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Emerging GLP-1 receptor agonists

, MD, , MD PhD & , MD DMSc
Pages 607-618 | Published online: 09 Sep 2011

Bibliography

  • Holst JJ. The physiology of glucagon-like peptide 1. Physiol Rev 2007;87:1409-39
  • Doyle ME, Egan JM. Mechanisms of action of glucagon-like peptide 1 in the pancreas. Pharmacol Ther 2007;113:546-93
  • Kjems LL, Holst JJ, Vølund A, Madsbad S. The influence of GLP-1 on glucose-stimulated insulin secretion: effects on beta-cell sensitivity in type 2 and nondiabetic subjects. Diabetes 2003;52:380-6
  • Nauck MA, Heimesaat MM, Orskov C, 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 1993;91:301-7
  • Vilsboll T, Krarup T, Madsbad S, Holst JJ. Defective amplification of the late phase insulin response to glucose by GIP in obese type II diabetic patients. Diabetologia 2002;45:1111-19
  • Holz GG. Epac: A new cAMP-binding protein in support of glucagon-like peptide-1 receptor-mediated signal transduction in the pancreatic beta-cell. Diabetes 2004;53:5-13
  • Renstrom E, Eliasson L, Rorsman P. Protein kinase A-dependent and -independent stimulation of exocytosis by cAMP in mouse pancreatic B-cells. J Physiol (Lond) 1997;502(Pt 1):105-18
  • Shibasaki T, Takahashi H, Miki T, Essential role of Epac2/Rap1 signaling in regulation of insulin granule dynamics by cAMP. Proc Natl Acad Sci USA 2007;104:19333-8
  • Xu G, Stoffers DA, Habener JF, Bonner-Weir S. Exendin-4 stimulates both beta-cell replication and neogenesis, resulting in increased beta-cell mass and improved glucose tolerance in diabetic rats. Diabetes 1999;48:2270-6
  • Stoffers DA, Kieffer TJ, Hussain MA, Insulinotropic glucagon-like peptide 1 agonists stimulate expression of homeodomain protein IDX-1 and increase islet size in mouse pancreas. Diabetes 2000;49:741-8
  • Zhou J, Wang X, Pineyro MA, Egan JM. Glucagon-like peptide 1 and exendin-4 convert pancreatic AR42J cells into glucagon- and insulin-producing cells. Diabetes 1999;48:2358-66
  • Buteau J, El-Assaad W, Rhodes CJ, Glucagon-like peptide-1 prevents beta cell glucolipotoxicity. Diabetologia 2004;47:806-15
  • Larsson H, Holst JJ, Ahren B. Glucagon-like peptide-1 reduces hepatic glucose production indirectly through insulin and glucagon in humans. Acta Physiol Scand 1997;160:413-22
  • Willms B, Werner J, Holst JJ, Gastric emptying, glucose responses, and insulin secretion after a liquid test meal: effects of exogenous glucagon-like peptide-1 (GLP-1)-(7-36) amide in type 2 (noninsulin-dependent) diabetic patients. J Clin Endocrinol Metab 1996;81:327-32
  • Flint A, Raben A, Astrup A, Holst JJ. Glucagon-like peptide 1 promotes satiety and suppresses energy intake in humans. J Clin Invest 1998;101:515-20
  • Zander M, Madsbad S, Madsen JL, Holst JJ. 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 2002;359:824-30
  • Deacon CF, Johnsen AH, Holst JJ. 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 1995;80:952-7
  • Vilsboll T, Agerso H, Krarup T, Holst JJ. Similar elimination rates of glucagon-like peptide-1 in obese type 2 diabetic patients and healthy subjects. J Clin Endocrinol Metab 2003;88:220-4
  • Zhang P, Zhang X, Brown J, Global healthcare expenditure on diabetes for 2010 and 2030. Diabetes Res Clin Pract 2010;87:293-301
  • Farag YMK, Gaballa MR. Diabesity: an overview of a rising epidemic. Nephrol Dial Transplant 2011;26:28-35
  • UK Prospective Diabetes Study (UKPDS) Group. Intensive blood-glucose control with sulphonylureas or insulin compared with conventional treatment and risk of complications in patients with type 2 diabetes (UKPDS 33). Lancet 1998;352:837-53
  • Holman RR, Paul SK, Bethel MA, 10-year follow-up of intensive glucose control in type 2 diabetes. N Engl J Med 2008;359:1577-89
  • Gakidou E, Mallinger L, Abbott-Klafter J, Management of diabetes and associated cardiovascular risk factors in seven countries: a comparison of data from national health examination surveys. Bull World Health Organ 2011;89:172-83
  • Carver C. Insulin treatment and the problem of weight gain in type 2 diabetes. Diabetes Educ 2006;32:910-17
  • Korytkowski M. When oral agents fail: practical barriers to starting insulin. Int J Obes Relat Metab Disord 2002;26(Suppl 3):S18-24
  • Blonde L. Current antihyperglycemic treatment guidelines and algorithms for patients with type 2 diabetes mellitus. Am J Med 2010;123:S12-18
  • UK Prospective Diabetes Study (UKPDS) Group. Effect of intensive blood-glucose control with metformin on complications in overweight patients with type 2 diabetes (UKPDS 34). Lancet 1998;352:854-65
  • Nathan DM, Buse JB, Davidson MB, 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 2006;29:1963-72
  • Nathan DM, Buse JB, Davidson MB, Medical management of hyperglycemia in type 2 diabetes: a consensus algorithm for the initiation and adjustment of therapy: a consensus statement of the American Diabetes Association and the European Association for the Study of Diabetes. Diabetes Care 2009;32:193-203
  • Riddle MC. Therapy: what evidence should guide the use of thiazolidinediones? Nat Rev Endocrinol 2010;6:600-2
  • Lovshin JA, Drucker DJ. Incretin-based therapies for type 2 diabetes mellitus. Nat Rev Endocrinol 2009;5:262-9
  • Eng J, Kleinman WA, Singh L, 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. J Biol Chem 1992;267:7402-5
  • Linnebjerg H, Kothare PA, Park S, Effect of renal impairment on the pharmacokinetics of exenatide. Br J Clin Pharmacol 2007;64:317-27
  • Buse JB, Rosenstock J, Sesti G, Liraglutide once a day versus exenatide twice a day for type 2 diabetes: a 26-week randomised, parallel-group, multinational, open-label trial (LEAD-6). Lancet 2009;374:39-47
  • Buse JB, Henry RR, Han J, Effects of exenatide (exendin-4) on glycemic control over 30 weeks in sulfonylurea-treated patients with type 2 diabetes. Diabetes Care 2004;27:2628-35
  • Kendall DM, Riddle MC, Rosenstock J, 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 2005;28:1083-91
  • DeFronzo RA, Ratner RE, Han J, Effects of exenatide (exendin-4) on glycemic control and weight over 30 weeks in metformin-treated patients with type 2 diabetes. Diabetes Care 2005;28:1092-100
  • Madsbad S, Krarup T, Deacon CF, Holst JJ. Glucagon-like peptide receptor agonists and dipeptidyl peptidase-4 inhibitors in the treatment of diabetes: a review of clinical trials. Curr Opin Clin Nutr Metab Care 2008;11:491-9
  • Okerson T, Yan P, Stonehouse A, Brodows R. Effects of exenatide on systolic blood pressure in subjects with type 2 diabetes. Am J Hypertens 2010;23:334-9
  • Best JH, Hoogwerf BJ, Herman WH, Risk of cardiovascular disease events in patients with type 2 diabetes prescribed the glucagon-like peptide 1 (GLP-1) receptor agonist exenatide twice daily or other glucose-lowering therapies: a retrospective analysis of the LifeLink database. Diabetes Care 2011;34:90-5
  • Neumiller JJ, Sonnett TE, Wood LD, Pharmacology, efficacy and safety of liraglutide in the management of type 2 diabetes. Diabetes Metab Syndr Obes 2010;3:215-26
  • Madsbad S. Exenatide and liraglutide: different approaches to develop GLP-1 receptor agonists (incretin mimetics)–preclinical and clinical results. Best Pract Res Clin Endocrinol Metab 2009;23:463-77
  • Joffe D. Liraglutide: a once-daily human glucagon-like peptide-1 analogue for type 2 diabetes mellitus. Am J Health Syst Pharm 2010;67:1326-36
  • Marre M, Shaw J, Brandle M, 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). Diabet Med 2009;26:268-78
  • Russell-Jones D, Vaag A, Schmitz O, Liraglutide vs insulin glargine and placebo in combination with metformin and sulfonylurea therapy in type 2 diabetes mellitus (LEAD-5 met+SU): a randomised controlled trial. Diabetologia 2009;52:2046-55
  • Garber A, Henry R, Ratner R, Liraglutide versus glimepiride monotherapy for type 2 diabetes (LEAD-3 Mono): a randomised, 52-week, phase III, double-blind, parallel-treatment trial. Lancet 2009;373:473-81
  • Buse JB, Rosenstock J, Sesti G, Liraglutide once a day versus exenatide twice a day for type 2 diabetes: a 26-week randomised, parallel-group, multinational, open-label trial (LEAD-6). Lancet 2009;374:39-47
  • Zinman B, Gerich J, Buse JB, Efficacy and safety of the human glucagon-like peptide-1 analog liraglutide in combination with metformin and thiazolidinedione in patients with type 2 diabetes (LEAD-4 Met+TZD). Diabetes Care 2009;32:1224-30
  • Nauck M, Frid A, Hermansen K, 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 2009;32:84-90
  • Buse JB, Sesti G, Schmidt WE, Switching to once-daily liraglutide from twice-daily exenatide further improves glycemic control in patients with type 2 diabetes using oral agents. Diabetes Care 2010;33:1300-3
  • Amori RE, Lau J, Pittas AG. Efficacy and safety of incretin therapy in type 2 diabetes: systematic review and meta-analysis. JAMA 2007;298:194-206
  • Ahren B. GLP-1 for type 2 diabetes. Exp Cell Res 2011;317:1239-45
  • Blonde L, Russell-Jones D. The safety and efficacy of liraglutide with or without oral antidiabetic drug therapy in type 2 diabetes: an overview of the LEAD 1-5 studies. Diabetes Obes Metab 2009;11(Suppl 3):26-34
  • Byetta: scientific discussion. European Medicines Agency - EPARs for authorised medicinal products for human use. Available from: http://www.ema.europa.eu/ema/index.jsp?curl=search.jsp&q=byetta%3A+scientific+discussion+&btnG=Search&murl=menus%2Fmedicines%2Fmedicines.jsp&mid=WC0b01ac058001d125 [Last accessed 13 April 2011]
  • Anderson SL, Trujillo JM. Association of pancreatitis with glucagon-like peptide-1 agonist use. Ann Pharmacother 2010;44:904-9
  • Noel RA, Braun DK, Patterson RE, Bloomgren GL. Increased risk of acute pancreatitis and biliary disease observed in patients with type 2 diabetes: a retrospective cohort study. Diabetes Care 2009;32:834-8
  • Elashoff M, Matveyenko AV, Gier B, Pancreatitis, pancreatic, and thyroid cancer with glucagon-like Peptide-1-based therapies. Gastroenterology 2011;141:150-6
  • Aus der UAW-Datenbank. Pankreaskarzinome im Zusammenhang mit Exenatid (Byetta®) (Aus der UAW-Datenbank). 2011. Available from: http://www.akdae.de/Arzneimittelsicherheit/Bekanntgaben/20110513.html [Last accessed 1 August 2011]
  • European Medicine Agency. Anti diabetic drugs: Cardio/cerebrovascular adverse effect and pancreatitis/pancreatic cancer. Available from: http://www.ema.europa.eu/ema/index.jsp?curl=search.jsp&site=pfoi_collection&entsp=0&sort=date:D:L:d1&client=pfoi_frontend&curl=search.jsp&curl=search.jsp&btnG=Search&entqr=0&access=p&ip=172.16.100.1&oe=UTF-8&proxyreload=1&q=GLP-1+pancreatic+cancer&ie=UTF-8&ud=1&mid=&murl=menus/special_topics/special_topics.jsp&output=xml_no_dtd&proxystylesheet=pfoi_frontend&filter=0&filter=0&start=0 [Last accessed 1 August 2011]
  • FDA. Briefing materials: liraglutide. Available from: http://www.fda.gov/ohrms/dockets/ac/09/briefing/2009-4422b2-01-FDA.pdf [Last accessed 12 April 2011]
  • Bjerre Knudsen L, Madsen LW, Andersen S, Glucagon-like Peptide-1 receptor agonists activate rodent thyroid C-cells causing calcitonin release and C-cell proliferation. Endocrinology 2010;151:1473-86
  • Rosenstock J, Reusch J, Bush M, Potential of albiglutide, a long-acting GLP-1 receptor agonist, in type 2 diabetes: a randomized controlled trial exploring weekly, biweekly, and monthly dosing. Diabetes Care 2009;32:1880-6
  • Verspohl EJ. Novel therapeutics for type 2 diabetes: incretin hormone mimetics (glucagon-like peptide-1 receptor agonists) and dipeptidyl peptidase-4 inhibitors. Pharmacol Ther 2009;124:113-38
  • Bergenstal RM, Wysham C, Macconell L, Efficacy and safety of exenatide once weekly versus sitagliptin or pioglitazone as an adjunct to metformin for treatment of type 2 diabetes (DURATION-2): a randomised trial. Lancet 2010;376:431-9
  • Diamant M, Van Gaal L, Stranks S, Once weekly exenatide compared with insulin glargine titrated to target in patients with type 2 diabetes (DURATION-3): an open-label randomised trial. Lancet 2010;375:2234-43
  • Amylin Pharmaceuticals, Inc. Press-Release: duration-4 study results: Bydureon Efficacy and Tolerability Extended to Monotherapy Treatment. Available from: http://phx.corporate-ir.net/phoenix.zhtml?c=101911&p=irol-newsArticle&ID=1438147&highlight= [Last accessed 8 April 2011]
  • Blevins T, Pullman J, Malloy J, DURATION-5: exenatide once weekly resulted in greater improvements in Glycemic control compared with exenatide twice daily in patients with type 2 diabetes. J Clin Endocrinol Metab 2011; Available from: http://www.ncbi.nlm.nih.gov/pubmed/21307137 [Last accessed 28 March 2011]
  • Amylin Pharmaceuticals, Inc. Press-Release: Duration-6 Top-Line Study Results Announced. Available from: http://phx.corporate-ir.net/phoenix.zhtml?c=101911&p=irol-newsArticle&ID=1535419&highlight= [Last accessed 8 April 2011]
  • Drucker DJ, Buse JB, Taylor K, Exenatide once weekly versus twice daily for the treatment of type 2 diabetes: a randomised, open-label, non-inferiority study. Lancet 2008;372:1240-50
  • Buse JB, Drucker DJ, Taylor KL, DURATION-1: exenatide once weekly produces sustained glycemic control and weight loss over 52 weeks. Diabetes Care 2010;33:1255-61
  • Bruce S, Han J, Brown C, Safety and tolerability of exenatide once weekly pooled summary of 1095 patients from DURATION-1, 2, and 3. Diabetes 2010;59:A16-17
  • Linnebjerg H, Seger M, Kothare P, The effect of exonatide on QTc interval in healthy subjects. Diabetes 2009;58:A161-1
  • Idris I. FDA Request further studies on the once weekly exenatide, bydureon. Diabetes Obes Metab 2011;13:94-4
  • Christensen M, Knop FK, Vilsboll T, Holst JJ. Lixisenatide for type 2 diabetes mellitus. Expert Opin Investig Drugs 2011;20:549-57
  • Thorkildsen C, Neve S, Larsen BD, Glucagon-like peptide 1 receptor agonist ZP10A increases insulin mRNA expression and prevents diabetic progression in db/db mice. J Pharmacol Exp Ther 2003;307:490-6
  • Distiller L, Ruus P. Pharmacokinetics and pharmacodynamics of GLP-1 agonist AVE0010 in type 2 diabetes patients. Diabetes 2008;57:A154-5
  • Liu Y, Ruus P. Pharmacokinetics and Safety of the GLP-1 Agonist AVE0010 in patients with renal impairment. Diabetes 2009;58:A149-50
  • Gerich J, Fonseca V, Alvarado-Ruiz R, Monotherapy with GLP-1 receptor agonist, Lixisenatide, significantly improves glycaemic control in type 2 diabetic patients. Diabetologia 2010;53:830
  • Ratner RE, Rosenstock J, Boka G. Dose-dependent effects of the once-daily GLP-1 receptor agonist lixisenatide in patients with type 2 diabetes inadequately controlled with metformin: a randomized, double-blind, placebo-controlled trial. Diabetes Med 2010;27:1024-32
  • Christensen M, Knop FK, Holst JJ, Vilsboll T. Lixisenatide, a novel GLP-1 receptor agonist for the treatment of type 2 diabetes mellitus. IDrugs 2009;12:503-13
  • Sanofi-Aventis. Press-Release: Sanofi-Aventis Announces positive top-line lixisenatide phase III results. Available from: http://en.sanofi-aventis.com/press/press_releases/2011/news_list_2011.asp [Last accessed 8 April 2011]
  • Baggio LL, Huang Q, Cao X, Drucker DJ. An albumin-exendin-4 conjugate engages central and peripheral circuits regulating murine energy and glucose homeostasis. Gastroenterology 2008;134:1137-47
  • Wang M, Kipnes M, Matheson S, Safety and pharmacodynamics of CJC-1134-PC, a novel GLP-1 receptor agonist, in patients with type 2 diabetes mellitus: a randomized, placebo-controlled, double-blind, dose-escalation study. Diabetes 2007;56:A133-3
  • Wang M, Matheson S, Picard J, PC-DAC (TM): Exendin-4 (CJC-1134-PC) significantly reduces hba1c and body weight as an adjunct therapy to metformin: Two randomized, double-blind, placebo-controlled, 12 week, phase ii studies in patients with type 2 diabetes mellitus. Diabetes 2009;58:A148-8
  • St Onge EL, Miller SA. Albiglutide: a new GLP-1 analog for the treatment of type 2 diabetes. Expert Opin Biol Ther 2010;10:801-6
  • Bush MA, Matthews JE, De Boever EH, Safety, tolerability, pharmacodynamics and pharmacokinetics of albiglutide, a long-acting glucagon-like peptide-1 mimetic, in healthy subjects. Diabetes Obes Metab 2009;11:498-505
  • Matthews JE, Stewart MW, De Boever EH, Pharmacodynamics, pharmacokinetics, safety, and tolerability of albiglutide, a long-acting glucagon-like peptide-1 mimetic, in patients with type 2 diabetes. J Clin Endocrinol Metab 2008;93:4810-17
  • Seino Y, Nakajima H, Miyahara H, Safety, tolerability, pharmacokinetics and pharmacodynamics of albiglutide, a long-acting GLP-1-receptor agonist, in Japanese subjects with type 2 diabetes mellitus. Curr Med Res Opin 2009;25:3049-57
  • Glaesner W, Vick AM, Millican R, Engineering and characterization of the long-acting glucagon-like peptide-1 analogue LY2189265, an Fc fusion protein. Diabetes Metab Res Rev 2010;26:287-96
  • Barrington P, Chien JY, Showalter HDH, A 5-week study of the pharmacokinetics and pharmacodynamics of LY2189265, a novel, long-acting glucagon-like peptide-1 analog, in patients with type 2 diabetes. Diabetes Obes Metab 2011; Available from: http://www.ncbi.nlm.nih.gov/pubmed/21251178 [Last accessed 1 Februar 2011]
  • Barrington P, Chien JY, Tibaldi F, LY2189265, a long-acting glucagon like-peptide-1 analog, demonstrated dose-dependent insulin secretion in healthy subjects. Diabetes Obes Metab 2011;13:343-438
  • Umpierrez GE, Blevins T, Rosenstock J, The effects of LY2189265, a long-acting glucagon-like peptide-1 analog, in a randomized, placebo-controlled, double-blind study of overweight/obese patients with type 2 diabetes: the EGO study. Diabetes Obes Metab 2011; Available from: http://www.ncbi.nlm.nih.gov/pubmed/21251180 [Last accessed 1 February 2011]
  • Schernthaner G, Barnett AH, Betteridge DJ, Is the ADA/EASD algorithm for the management of type 2 diabetes (January 2009) based on evidence or opinion? A critical analysis. Diabetologia 2010;53:1258-69

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