Role and development of GLP-1 receptor agonists in the management of diabetes

Diabetes, Metabolic Syndrome and Obesity

Volumn 2, Issue , 2009, Pages 37-49

  Chia, Chee W ^a   Egan, Josephine M ^a  

^a NATIONAL INSTITUTE ON AGING   (United States)

Author keywords

Diabetes; GLP 1; GLP 1R agonist; Incretin

Indexed keywords

ALBIGLUTIDE; ANTIDIABETIC AGENT; AVE 0010; BIPHASIC INSULIN; CJC 1134PC; EXENDIN 4; GLIMEPIRIDE; INSULIN GLARGINE; LIRAGLUTIDE; LY 2189265; LY 2428757; METFORMIN; NN 9535; ORAL ANTIDIABETIC AGENT; PIOGLITAZONE; PLACEBO; ROSIGLITAZONE; SULFONYLUREA; TASPOGLUTIDE; UNCLASSIFIED DRUG;

ACUTE HEMORRHAGIC PANCREATITIS; ADD ON THERAPY; CELL FUNCTION; CLINICAL TRIAL; CONTROLLED CLINICAL TRIAL; DRUG BLOOD LEVEL; DRUG EFFECT; DRUG EFFICACY; DRUG FORMULATION; DRUG SAFETY; DRUG TOLERABILITY; FOOD INTAKE; GASTROINTESTINAL SYMPTOM; GLUCAGON RELEASE; HEMORRHAGIC PANCREATITIS; HORMONE RELEASE; HUMAN; HYPERGLYCEMIA; HYPOGLYCEMIA; INJECTION SITE PRURITUS; INSULIN RELEASE; NAUSEA; NAUSEA AND VOMITING; NON INSULIN DEPENDENT DIABETES MELLITUS; NONHUMAN; PANCREAS ISLET BETA CELL; PANCREATITIS; RANDOMIZED CONTROLLED TRIAL; REVIEW; SATIETY; SIDE EFFECT; STOMACH EMPTYING; VOMITING; WEIGHT GAIN; WEIGHT REDUCTION;

EID: 77953423822     PISSN: None     EISSN: 11787007     Source Type: Journal    
DOI: 10.2147/dmso.s4283     Document Type: Review

References (77)

1. Elrick H, Stimmler L, Hlad CJ, Jr, Arai Y. Plasma insulin response to oral and intravenous glucose administration. J Clin Endocrinol Metab. 1964;24:1076-1082.
2. McIntyre N, Holdsworth CD, Turner DS. Intestinal factors in the control of insulin secretion. J Clin Endocrinol Metab. 1965;25(10): 1317-1324.
3. Perley MJ, Kipnis DM. Plasma insulin responses to oral and intravenous glucose: studies in normal and diabetic sujbjects. J Clin Invest. 1967;46(12):1954-1962.
4. Buffa R, Polak JM, Pearse AGE, Solcia E, Grimelius L, Capella C. Identification of the Intestinal Cell Storing Gastric Inhibitory Peptide. Histochemistry. 1975;43:249-255.
5. Orskov C, Holst JJ, Knuhtsen S, Baldissera FG, Poulsen SS, Nielsen OV. Glucagon-like peptides GLP-1 and GLP-2, predicted products of the glucagon gene, are secreted separately from pig small intestine but not pancreas. Endocrinology. 1986;119(4):1467-1475.
6. Theodorakis MJ, Carlson O, Michopoulos S, et al. Human duodenal enteroendocrine cells: source of both incretin peptides, GLP-1 and GIP. Am J Physiol Endocrinol Metab. 2006;290(3):E550-E559.
7. Eissele R, Goke R, Willemer S, et al. Glucagon-like peptide-1 cells in the gastrointestinal tract and pancreas of rat, pig and man. Eur J Clin Invest. 1992;22(4):283-291.
8. Meier JJ, Nauck MA. Glucagon-like peptide 1(GLP-1) in biology and pathology. Diabetes Metab Res Rev. 2005;21(2):91-117.
9. Krarup T, Saurbrey N, Moody AJ, Kuhl C, Madsbad S. Effect of porcine gastric inhibitory polypeptide on beta-cell function in type I and type II diabetes mellitus. Metabolism. 1987;36(7):677-682.
10. Nauck MA, Heimesaat MM, Orskov C, Holst JJ, Ebert R, Creutzfeldt W. 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(1):301-307.
11. Elahi D, McAloon-Dyke M, Fukagawa NK, et al. The insulinotropic actions of glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (7-37) in normal and diabetic subjects. Regul Pept. 14 1994;51(1):63-74.
12. Feinle C, Chapman IM, Wishart J, Horowitz M. Plasma glucagon-like peptide-1 (GLP-1) responses to duodenal fat and glucose infusions in lean and obese men. Peptides. 2002;23(8):1491-1495.
13. Jang HJ, Kokrashvili Z, Theodorakis MJ, et al. Gut-expressed gustducin and taste receptors regulate secretion of glucagon-like peptide-1. Proc Natl Acad Sci U S A. 2007;104(38):15069-15074.
14. Elliott RM, Morgan LM, Tredger JA, Deacon S, Wright J, Marks V. Glucagon-like peptide-1 (7-36)amide and glucose-dependent insulinotropic polypeptide secretion in response to nutrient ingestion in man: acute post-prandial and 24-h secretion patterns. J Endocrinol. 1993;138(1):159-166.
15. Kim W, Egan JM. The role of incretins in glucose homeostasis and diabetes treatment. Pharmacol Rev. 2008;60(4):470-512.
16. Vollmer K, Holst JJ, Baller B, et al. Predictors of incretin concentrations in subjects with normal, impaired, and diabetic glucose tolerance. Diabetes. 2008;57(3):678-687.
17. Nauck MA, Heimesaat MM, Behle K, et al. Effects of glucagon-like peptide 1 on counterregulatory hormone responses, cognitive functions, and insulin secretion during hyperinsulinemic, stepped hypoglycemic clamp experiments in healthy volunteers. J Clin Endocrinol Metab. 2002;87(3):1239-1246.
18. Toft-Nielsen MB, Damholt MB, Madsbad S, et al. Determinants of the impaired secretion of glucagon-like peptide-1 in type 2 diabetic patients. J Clin Endocrinol Metab. 2001;86(8):3717-3723.
19. Vilsboll T, Krarup T, Deacon CF, Madsbad S, Holst JJ. Reduced postprandial concentrations of intact biologically active glucagon-like peptide 1 in type 2 diabetic patients. Diabetes. 2001;50(3):609-613.
20. Kieffer TJ, McIntosh CH, Pederson RA. Degradation of glucose-dependent insulinotropic polypeptide and truncated glucagon-like peptide 1 in vitro and in vivo by dipeptidyl peptidase IV. Endocrinology. 1995;136(8):3585-3596.
21. Hupe-Sodmann K, McGregor GP, Bridenbaugh R, et al. Characterisation of the processing by human neutral endopeptidase 24.11 of GLP-1 (7-36) amide and comparison of the substrate specificity of the enzyme for other glucagon-like peptides. Regul Pept. 1995;58(3):149-156.
22. Meier JJ, Nauck MA, Kranz D, et al. Secretion, degradation, and elimination of glucagon-like peptide 1 and gastric inhibitory polypeptide in patients with chronic renal insufficiency and healthy control subjects. Diabetes. 2004;53(3):654-662.
23. Hansen L, Deacon CF, Orskov C, Holst JJ. Glucagon-like peptide-1-(7-36)amide is transformed to glucagon-like peptide-1-(9-36)amide by dipeptidyl peptidase IV in the capillaries supplying the L cells of the porcine intestine. Endocrinology. 1999;140(11): 5356-5363.
24. Ruiz-Grande C, Alarcon C, Alcantara A, et al. Renal catabolism of truncated glucagon-like peptide 1. Horm Metab Res. 1993;25(12):612-616.
25. Thorens B, Porret A, Buhler L, Deng SP, Morel P, Widmann C. Cloning and functional expression of the human islet GLP-1 receptor. Demonstration that exendin-4 is an agonist and exendin-(9-39) an antagonist of the receptor. Diabetes. 1993;42(11):1678-1682.
26. Kieffer TJ, Habener JF. The glucagon-like peptides. Endocr Rev. 1999;20(6):876-913.
27. Kjems LL, Holst JJ, Volund 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(2):380-386.
28. Rachman J, Gribble FM, Barrow BA, Levy JC, Buchanan KD, Turner RC. Normalization of insulin responses to glucose by overnight infusion of glucagon-like peptide 1 (7-36) amide in patients with NIDDM. Diabetes. 1996;45(11):1524-1530.
29. 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(9309):824-830.
30. Meneilly GS, Greig N, Tildesley H, Habener JF, Egan JM, Elahi D. Effects of 3 months of continuous subcutaneous administration of glucagon-like peptide 1 in elderly patients with type 2 diabetes. Diabetes Care. 2003;26(10):2835-2841.
31. Meneilly GS, Veldhuis JD, Elahi D. Deconvolution analysis of rapid insulin pulses before and after six weeks of continuous subcutaneous administration of glucagon-like peptide-1 in elderly patients with type 2 diabetes. J Clin Endocrinol Metab. 2005;90(11):6251-6256.
32. Nauck MA, Kleine N, Orskov C, Holst JJ, Willms B, Creutzfeldt W. Normalization of fasting hyperglycaemia by exogenous glucagon-like peptide 1 (7-36 amide) in type 2 (non-insulin-dependent) diabetic patients. Diabetologia. 1993;36(8):741-744.
33. Meier JJ, Gallwitz B, Salmen S, et al. Normalization of glucose concentrations and deceleration of gastric emptying after solid meals during intravenous glucagon-like peptide 1 in patients with type 2 diabetes. J Clin Endocrinol Metab. 2003;88(6):2719-2725.
34. Verdich C, Flint A, Gutzwiller JP, et al. A meta-analysis of the effect of glucagon-like peptide-1 (7-36) amide on ad libitum energy intake in humans. J Clin Endocrinol Metab. 2001;86(9):4382-4389.
35. Naslund E, Gutniak M, Skogar S, Rossner S, Hellstrom PM. Glucagon-like peptide 1 increases the period of postprandial satiety and slows gastric emptying in obese men. Am J Clin Nutr. 1998;68(3):525-530.
36. Brubaker PL, Drucker DJ. Minireview: Glucagon-like peptides regulate cell proliferation and apoptosis in the pancreas, gut, and central nervous system. Endocrinology. 2004;145(6):2653-2659.
37. Egan JM, Bulotta A, Hui H, Perfetti R. GLP-1 receptor agonists are growth and differentiation factors for pancreatic islet beta cells. Diabetes Metab Res Rev. 2003;19(2):115-123.
38. Byrne MM, Gliem K, Wank U, et al. Glucagon-like peptide 1 improves the ability of the beta-cell to sense and respond to glucose in subjects with impaired glucose tolerance. Diabetes. 1998;47(8):1259-1265.
39. Migoya EM, Miller J, Larson P, et al. Sitagliptin, a selective DPP-4 inhibitor, and metformin have complementary effects to increase active GLP-1 concentrations. Diabetes. 2007;56(S1):A74.
40. Green BD, Gault VA, O'Harte FP, Flatt PR. Structurally modified analogues of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP) as future antidiabetic agents. Curr Pharm Des. 2004;10(29):3651-3662.
41. Kolterman OG, Kim DD, Shen L, et al. Pharmacokinetics, pharmacodynamics, and safety of exenatide in patients with type 2 diabetes mellitus. Am J Health Syst Pharm. 2005;62(2):173-181.
42. Simonsen L, Holst JJ, Deacon CF. Exendin-4, but not glucagon-like peptide-1, is cleared exclusively by glomerular filtration in anaesthetised pigs. Diabetologia. 2006;49(4):706-712.
43. Buse JB, Henry RR, Han J, Kim DD, Fineman MS, Baron AD. Effects of exenatide (exendin-4) on glycemic control over 30 weeks in sulfonylurea-treated patients with type 2 diabetes. Diabetes Care. 2004;27(11):2628-2635.
44. DeFronzo RA, Ratner RE, Han J, Kim DD, Fineman MS, Baron AD. 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(5):1092-1100.
45. Kendall DM, Riddle MC, Rosenstock J, 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. 2005;28(5):1083-1091.
46. Klonoff DC, Buse JB, Nielsen LL, et al. 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. 2008;24(1):275-286.
47. Zinman B, Hoogwerf BJ, Duran Garcia S, et al. The effect of adding exenatide to a thiazolidinedione in suboptimally controlled type 2 diabetes: a randomized trial. Ann Intern Med. 2007;146(7):477-485.
48. Heine RJ, Van Gaal LF, Johns D, Mihm MJ, Widel MH, Brodows RG. Exenatide versus insulin glargine in patients with suboptimally controlled type 2 diabetes: a randomized trial. Ann Intern Med. 2005;143(8): 559-569.
49. Nauck MA, Meininger G, Sheng D, Terranella L, Stein PP. Efficacy and safety of the dipeptidyl peptidase-4 inhibitor, sitagliptin, compared with the sulfonylurea, glipizide, in patients with type 2 diabetes inadequately controlled on metformin alone: a randomized, double-blind, non-inferiority trial. Diabetes Obes Metab. 2007;9(2):194-205.
50. Moretto TJ, Milton DR, Ridge TD, et al. Efficacy and tolerability of exenatide monotherapy over 24 weeks in antidiabetic drug-naive patients with type 2 diabetes: a randomized, double-blind, placebo-controlled, parallel-group study. Clin Ther. 2008;30(8):1448-1460.
51. Eli Lilly and Company. Amylin, Lilly Update on FDA Review of Byetta (exenatide) Injection Monotherapy Submission. 2008. Accessed February 17, 2009. Available from: http://newsroom.lilly.com/releasedetail.cfm?releaseid=352884.
52. Amori RE, Lau J, Pittas AG. Efficacy and safety of incretin therapy in type 2 diabetes: systematic review and meta-analysis. JAMA. 2007;298(2):194-206.
53. Bain SC, Stephens JW. Exenatide and pancreatitis: an update. Expert Opin Drug Saf. 2008;7(6):643-644.
54. Fehse F, Trautmann M, Holst JJ, et al. Exenatide augments first-and second-phase insulin secretion in response to intravenous glucose in subjects with type 2 diabetes. J Clin Endocrinol Metab. 2005;90(11):5991-5997.
55. Mari A, Nielsen LL, Nanayakkara N, DeFronzo RA, Ferrannini E, Halseth A. Mathematical modeling shows exenatide improved beta-cell function in patients with type 2 diabetes treated with metformin or metformin and a sulfonylurea. Horm Metab Res. 2006;38(12):838-844.
56. Bunck MC, Diamant M, Corner A, et al. One-year treatment with exenatide improves beta-cell function, compared to insulin glargine, in metformin treated type 2 diabetes patients: A randomized, controlled trial. Diabetes Care. 2009 Feb 5. [Epub ahead of print]
57. Knudsen LB, Knudsen SM, Wilken M, et al. Plasma protein binding of NN2211, a long-acting derivative of GLP-1, is important for its efficacy. Diabetes. 2003;52(Suppl 1):A321-A322.
58. Knudsen LB, Nielsen PF, Huusfeldt PO, et al. Potent derivatives of glucagon-like peptide-1 with pharmacokinetic properties suitable for once daily administration. J Med Chem. 2000;43(9):1664-1669.
59. Agerso H, Jensen LB, Elbrond B, Rolan P, Zdravkovic M. The pharmacokinetics, pharmacodynamics, safety and tolerability of NN2211, a new long-acting GLP-1 derivative, in healthy men. Diabetologia. 2002;45(2):195-202.
60. Garber A, Henry R, Ratner R, 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. 2009;373(9662):473-481.
61. Nauck M, Frid A, Hermansen K, et al. 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(1):84-90.
62. Marre M, Shaw J, Brandle M, et al. Liraglutide, a once-daily human GLP-1 analog, added to a sulfonylurea (SU) offers significantly better glycemic control and favorable weight change compared with rosiglitazone and SU combination therapy in subjects with type 2 diabetes. Abstract presented at San Francisco, CA: American Diabetes Association 68th Scientific Sessions, 2008.
63. Russell-Jones D, Vaag A, Schmitz O, 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. Abstract presented at San Francisco, CA: American Diabetes Association 68th Scientific Sessions; June 6-10, 2008.
64. Chang AM, Jakobsen G, Sturis J, et al. The GLP-1 derivative NN2211 restores beta-cell sensitivity to glucose in type 2 diabetic patients after a single dose. Diabetes. 2003;52(7):1786-1791.
65. Mari A, Degn K, Brock B, Rungby J, Ferrannini E, Schmitz O. Effects of the long-acting human glucagon-like peptide-1 analog liraglutide on beta-cell function in normal living conditions. Diabetes Care. 2007;30(8):2032- 2033.
66. Degn KB, Juhl CB, Sturis J, et al. 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. 2004;53(5):1187-1194.
67. Drucker DJ, Buse JB, Taylor K, et al. Exenatide once weekly versus twice daily for the treatment of type 2 diabetes: a randomised, open-label, non-inferiority study. Lancet. 2008;372(9645):1240-1250.
68. Kim D, MacConell L, Zhuang 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. 2007;30(6):1487-1493.
69. Eli Lilly. Eli Lilly Investment community Update. December 11, 2008. Accessed on: March 10, 2009. Available from: http://files.shareholder.com/ downloads/LLY/544477551x0x258459/5acdc123-b0e7-498c-ab5c-92c599f205f2/ Eli%20Lilly%2012-11-08.pdf.
70. 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(4):1137-1147.
71. ConjuChem. PD-DACTM: Exendin-4 (CJC-1145-PC). 2009. Accessed February 7, 2009. Available from: http://www.conjuchem.com/.
72. GlaxoSmithKline. GSK initiates phase III programme for novel type 2 diabetes medication, Syncria® (albiglutide). February 17, 2009. Accessed March 31, 2009. Available from: http://us.gsk.com/html/media-news/pressreleases/ 2009/2009-pressrelease-10025.htm.
73. Novo Nordisk. Once-weekly GLP-1 analogue (NN9535). 2009. Accessed March 7, 2009. Available from: http://www.novonordisk.com/science/pipeline/rd- pipeline.asp?showid=10.
74. F-Hoffmann-La Roche Ltd. Roche moves investigational diabetes drug, Taspoglutide, into Phase III clinical trials. June 10, 2008. Accessed March 28, 2009. Available from: http://www.roche.com/med-cor-2008-06-10-e.pdf.
75. Sanofi-Aventis. New diabetes compound AVE0010 showed clear dose response results with once-a-day injection in phase IIb study. June 7, 2008. Accessed March 28, 2009. Available from: http://se.sanofi-aventis.com/live/se/sv/layout. jsp?cnt=A920FF21-6EA2-42A0-80BE-E242E4D1E088.
76. Merrion Pharmaceuticals. Merrion announces license agreement with Novo Nordisk to develop oral formulation of GLP-1 receptor agonist(s). January 16, 2009. Accessed January 16, 2009. Available from: http://www.merrionpharma.com/ archive/Merrion-NN-GLP-1.pdf.
77. Nauck MA, Duran S, Kim D, 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. 2007;50(2):259-267.