
  Article Google Scholar
• Sokos, G. G. et al. Glucagon-like peptide-1 infusion improves left ventricular ejection fraction and functional status in patients with chronic heart failure. J. Card. Fail. 12, 694–699 (2006).
  Article CAS Google Scholar
• Nikolaidis, L. A. et al. Effects of glucagon-like peptide-1 in patients with acute myocardial infarction and left ventricular dysfunction after successful reperfusion. Circulation 109, 962–965 (2004).
  Article CAS Google Scholar