Exenatide and liraglutide: different approaches to develop GLP-1 receptor agonists (incretin mimetics) – preclinical and clinical results

Wild, 2004, Global prevalence of diabetes: estimates for the year 2000 and projections for 2030, Diabetes Care, 27, 1047, 10.2337/diacare.27.5.1047 Amori, 2007, Efficacy and safety of incretin therapy in type 2 diabetes: systematic review and meta-analysis, The Journal of the American Medical Association, 298, 194, 10.1001/jama.298.2.194 Bolen, 2007, Systematic review: comparative effectiveness and safety of oral medications for type 2 diabetes mellitus 5, Annals of Internal Medicine, 147, 386, 10.7326/0003-4819-147-6-200709180-00178 Turner, 1998, The U.K. prospective diabetes study. A review, Diabetes Care, 21, C35, 10.2337/diacare.21.3.C35 Turner, 1999, Glycemic control with diet, sulfonylurea, metformin, or insulin in patients with type 2 diabetes mellitus: progressive requirement for multiple therapies (UKPDS 49). UK Prospective Diabetes Study (UKPDS) Group, The Journal of the American Medical Association, 281, 2005, 10.1001/jama.281.21.2005 Nauck, 1986, Reduced incretin effect in type 2 (non-insulin-dependent) diabetes, Diabetologia, 29, 46, 10.1007/BF02427280 Vilsboll, 2004, Incretins, insulin secretion and Type 2 diabetes mellitus, Diabetologia, 47, 357, 10.1007/s00125-004-1342-6 Kjems, 2003, The influence of GLP-1 on glucose-stimulated insulin secretion: effects on beta-cell sensitivity in type 2 and nondiabetic subjects, Diabetes, 52, 380, 10.2337/diabetes.52.2.380 Baggio, 2007, Biology of incretins: GLP-1 and GIP, Gastroenterology, 132, 2131, 10.1053/j.gastro.2007.03.054 Zander, 2002, Effect of 6-week course of glucagon-like peptide 1 on glycaemic control, insulin sensitivity, and beta-cell function in type 2 diabetes: a parallel-group study, Lancet, 359, 824, 10.1016/S0140-6736(02)07952-7 Eng, 1992, Isolation and characterization of exendin-4, an exendin-3 analogue, from Heloderma suspectum venom. Further evidence for an exendin receptor on dispersed acini from guinea pig pancreas, The Journal of Biological Chemistry, 267, 7402, 10.1016/S0021-9258(18)42531-8 Kolterman, 2005, Pharmacokinetics, pharmacodynamics, and safety of exenatide in patients with type 2 diabetes mellitus, American Journal of Health-system Pharmacy, 62, 173, 10.1093/ajhp/62.2.173 Cvetkovic, 2007, Exenatide: a review of its use in patients with type 2 diabetes mellitus (as an adjunct to metformin and/or a sulfonylurea), Drugs, 67, 935, 10.2165/00003495-200767060-00008 Fineman, 2003, Effect on glycemic control of exenatide (synthetic exendin-4) additive to existing metformin and/or sulfonylurea treatment in patients with type 2 diabetes, Diabetes Care, 26, 2370, 10.2337/diacare.26.8.2370 Joy, 2005, Incretin mimetics as emerging treatments for type 2 diabetes 5, Annals of Pharmacotherapy, 39, 110, 10.1345/aph.1E245 Cervera, 2008, Mechanism of action of exenatide to reduce postprandial hyperglycemia in type 2 diabetes 11, American Journal of Physiology. Endocrinology and Metabolism, 294, E846, 10.1152/ajpendo.00030.2008 Buse, 2004, Effects of exenatide (exendin-4) on glycemic control over 30 weeks in sulfonylurea-treated patients with type 2 diabetes, Diabetes Care, 27, 2628, 10.2337/diacare.27.11.2628 DeFronzo, 2005, 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, 10.2337/diacare.28.5.1092 Kendall, 2005, 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, 10.2337/diacare.28.5.1083 Blonde, 2006, Interim analysis of the effects of exenatide treatment on A1C, weight and cardiovascular risk factors over 82 weeks in 314 overweight patients with type 2 diabetes, Diabetes, Obesity and Metabolism, 8, 436, 10.1111/j.1463-1326.2006.00602.x 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, Current Medical Research and Opinion, 24, 275, 10.1185/030079908X253870 Schwartz, 2008, Effect of exenatide on 24-hour blood glucose profile compared with placebo in patients with type 2 diabetes: a randomized, double-blind, two-arm, parallel-group, placebo-controlled, 2-week study 1, Clinical Therapeutics, 30, 858, 10.1016/j.clinthera.2008.05.004 Zinman, 2007, The effect of adding exenatide to a thiazolidinedione in suboptimally controlled type 2 diabetes: a randomized trial, Annals of Internal Medicine, 146, 477, 10.7326/0003-4819-146-7-200704030-00003 Heine, 2005, Exenatide versus insulin glargine in patients with suboptimally controlled type 2 diabetes: a randomized trial, Annals of Internal Medicine, 143, 559, 10.7326/0003-4819-143-8-200510180-00006 Nauck, 2007, 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, 10.1007/s00125-006-0510-2 Viswanathan, 2007, Exenatide therapy in obese patients with type 2 diabetes mellitus treated with insulin, Endocrine Practice, 13, 444, 10.4158/EP.13.5.444 Davis, 2007, Exploring the substitution of exenatide for insulin in patients with type 2 diabetes treated with insulin in combination with oral antidiabetes agents, Diabetes Care, 30, 2767, 10.2337/dc06-2532 Fehse, 2005, Exenatide augments first- and second-phase insulin secretion in response to intravenous glucose in subjects with type 2 diabetes, The Journal of Clinical Endocrinology and Metabolism, 90, 5991, 10.1210/jc.2005-1093 Bunck, 2008, Beta-cell function and glycemic control following one year exenatide therapy, and after 12 week wash out, in patients with type 2 diabetes 1, Diabetes, 57, A32 Kim, 2007, 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, 10.2337/dc06-2375 Drucker, 2008, Exenatide once weekly versus twice daily for the treatment of type 2 diabetes: a randomised, open-label, non-inferiority study, Lancet, 372, 1240, 10.1016/S0140-6736(08)61206-4 Degn, 2004, Effect of intravenous infusion of exenatide (synthetic exendin-4) on glucose-dependent insulin secretion and counterregulation during hypoglycemia, Diabetes, 53, 2397, 10.2337/diabetes.53.9.2397 Nauck, 2002, Effects of glucagon-like peptide 1 on counterregulatory hormone responses, cognitive functions, and insulin secretion during hyperinsulinemic, stepped hypoglycemic clamp experiments in healthy volunteers, The Journal of Clinical Endocrinology and Metabolism, 87, 1239, 10.1210/jcem.87.3.8355 Denker, 2006, Exenatide (exendin-4)-induced pancreatitis: a case report, Diabetes Care, 29, 471, 10.2337/diacare.29.02.06.dc05-2043 Agerso, 2003, Pharmacodynamics of NN2211, a novel long acting GLP-1 derivative, European Journal of Pharmaceutical Sciences, 19, 141, 10.1016/S0928-0987(03)00073-3 Damholt, 2006, An open-label, parallel group study investigating the effects of age and gender on the pharmacokinetics of the once-daily glucagon-like peptide-1 analogue liraglutide 2, Journal of Clinical Pharmacology, 46, 635, 10.1177/0091270006288215 Madsbad, 2004, Improved glycemic control with no weight increase in patients with type 2 diabetes after once-daily treatment with the long-acting glucagon-like peptide 1 analog liraglutide (NN2211): a 12-week, double-blind, randomized, controlled trial, Diabetes Care, 27, 1335, 10.2337/diacare.27.6.1335 Feinglos, 2005, Effects of liraglutide (NN2211), a long-acting GLP-1 analogue, on glycaemic control and bodyweight in subjects with Type 2 diabetes, Diabetic Medicine, 22, 1016, 10.1111/j.1464-5491.2005.01567.x Harder, 2004, The effect of liraglutide, a long-acting glucagon-like peptide 1 derivative, on glycemic control, body composition, and 24-h energy expenditure in patients with type 2 diabetes, Diabetes Care, 27, 1915, 10.2337/diacare.27.8.1915 Nauck, 2006, Five weeks of treatment with the GLP-1 analogue liraglutide improves glycaemic control and lowers body weight in subjects with type 2 diabetes, Experimental and Clinical Endocrinology & Diabetes, 114, 417, 10.1055/s-2006-924230 Vilsboll, 2007, Liraglutide, a long-acting human glucagon-like peptide-1 analog, given as monotherapy significantly improves glycemic control and lowers body weight without risk of hypoglycemia in patients with type 2 diabetes, Diabetes Care, 30, 1608, 10.2337/dc06-2593 Vilsboll, 2008, Liraglutide, a once-daily human GLP-1 analogue, improves pancreatic B-cell function and arginine-stimulated insulin secretion during hyperglycaemia in patients with Type 2 diabetes mellitus, Diabetic Medicine, 10.1111/j.1464-5491.2007.02333.x Degn, 2004, One week's treatment with the long-acting glucagon-like peptide 1 derivative liraglutide (NN2211) markedly improves 24-h glycemia and alpha- and beta-cell function and reduces endogenous glucose release in patients with type 2 diabetes, Diabetes, 53, 1187, 10.2337/diabetes.53.5.1187 Seino, 2008, 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 1, Diabetes Research and Clinical Practice, 81, 161, 10.1016/j.diabres.2008.03.018 Garber, 2009, 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, 10.1016/S0140-6736(08)61246-5 Marre, 2009, 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, 26, 268, 10.1111/j.1464-5491.2009.02666.x 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 Zinman, 2009, 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), Diabetes Care, 10.2337/dc08-2124 Russell-Jones, 2008, 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 7, Diabetes, 57, A159 Davies, 2008, Initiation of insulin glargine therapy in type 2 diabetes subjects suboptimally controlled on oral antidiabetic agents: results from the AT.LANTUS trial 1, Diabetes, Obesity and Metabolism, 10, 387, 10.1111/j.1463-1326.2008.00873.x Nauck, 2008, The once-daily human GLP-1 analog liraglutide substantially reduces HbA(1c) in subjects with type 2 diabetes, irrespective of HbA(1c) at baseline 18, Diabetes, 57, A594 Russell-Jones, 2008, The once-daily human GLP-1 analog liraglutide reduces body weight in subjects with type 2 diabetes, irrespective of body mass index at baseline 17, Diabetes, 57, A593 Colagiuri, 2008, The once-daily human GLP-1 analog-liraglutide reduces systolic blood pressure in patients with type 2 diabetes, Diabetes, 57, A164 Matthews, 2008, Liraglutide, a once-daily human GLP-1 analog, significantly improves beta-cell function in subjects with type 2 diabetes 6, Diabetes, 57, A150 Moreno, 2002, Renal effects of glucagon-like peptide in rats, European Journal of Pharmacology, 434, 163, 10.1016/S0014-2999(01)01542-4 Nathan, 2006, Management of hyperglycemia in type 2 diabetes: A consensus algorithm for the initiation and adjustment of therapy: a consensus statement from the American Diabetes Association and the European Association for the Study of Diabetes, Diabetes Care, 29, 1963, 10.2337/dc06-9912 Nathan, 2008, Diabetes Care, 31, 173, 10.2337/dc08-9016