DPP-4 inhibition and islet function

Journal of Diabetes Investigation

Volumn 3, Issue 1, 2012, Pages 3-10

  Ahrén, Bo ^a  

^a LUND UNIVERSITY   (Sweden)

Author keywords

Dipeptidyl peptidase 4 inhibition; Glucagon secretion; Insulin secretion

Indexed keywords

2,4 THIAZOLIDINEDIONE DERIVATIVE; 6 [[2 [[2 (2 CYANO 1 PYRROLIDINYL) 2 OXOETHYL]AMINO]ETHYL]AMINO]NICOTINONITRILE; ALOGLIPTIN; DIPEPTIDYL PEPTIDASE IV; DIPEPTIDYL PEPTIDASE IV INHIBITOR; GLIPIZIDE; GLUCAGON; GLUCAGON LIKE PEPTIDE 1; HEMOGLOBIN A1C; INSULIN; ISOLEUCINE THIAZOLIDIDE; LINAGLIPTIN; METFORMIN; PLACEBO; SAXAGLIPTIN; SITAGLIPTIN; SULFONYLUREA DERIVATIVE; VALINE PYRROLIDIDE; VILDAGLIPTIN;

COMBINATION CHEMOTHERAPY; DIABETES MELLITUS; GLUCAGON RELEASE; GLUCOSE TOLERANCE; GLYCEMIC CONTROL; HUMAN; HYPOGLYCEMIA; INSULIN RELEASE; INSULIN RESISTANCE; LIPID DIET; LONG TERM CARE; LOW DRUG DOSE; MONOTHERAPY; NON INSULIN DEPENDENT DIABETES MELLITUS; NONHUMAN; PANCREAS ISLET BETA CELL; PANCREAS ISLET BETA CELL MASS; PANCREAS ISLET CELL FUNCTION; PRIORITY JOURNAL; REVIEW; SIDE EFFECT; STREPTOZOCIN DIABETES; WEIGHT GAIN;

EID: 84857226676     PISSN: 20401116     EISSN: 20401124     Source Type: Journal    
DOI: 10.1111/j.2040-1124.2011.00184.x     Document Type: Review

References (61)

1. Gutniak M, Ørskov C, Holst JJ, et al. Antidiabetic effect of glucagon-like peptide-1 (7-36) amide in normal subjects and patients with diabetes mellitus. N Engl J Med 1992; 326: 1316-1322.
2. Drucker DJ, Nauck MA. The incretin system: glucagon-like peptide-1 receptor agonists and dipeptidyl peptidase-4 inhibitors in type 2 diabetes. Lancet 2006; 368: 1696-1705.
3. Ahrén B. GLP-1 for type 2 diabetes. Exp Cell Res 2011; 317: 1239-1245.
4. Piya MK, Tahrani AA, Barnett AH. Emerging treatment options for type 2 diabetes. Br J Clin Pharmacol 2010; 70: 631-644.
5. Ahrén B, Foley JE. The islet enhancer vildagliptin: mechanisms of improved glucose metabolism. Int J Clin Pract 2008; 62: 159.
6. Doyle ME, Egan JM. Mechanisms of action of glucagon-like peptide 1 in the pancreas. Pharmacol Ther 2007; 113: 549-593.
7. Drucker DJ. Glucagon-like peptide-1 and the islet β-cell: augmentation of cell proliferation and inhibition of apoptosis. Endocrinology 2003; 144: 5145-5148.
8. Perfetti R, Hui H. The role of GLP-1 in the life and death of pancreatic beta cells. Horm Metab Res 2004; 36: 804-810.
9. Dunning BE, Foley J, Ahrén B. Alpha-cell function in health and disease: influence of GLP-1. Diabetologia 2005; 48: 1700-1713.
10. Ahrén B. Type 2 diabetes, insulin secretion and beta-cell mass. Curr Mol Med 2005; 5: 275-286.
11. Ahrén B, Simonsson E, Larsson H. Inhibition of dipeptidyl peptidase IV improves metabolic control over a 4 week study period in type 2 diabetes. Diabetes Care 2002; 25: 869-875.
12. Ahrén B. Vildagliptin: an inhibitor of dipeptidyl peptidase-4 with antidiabetic properties. Exp Opin Invest Drugs 2006; 15: 431-442.
13. Ahrén B. Use of DPP-4 inhibitors in type 2 diabetes - Focus on sitagliptin. Diabetes Metab Syndr Obes 2010; 3: 31-41.
14. Deacon CF, Holst JJ. Saxagliptin: a new dipeptidyl peptidase-4 inhibitor for the treatment of type 2 diabetes. Adv Ther 2009; 26: 488-499.
15. Deacon CF, Holst JJ. Linagliptin, a xanthine-based dipeptidyl peptidase-4 inhibitor with an unusual profile for the treatment of type 2 diabetes. Exp Opin Invest Drugs 2010; 19: 133-140.
16. Pratley RP. Alogliptin: a new, highly selective dipeptidyl peptidase-4 inhibitor for the treatment of type 2 diabetes. Exp Opin Pharmacother 2009; 20: 503-512.
17. Deacon CF. Dipeptidyl peptidase-4 inhibitors in the treatment of type 2 diabetes: a comparative review. Diabetes Obes Metab 2011; 13: 7-18.
18. Pederson RA, White HA, Schlenzig D, et al. Improved glucose tolerance in Zucker fatty rats by oral administration of the dipeptidyl peptidase IV inhibitor isoleucine thiazolidide. Diabetes 1998; 47: 1253-1258.
19. Balkan B, Kwasnik L, Miserendino R, et al. Inhibition of dipeptidyl peptidase IV with NVP-DPP728 increases plasma GLP-1 (7-36 amide) concentrations and improves oral glucose tolerance in obese Zucker rats. Diabetologia 1999; 42: 1324-1331.
20. Ahrén B, Holst JJ, Mårtensson H, et al. Improved glucose tolerance and insulin secretion by inhibition of dipeptidyl peptidase IV in mice. Eur J Pharmacol 2000; 404: 239-245.
21. Sörhede Winzell M, Ahrén B. The high-fat diet-fed mouse: a model for studying mechanisms and treatment of impaired glucose tolerance and type 2 diabetes. Diabetes 2004; 53 (suppl 3): S215-S219.
22. Mu J, Petrov A, Eiermann GJ, et al. Inhibition of DPP-4 with sitagliptin improves glycemic control and restores islet cell mass and function in a rodent model of type 2 diabetes. Eur J Pharmacol 2009; 623: 148-154.
23. Thomas L, Eckhardt M, Langkopf E, et al. (R)-8-(3-amino-piperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3, 7-dihydro-purine-2, 6-dione (BI 1356), a novel xanthine-based dipeptidyl peptidase 4 inhibitor, has a superior potency and longer duration of action compared with other dipeptidyl peptidase-4 inhibitors. J Pharmacol Exptl Ther 2008; 325: 175-182.
24. Simonsson E, Ahrén B. Potentiated beta-cell response to non-glucose stimuli in insulin-resistant C57BL/6J mice. Eur J Pharmacol 1999; 350: 243-250.
25. Mari A, Sallas WM, He YL, et al. Vildagliptin, a dipeptidyl peptidase-IV inhibitor, improves model-assessed beta-cell function in patients with type 2 diabetes. J Clin Endocrinol 2005; 90: 4888-4894.
26. Lambeir AM, Durinx C, Proost P, et al. Kinetic study of the processing by dipeptidyl-peptidase IV/CD26 of neuropeptides involved in pancreatic insulin secretion. FEBS Lett 2001; 507: 327-330.
27. Ahrén B, Hughes TE. Inhibition of dipeptidyl peptidase-4 augments insulin secretion in response to exogenously administered glucagon-like peptide-1, glucose-dependent insulinotropic polypeptide, pituitary adenylate cyclase-activating polypeptide, and gastrin-releasing peptide in mice. Endocrinology 2005; 146: 2055-2059.
28. Hansotia T, Baggio LL, Delmeire D, 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 2004; 53: 1326-1335.
29. Waget A, Cabou C, Masseboeuf M, et al. Physiological and pharmacological mechanisms through which the DPP-4 inhibitor sitagliptin regulates glycemia in mice. Endocrinology 2011; 152: 3018-3029.
30. Balkan B, Li X. Portal GLP-1 administration in rats augments the insulin response to glucose via neuronal mechanisms. Am J Physiol Regul Integr Comp Physiol 2000; 279: R1449-R1454.
31. Ahrén B. Sensory nerves contribute to insulin secretion by glucagon-like peptide-1 in mice. Am J Physiol Regul Integr Comp Physiol 2004; 286: R269-R272.
32. Holst JJ, Deacon CF. Glucagon-like peptide-1 mediates the therapeutic actions of DPP-IV inhibitors. Diabetologia 2005; 48: 612-615.
33. Ahrén B, Sörhede Winzell M, Burkey B, et al. Beta-cell expression of a dominant-negative HNF-1alpha compromises the ability of inhibition of dipeptidyl peptidase-4 to elicit a long-term augmentation of insulin secretion in mice. Eur J Pharmacol 2005; 521: 164-168.
34. Reimer MK, Holst JJ, Ahrén B. Long-term inhibition of dipeptidyl peptidase IV improves glucose tolerance and preserves islet function in mice. Eur J Endocrinol 2002; 146: 717-727.
35. Ahrén B, Winzell MS, Wierup N, et al. DPP-4 inhibition improves glucose tolerance and increases insulin and GLP-1 responses to gastric glucose in association with normalized islet topography in mice with beta-cell-specific overexpression of human islet amyloid polypeptide. Regul Pept 2007; 143: 97-103.
36. Pospisilik JA, Martin J, Doty T, et al. Dipeptidyl peptidase IV inhibitor treatment stimulates β-cell survival and islet neogenesis in streptozotocin-induced diabetic rats. Diabetes 2003; 523: 741-750.
37. Duttaroy A, Voelker F, Merriam K, et al. The DPP-4 inhibitor vildagliptin increases pancreatic beta cell mass in neonatal rats. Eur J Pharmacol 2011; 650: 7034-7037.
38. Riche DM, East He, Riche KD. Impact of sitagliptin on markers of beta-cell function: a meta-analysis. Am J Med Sci 2009; 337: 321-328.
39. Pratley RE, Schweizer A, Rosenstock J, et al. Robust improvements in fasting and prandial measures of beta-cell function with vildagliptin in drug-naïve patients: analysis of pooled vildagliptin monotherapy database. Diabetes Obes Metab 2008; 10: 931-938.
40. Chacra AR. Saxagliptin for type 2 diabetes. Diabetes Metab Syndr Obes 2010; 3: 325-335.
41. Del Prato S, Barnett AH, Huisman H, et al. Effect of linagliptin monotherapy on glycaemic control and markers of β-cell function in patients with inadequately controlled type 2 diabetes: a randomized controlled trial. Diabetes Obes Metab 2011; 13: 258-267.
42. Ahrén B, Pacini G, Tura A, et al. Improved meal-related insulin processing contributes to the enhancement of B-cell function by the DPP-4 inhibitor vildagliptin in patients with type 2 diabetes. Horm Metab Res 2007; 39: 826-829.
43. Rosenstock J, Brazg R, Andryuk PJ, 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 2006; 28: 1556-1568.
44. Ahrén B, Landin-Olsson M, Jansson PA, et al. Inhibition of dipeptidyl peptidase-4 reduces glycemia, sustains insulin levels and reduces glucagon levels in type 2 diabetes. J Clin Endocrinol Metab 2004; 89: 2078-2084.
45. Azuma K, Radikova Z, Mancino J, et al. Measurements of islet function and glucose metabolism with the dipeptidyl peptidase 4 inhibitor vildagliptin in patients with type 2 diabetes. J Clin Endocrinol Metab 2008; 93: 459-464.
46. Ahrén B, Pacini G, Foley JE, et al. Improved meal-related beta-cell function and insulin sensitivity by the dipeptidyl peptidase-IV inhibitor vildagliptin in metformin-treated patients with type 2 diabetes over 1year. Diabetes Care 2005; 28: 1936-1940.
47. He YL, Wang Y, Bullock JM, et al. Pharmacodynamics of vildagliptin in patients with type 2 diabetes during OGTT. J Clin Pharmacol 2007; 47: 633-641.
48. Herman GA, Bergman A, Stevens C, et al. Effect of single oral doses of sitagliptin, a dipeptidyl peptidase-4 inhibitor, on incretin and plasma glucose levels after an oral glucose tolerance test in patients with type 2 diabetes. J Clin Endocrinol Metab 2006; 9: 4612-4619.
49. El-Ouaghlidi A, Rehring E, Holst JJ, et al. The dipeptidyl peptidase 4 inhibitor vildagliptin does not accentuate glibenclamide-induced hypoglycemia but reduces glucose-induced glucagon-like peptide 1 and gastric inhibitory polypeptide secretion. J Clin Endocrinol Metab 2007; 92: 4165-4171.
50. D'Alessio DA, Denney AM, Hermiller LM, et al. Treatment with the dipeptidyl peptidase-4 inhibitor vildagliptin improves fasting islet-cell function in subjects with type 2 diabetes. J Clin Endocrinol Metab 2009; 94: 81-88.
51. Henry RR, Smith SR, Schwartz SL, et al. Effects of saxagliptin on ß-cell stimulation and insulin secretion in patients with type 2 diabetes. Diabetes Obes Metab 2011; 13: 850-858.
52. Foley JE, Bunck MC, Möller-Goede DL, et al. Beta cell function following 1year vildagliptin or placebo treatment and after 12week washout in drug-naive patients with type 2 diabetes and mild hyperglycaemia: a randomised controlled trial. Diabetologia 2011; 54: 1985-1991.
53. Scherbaum WA, Schweizer A, Mari A, et al. Evidence that vildagliptin attenuates deterioration of glycaemic control during 2-year treatment of patients with type 2 diabetes and mild hyperglycaemia. Diabetes Obes Metab 2008; 10: 1114-1124.
54. Fridolf T, Böttcher G, Sundler F, et al. GLP-1 and GLP-1(7-36) amide: influences on basal and stimulated insulin and glucagon secretion in the mouse. Pancreas 1991; 6: 208-215.
55. Ahrén B, Larsson H, Holst JJ. Effects of glucagon-like peptide-1 on islet function and insulin sensitivity in noninsulin-dependent diabetes mellitus. J Clin Endocrinol Metab 1997; 82: 473-478.
56. Hare KJ, Vilsbøll T, Asmar M, et al. The glucagonostatic and insulinotropic effects of glucagon-like peptide 1 contribute equally to its glucose-lowering action. Diabetes 2010; 59: 1765-1770.
57. Balas B, Baig MR, Watson C, et al. The dipeptidyl peptidase IV inhibitor vildagliptin suppresses endogenous glucose production and enhances islet function after single-dose administration in type 2 diabetic patients. J Clin Endocrinol Metab 2007; 92: 1249-1255.
58. Ahrén B, Foley JE, Ferrannini E, et al. Changes in prandial glucagon levels after a 2-year treatent with vildagliptin or glimepiride in patients with type 2 diabetes inadequately controlled with metformin monotherapy. Diabetes Care 2010; 33: 730-732.
59. Ahrén B, Schweizer A, Dejager S, et al. Vildagliptin enhances islet responsiveness to both hyper- and hypoglycaemia in patients with type 2 diabetes. J Clin Endocrinol Metab 2009; 94: 1236-1243.
60. Meier JJ, Gallwitz B, Siepmann N, et al. Gastric inhibitory polypeptide (GIP) dose-dependently stimulates glucagon secretion in healthy human subjects at euglycaemia. Diabetologia 2003; 46: 798-801.
61. Fonseca V, Schweizer A, Albrecht D, et al. Addition of vildagliptin to insulin improves glycaemic control in type 2 diabetes. Diabetologia 2007; 50: 1148-1155.