Incretins: The novel therapy of type 2 diabetes

Journal of the Medical Association of Thailand

Volumn 91, Issue 6, 2008, Pages 943-954

  Thongtang, Nuntakon ^a   Sriwijitkamol, Apiradee ^a  

^a MAHIDOL UNIVERSITY   (Thailand)

Author keywords

DPP IV inhibitors; GLP 1; Incretins; Type 2 diabetes

Indexed keywords

ALBIGLUTIDE; ALOGLIPTIN; BIM 51077; CJC 1131; DENAGLIPTIN; DIPEPTIDYL PEPTIDASE IV INHIBITOR; EXENDIN 4; GLITAZONE DERIVATIVE; GLUCAGON LIKE PEPTIDE 1 DERIVATIVE; INCRETIN; INSULIN GLARGINE; LIRAGLUTIDE; METFORMIN; NN 221; PIOGLITAZONE; PLACEBO; PSN 9301; SAXAGLIPTIN; SITAGLIPTIN; SULFONYLUREA; TA 6666; VILDAGLIPTIN; ZP 10;

CLINICAL TRIAL; DIARRHEA; DRUG HALF LIFE; GASTROINTESTINAL SYMPTOM; HEADACHE; HUMAN; INFECTION; NAUSEA; NAUSEA AND VOMITING; NON INSULIN DEPENDENT DIABETES MELLITUS; NONHUMAN; PROTEIN BINDING; PROTEIN METABOLISM; PROTEIN SECRETION; REVIEW; VOMITING;

DIABETES MELLITUS, TYPE 2; DIPEPTIDYL-PEPTIDASE IV INHIBITORS; GLUCAGON-LIKE PEPTIDE 1; HUMANS; INCRETINS;

EID: 47149103357     PISSN: 01252208     EISSN: 01252208     Source Type: Journal    
DOI: None     Document Type: Review

References (72)

1. Wild S, Roglic G, Green A, Sicree R, King H. Global prevalence of diabetes: estimates for the year 2000 and projections for 2030. Diabetes Care 2004; 27: 1047-53.
2. Perley MJ, Kipnis DM. Plasma insulin responses to oral and intravenous glucose: studies in normal and diabetic sujbjects. J Clin Invest 1967; 46:1954-62.
3. 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; 50:609-13.
4. Xu G Staffers 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.
5. Perfetti R, Zhou J, Doyle ME, Egan JM. Glucagon-like peptide-1 induces cell proliferation and pancreatic-duodenum homeobox-1 expression and increases endocrine cell mass in the pancreas of old, glucose-intolerant rats. Endocrinology 2000; 141:4600-5.
6. Rouille Y, Martin S, Steiner DF. Differential processing of proglucagon by the subtilisin-like prohormone convertases PC2 and PC3 to generate either glucagon or glucagon-like peptide. J Biol Chem 1995;270:26488-96.
7. 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; 138:159-66.
8. De Leon DD, Crutchlow MF, Ham JY, Stoffers DA. Role of glucagon-like peptide-1 in the pathogenesis and treatment of diabetes mellitus. Int J Biochem Cell Biol 2006; 38:845-59.
9. Bojanowska E. Physiology and pathophysiology of glucagon-like peptide-1 (GLP-1): the role of GLP-1 in the pathogenesis of diabetes mellitus, obesity, and stress. Med Sci Monit 2005; 11: RA271-RA278.
10. Theodorakis MJ, Carlson O, Michopoulos S, Doyle ME, Juhaszova M, Petraki K, et al. Human duodenal enteroendocrine cells: source of both incretin peptides, GLP-1 and GIP. Am J Physiol Endocrinol Metab 2006; 290: E550-E559.
11. Dunning BE, Foley JE, Ahren B. Alpha cell function in health and disease: influence of glucagon-like peptide-l.Diabetologia 2005; 48:1700-13.
12. Gribble FM, Williams L, Simpson AK, Reimann F. A novel glucose-sensing mechanism contributing to glucagon-like peptide-1 secretion from the GLUTag cell line. Diabetes 2003; 52:1147-54.
13. Mojsov S, Weir GC, Habener JF. Insulinotropin: glucagon-like peptide I (7-37) co-encoded in the glucagon gene is a potent stimulator of insulin release in the perfused rat pancreas. J Clin Invest 1987; 79:616-9.
14. Ahren B. Type 2 diabetes, insulin secretion and beta-cell mass. Curr Mol Med 2005; 5:275-86.
15. 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.
16. Abraham EJ, Leech CA, Lin JC, Zulewski H, Habener JF. Insulinotropic hormone glucagon-like peptide-1 differentiation of human pancreatic islet-derived progenitor cells into insulin-producing cells. Endocrinology 2002; 143:3152-61.
17. Heller RS, Kieffer TJ, Habener JF. Insulinotropic glucagon-like peptide I receptor expression in glucagon-producing alpha-cells of the rat endocrine pancreas. Diabetes 1997;46:785-91.
18. Fehmann HC, Habener JF. Insulinotropic hormone glucagon-like peptide-I (7-37) stimulation of proinsulin gene expression and proinsulin biosynthesis in insulinoma beta TC-1 cells. Endocrinology 1992; 130:159-66.
19. 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.
20. Gutzwiller JP, Goke B, Drewe J, Hildebrand P, Ketterer S, Handschin D, et al. Glucagon-like peptide-1: a potent regulator of food intake in humans. Gut 1999; 44:81-6.
21. During MJ, Cao L, Zuzga DS, Francis JS, Fitzsimons HL, Jiao X, et al. Glucagon-like peptide-1 receptor is involved in learning and neuroprotection. Nat Med 2003; 9:1173-9.
22. Perry T, Greig NH. Enhancing central nervous system endogenous GLP-1 receptor pathways for intervention in Alzheimer's disease. Curr Alzheimer Res 2005; 2:377-85.
23. Perry T, Haughey NJ, Mattson MP, Egan JM, Greig NH. Protection and reversal of excitotoxic neuronal damage by glucagon-like peptide-1 and exendin-4. J Pharmacol Exp Ther 2002; 302:881-8.
24. Imeryuz N, Yegen BC, Bozkurt A, Coskun T, Villanueva-Penacarrillo ML, Ulusoy NB. Glucagon-like peptide-1 inhibits gastric emptying via vagal afferent-mediated central mechanisms. Am J Physiol 1997; 273: G920-G927.
25. Combettes MM. GLP-1 and type 2 diabetes: physiology and new clinical advances. Curr Opin Pharmacol 2006; 6:598-605.
26. Yu M, Moreno C, Hoagland KM, Dahly A, Ditter K, Mistry M, et al. Antihypertensive effect of glucagon-like peptide 1 in Dahl salt-sensitive rats. J Hypertens 2003; 21: 1125-35.
27. Nystrom T, Gutniak MK, Zhang Q, Zhang F, Holst JJ, Ahren B, et al. Effects of glucagon-like peptide-1 on endothelial function in type 2 diabetes patients with stable coronary artery disease. Am J Physiol Endocrinol Metab 2004; 287: E1209-E1215.
28. Nauck M, Stockmann F, Ebert R, Creutzfeldt W. Reduced incretin effect in type 2 (non-insulin-dependent) diabetes. Diabetologia 1986; 29:46-52.
29. Gautier JF, Fetita S, Sobngwi E, Salaun-Martin C. Biological actions of the incretins GIP and GLP-1 and therapeutic perspectives in patients with type 2 diabetes. Diabetes Metab 2005; 31: 233-42.
30. 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; 36:741-4.
31. Arulmozhi DK, Portha B. GLP-1 based therapy for type 2 diabetes. Eur J Pharm Sci 2006; 28:96-108.
32. Egan JM, Clocquet AR, Elahi D. The insulinotropic effect of acute exendin-4 administered to humans: comparison of nondiabetic state to type 2 diabetes. J Clin Endocrinol Metab 2002; 87:1282-90.
33. Kendall DM, Riddle MC, Rosenstock J, Zhuang D, Kim DD, Fineman MS, 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: 1083-91.
34. 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; 28:1092-100.
35. Buse JB, Henry RR, Han J, Kim DD, Fineman MS, Baron AD. Effects of exenatide (exendin-4) on glycemic control over 30 weeks in sulfonylureatreated patients with type 2 diabetes. Diabetes Care 2004; 27:2628-35.
36. Riddle MC, Henry RR, Poon TH, Zhang B, Mac SM, Holcombe JH, et al. Exenatide elicits sustained glycaemic control and progressive reduction of body weight in patients with type 2 diabetes inadequately controlled by sulphonylureas with or without metformin. Diabetes Metab Res Rev 2006; 22:483-91.
37. 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; 143:559-69.
38. Knudsen LB, Nielsen PF, Huusfeldt PO, Johansen NL, Madsen K, Pedersen FZ, et al. Potent derivatives of glucagon-like peptide-1 with pharmaco-kinetic properties suitable for once daily administration. J Med Chem 2000; 43: 1664-9.
39. Rolin B, Larsen MO, Gotfredsen CF, Deacon CF, Carr RD, Wilken M, et al. The long-acting GLP-1 derivative NN2211 ameliorates glycemia and increases beta-cell mass in diabetic mice. Am J Physiol Endocrinol Metab 2002; 283: E745-E752.
40. Sturis J, Gotfredsen CF, Romer J, Rolin B, Ribel U, Brand CL, et al. GLP-1 derivative liraglutide in rats with beta-cell deficiencies: influence of metabolic state on beta-cell mass dynamics. Br J Pharmacol 2003; 140:123-32.
41. Ribel U, Larsen MO, Rolin B, Carr RD, Wilken M, Sturis J, et al. NN2211: a long-acting glucagon-like peptide-1 derivative with anti-diabetic effects in glucose-intolerant pigs. Eur J Pharmacol 2002; 451: 217-25.
42. Madsbad S, Schmitz O, Ranstam J, Jakobsen G Matthews DR. 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 2004; 27:1335-42.
43. Ahren B, Gomis R, Standl E, Mills D, Schweizer A. Twelve- and 52-week efficacy of the dipeptidy l peptidase IV inhibitor LAF237 in metformin-treated patients with type 2 diabetes. Diabetes Care 2004; 27:2874-80.
44. Vilsboll T. Liraglutide significantly improves glycemic control, and lowers body weight without risk of either major or minor hypoglycemic episodes in subject with type 2 diabetes. Diabetes 2006; 55:27-8.
45. Harder H, Nielsen L, Tu DT, Astrup A. 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 2004; 27:1915-21.
46. Kim JG, Baggio LL, Bridon DP, Castaigne JP, Robitaille MF, Jette L, et al. Development and characterization of a glucagon-like peptide 1-albumin conjugate: the ability to activate the glucagon-like peptide 1 receptor in vivo. Diabetes 2003; 52:751-9.
47. Zander M, Christiansen A, Madsbad S, Holst JJ. Additive effects of glucagon-like peptide 1 and pioglitazone in patients with type 2 diabetes. Diabetes Care 2004; 27:1910-4.
48. Nauck MA, Meier JJ, Creutzfeldt W. Incretins and their analogues as new antidiabetic drugs. Drug News Perspect 2003; 16:413-22.
49. Grouzmann E, Comoy E, Walker P, Burnier M, Bohuon C, Waeber B, et al. Production and characterization of four anti-neuropeptide Y monoclonal antibodies. Hybridoma 1992; 11:409-24.
50. Yamamoto H, Kishi T, Lee CE, Choi BJ, Fang H, Hollenberg AN, et al. Glucagon-like peptide-1-responsive catecholamine neurons in the area postrema link peripheral glucagon-like peptide-1 with central autonomic control sites. J Neurosci 2003; 23:2939-46.
51. Misumi Y, Hayashi Y, Arakawa F, Ikehara Y Molecular cloning and sequence analysis of human dipeptidyl peptidase IV, a serine proteinase on the cell surface. Biochim Biophys Acta 1992; 1131:333-6.
52. Hopsu-Havu VK, Glenner GG A new dipeptide naphthylamidase hydrolyzing glycyl-prolyl-beta-naphthylamide. Histochemie 1966; 7:197-201.
53. Kettmann U, Humbel B, Holzhausen HJ. Ultra-structural localization of dipeptidylpeptidase IV in the glomerulum of the rat kidney. Acta Histochem 1992; 92:225-7.
54. Nausch I, Mentlein R, Heymann E. The degradation of bioactive peptides and proteins by dipeptidyl peptidase IV from human placenta. Biol Chem Hoppe Seyler 1990; 371:1113-8.
55. Marguet D, Baggio L, Kobayashi T, Bernard AM, Pierres M, Nielsen PF, et al. Enhanced insulin secretion and improved glucose tolerance in mice lacking CD26. Proc Natl Acad Sci U S A 2000; 97: 6874-9.
56. Mitani H, Takimoto M, Hughes TE, Kimura M. Dipeptidyl peptidase IV inhibition improves impaired glucose tolerance in high-fat diet-fed rats: study using a Fischer 344 rat substrain deficient in its enzyme activity. Jpn J Pharmacol 2002; 88:442-50.
57. Brandt I, Joossens J, Chen X, Maes MB, Scharpe S, De M, I, et al. Inhibition of dipeptidyl-peptidase IV catalyzed peptide truncation by Vildagliptin ((2S)-{[(3-hydroxyadamantan-1-yl)amino]acetyl}-pyrrolidine-2- carbonitrile). Biochem Pharmacol 2005; 70:13443.
58. Mari A, Sallas WM, He YL, Watson C, Ligueros-Saylan M, Dunning BE, et al. Vildagliptin, a dipeptidyl peptidase-IV inhibitor, improves model-assessed beta-cell function in patients with type 2 diabetes. J Clin Endocrinol Metab 2005; 90: 4888-94.
59. Ahren B, Landin-Olsson M, Jansson PA, Svensson M, Holmes D, Schweizer A. Inhibition of dipeptidyl peptidase-4 reduces glycemia, sustains insulin levels, and reduces glucagon levels in type 2 diabetes. J Clin Endocrinol Metab 2004; 89:2078-84.
60. Ristic S, Byiers S, Foley J, Holmes D. Improved glycaemic control with dipeptidyl peptidase-4 inhibition in patients with type 2 diabetes: vildagliptin (LAF237) dose response. Diabetes Obes Metab 2005; 7:692-8.
61. Schweizer A, Couturier A, Foley JE, Dejager S. Comparison between vildagliptin and metformin to sustain reductions in HbA(lc) over 1 year in drug-naive patients with type 2 diabetes. Diabet Med 2007; 24:955-61.
62. Rosenstock J, Baron MA, Dejager S, Mills D, Schweizer A. Comparison of vildagliptin and rosiglitazone monotherapy in patients with type 2 diabetes: a 24-week, double-blind, randomized trial. Diabetes Care 2007; 30:217-23.
63. Fonseca V, Schweizer A, Albrecht D, Baron MA, Chang I, Dejager S. Addition of vildagliptin to insulin improves glycaemic control in type 2 diabetes. Diabetologia 2007; 50:1148-55.
64. Bosi E, Camisasca RP, Collober C, Rochotte E, Garber AJ. Effects of vildagliptin on glucose control over 24 weeks in patients with type 2 diabetes inadequately controlled with metformin. Diabetes Care 2007; 30:890-5.
65. Herman GA, Stevens C, Van Dyck K, Bergman A, Yi B, De Smet M, et al. Pharmacokinefics and pharmacodynamics of sitagliptin, an inhibitor of dipeptidyl peptidase IV, in healthy subjects: results from two randomized, double-blind, placebo-controlled studies with single oral doses. Clin Pharmacol Ther 2005; 78:675-88.
66. Aschner P, Kipnes MS, Lunceford JK, Sanchez M, Mickel C, Williams-Herman DE. Effect of the dipeptidyl peptidase-4 inhibitor sitagliptin as monotherapy on glycemic control in patients with type 2 diabetes. Diabetes Care 2006; 29:2632-7.
67. Rosenstock J, Brazg R, Andryuk PJ, Lu K, Stein P. 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 2006; 28:1556-68.
68. Charbonnel B, Karasik A, Liu J, Wu M, Meininger G 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 2006; 29:2638-43.
69. Augeri DJ, Robl JA, Betebenner DA, Magnin DR, Khanna A, Robertson JG, et al. Discovery and preclinical profile of Saxagliptin (BMS-477118): a highly potent, long-acting, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes. J Med Chem 2005; 48:5025-37.
70. Holst JJ, Deacon CF. Glucagon-like peptide 1 and inhibitors of dipeptidyl peptidase IV in the treatment of type 2 diabetes mellitus. Curr Opin Pharmacol 2004; 4:589-96.
71. Lankas GR, Leiting B, Roy RS, Eiermann GJ, Beconi MG Biftu T, et al. Dipeptidyl peptidase IV inhibition for the treatment of type 2 diabetes: potential importance of selectivity over dipeptidyl peptidases 8 and 9. Diabetes 2005; 54:2988-94.
72. 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.