DPP-4 inhibitors in the treatment of type 2 diabetes

Biochemical Pharmacology

Volumn 83, Issue 7, 2012, Pages 823-832

  Duez, Hélène ^a,b,c   Cariou, Bertrand ^b,d,e   Staels, Bart ^a,b,c  

^a UNIV LILLE   (France)

^b INSERM   (France)

^c INSTITUT PASTEUR DE LILLE   (France)

^d NANTES UNIVERSITY HOSPITAL   (France)

^e UNIVERSITÉ DE NANTES   (France)

Author keywords

Dipeptidylpeptidase (DPP) 4 inhibitors; Gliptins; Glucagon like peptide (GLP) 1; Glycaemic control; Type 2 diabetes

Indexed keywords

ALOGLIPTIN; BMS 510849; DIPEPTIDYL PEPTIDASE IV; DIPEPTIDYL PEPTIDASE IV INHIBITOR; DUTOGLIPTIN; EXENDIN 4; GASTRIC INHIBITORY POLYPEPTIDE; GLIBENCLAMIDE; GLIMEPIRIDE; GLIPIZIDE; GLUCAGON LIKE PEPTIDE 1; GLUCAGON LIKE PEPTIDE 1 [7-36] AMIDE; HEMOGLOBIN A1C; INCRETIN; INSULIN; KRP 104; LC 15 0444; LINAGLIPTIN; LIRAGLUTIDE; MELOGLIPTIN; METFORMIN; PIOGLITAZONE; PLACEBO; ROSIGLITAZONE; SAXAGLIPTIN; SITAGLIPTIN; TENELIGLIPTIN; TRELAGLIPTIN; UNCLASSIFIED DRUG; VILDAGLIPTIN;

CARDIOVASCULAR RISK; CONTINUOUS INFUSION; DIABETES MELLITUS; DIABETIC PATIENT; DRUG DOSE COMPARISON; ENZYME INHIBITION; GLUCAGON RELEASE; GLUCOSE BLOOD LEVEL; GLUCOSE HOMEOSTASIS; GLUCOSE TOLERANCE; GLUCOSE TRANSPORT; GLYCEMIC CONTROL; HEART FAILURE; HEART INFARCTION; HEART PROTECTION; HEMOGLOBIN BLOOD LEVEL; HUMAN; HYPOGLYCEMIA; INSULIN RELEASE; KIDNEY FAILURE; MONOTHERAPY; NAUSEA; NON INSULIN DEPENDENT DIABETES MELLITUS; PRIORITY JOURNAL; PROTEIN DEGRADATION; RANDOMIZED CONTROLLED TRIAL (TOPIC); REVIEW; RHINOPHARYNGITIS; SIDE EFFECT; SINGLE DRUG DOSE; STOMACH EMPTYING; STREPTOZOCIN DIABETES; URINARY TRACT INFECTION; WEIGHT REDUCTION;

EID: 84857368498     PISSN: 00062952     EISSN: 18732968     Source Type: Journal    
DOI: 10.1016/j.bcp.2011.11.028     Document Type: Note

References (107)

1. 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 352 1998 854 865
2. R.R. Holman, S.K. Paul, M.A. Bethel, D.R. Matthews, and H.A. Neil 10-year follow-up of intensive glucose control in type 2 diabetes N Engl J Med 359 2008 1577 1589
3. S.E. Kahn, S.M. Haffner, and M.A. Heise Glycemic durability of rosiglitazone, metformin, or glyburide monotherapy N Engl J Med 355 2006 2477 2480
4. M.A. Nauck, E. Homberger, and E.G. Siegel Incretin effects of increasing glucose loads in man calculated from venous insulin and C-peptide responses J Clin Endocrinol Metab 63 1986 492 498
5. T. Vilsboll, and J.J. Holst Incretins, insulin secretion and type 2 diabetes mellitus Diabetologia 47 2004 357 366
6. J. Dupre, S.A. Ross, D. Watson, and J.C. Brown Stimulation of insulin secretion by gastric inhibitory polypeptide in man J Clin Endocrinol Metab 37 1973 826 828
7. R.M. Elliott, L.M. Morgan, J.A. Tredger, S. Deacon, J. Wright, and V. Marks 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 138 1993 159 166
8. G.I. Bell, R. Sanchez-Pescador, P.J. Laybourn, and R.C. Najarian Exon duplication and divergence in the human preproglucagon gene Nature 304 1983 368 371
9. C. Orskov, J.J. Holst, S. Knuhtsen, F.G. Baldissera, S.S. Poulsen, and O.V. Nielsen 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 119 1986 1467 1475
10. B. Kreymann, G. Williams, M.A. Ghatei, and S.R. Bloom Glucagon-like peptide-1 7-36: a physiological incretin in man Lancet 2 1987 1300 1304
11. S. Mojsov, G.C. Weir, and J.F. Habener 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 79 1987 616 619
12. D.J. Drucker, J. Philippe, S. Mojsov, W.L. Chick, and J.F. Habener Glucagon-like peptide I stimulates insulin gene expression and increases cyclic AMP levels in a rat islet cell line Proc Natl Acad Sci USA 84 1987 3434 3438
13. L.L. Baggio, and D.J. Drucker Biology of incretins: GLP-1 and GIP Gastroenterology 132 2007 2131 2157
14. G.C. Weir, S. Mojsov, G.K. Hendrick, and J.F. Habener Glucagonlike peptide I (7-37) actions on endocrine pancreas Diabetes 38 1989 338 342
15. L.A. Scrocchi, B.A. Marshall, S.M. Cook, P.L. Brubaker, and D.J. Drucker Identification of glucagon-like peptide 1 (GLP-1) actions essential for glucose homeostasis in mice with disruption of GLP-1 receptor signaling Diabetes 47 1998 632 639
16. D.H. Song, L. Getty-Kaushik, E. Tseng, J. Simon, B.E. Corkey, and M.M. Wolfe Glucose-dependent insulinotropic polypeptide enhances adipocyte development and glucose uptake in part through Akt activation Gastroenterology 133 2007 1796 1805
17. P.L. McClean, N. Irwin, R.S. Cassidy, J.J. Holst, V.A. Gault, and P.R. Flatt GIP receptor antagonism reverses obesity, insulin resistance, and associated metabolic disturbances induced in mice by prolonged consumption of high-fat diet Am J Physiol Endocrinol Metab 293 2007 E1746 E1755
18. K. Miyawaki, Y. Yamada, and H. Yano Glucose intolerance caused by a defect in the entero-insular axis: a study in gastric inhibitory polypeptide receptor knockout mice Proc Natl Acad Sci USA 96 1999 14843 14847
19. K. Miyawaki, Y. Yamada, and N. Ban Inhibition of gastric inhibitory polypeptide signaling prevents obesity Nat Med 8 2002 738 742
20. T. Hansotia, L.L. Baggio, and D. Delmeire Double incretin receptor knockout (DIRKO) mice reveal an essential role for the enteroinsular axis in transducing the glucoregulatory actions of DPP-IV inhibitors Diabetes 53 2004 1326 1335
21. M. Nauck, F. Stockmann, R. Ebert, and W. Creutzfeldt Reduced incretin effect in type 2 (non-insulin-dependent) diabetes Diabetologia 29 1986 46 52
22. T. Vilsboll, T. Krarup, C.F. Deacon, S. Madsbad, and J.J. Holst Reduced postprandial concentrations of intact biologically active glucagon-like peptide 1 in type 2 diabetic patients Diabetes 50 2001 609 613
23. J.J. Meier, and M.A. Nauck Is the diminished incretin effect in type 2 diabetes just an epi-phenomenon of impaired beta-cell function? Diabetes 59 2010 1117 1125
24. M.B. Toft-Nielsen, M.B. Damholt, and S. Madsbad Determinants of the impaired secretion of glucagon-like peptide-1 in type 2 diabetic patients J Clin Endocrinol Metab 86 2001 3717 3723
25. E. Rask, T. Olsson, and S. Soderberg Impaired incretin response after a mixed meal is associated with insulin resistance in nondiabetic men Diabetes Care 24 2001 1640 1645
26. K. Vollmer, J.J. Holst, and B. Baller Predictors of incretin concentrations in subjects with normal, impaired, and diabetic glucose tolerance Diabetes 57 2008 678 687
27. L.R. Ranganath, J.M. Beety, L.M. Morgan, J.W. Wright, R. Howland, and V. Marks Attenuated GLP-1 secretion in obesity: cause or consequence Gut 38 1996 916 919
28. E. Muscelli, A. Mari, and A. Casolaro Separate impact of obesity and glucose tolerance on the incretin effect in normal subjects and type 2 diabetic patients Diabetes 57 2008 1340 1348
29. C.F. Deacon, M.A. Nauck, M. Toft-Nielsen, L. Pridal, B. Willms, and J.J. Holst Both subcutaneously and intravenously administered glucagon-like peptide I are rapidly degraded from the NH2-terminus in type II diabetic patients and in healthy subjects Diabetes 44 1995 1126 1131
30. C.F. Deacon, M.A. Nauck, J. Meier, K. Hucking, and J.J. Holst Degradation of endogenous and exogenous gastric inhibitory polypeptide in healthy and in type 2 diabetic subjects as revealed using a new assay for the intact peptide J Clin Endocrinol Metab 85 2000 3575 3581
31. S.L. Conarello, Z. Li, and J. Ronan Mice lacking dipeptidyl peptidase IV are protected against obesity and insulin resistance Proc Natl Acad Sci USA 100 2003 6825 6830
32. D. Marguet, L. Baggio, and T. Kobayashi Enhanced insulin secretion and improved glucose tolerance in mice lacking CD26 Proc Natl Acad Sci USA 97 2000 6874 6879
33. J.A. Pospisilik, S.G. Stafford, and H.U. Demuth Long-term treatment with the dipeptidyl peptidase IV inhibitor P32/98 causes sustained improvements in glucose tolerance, insulin sensitivity, hyperinsulinemia, and beta-cell glucose responsiveness in VDF (fa/fa) Zucker rats Diabetes 51 2002 943 950
34. J.A. Pospisilik, J. Martin, and T. Doty Dipeptidyl peptidase IV inhibitor treatment stimulates beta-cell survival and islet neogenesis in streptozotocin-induced diabetic rats Diabetes 52 2003 741 750
35. R.A. Pederson, H.A. White, D. Schlenzig, R.P. Pauly, C.H. McIntosh, and H.U. Demuth Improved glucose tolerance in Zucker fatty rats by oral administration of the dipeptidyl peptidase IV inhibitor isoleucine thiazolidide Diabetes 47 1998 1253 1258
36. J.A. Pospisilik, S.G. Stafford, H.U. Demuth, C.H. McIntosh, and R.A. Pederson Long-term treatment with dipeptidyl peptidase IV inhibitor improves hepatic and peripheral insulin sensitivity in the VDF Zucker rat: a euglycemic-hyperinsulinemic clamp study Diabetes 51 2002 2677 2683
37. B. Ahren, M.S. Winzell, N. Wierup, F. Sundler, B. Burkey, and T.E. Hughes 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 143 2007 97 103
38. K. Raun, P. von Voss, C.F. Gotfredsen, V. Golozoubova, B. Rolin, and L.B. Knudsen Liraglutide, a long-acting glucagon-like peptide-1 analog, reduces body weight and food intake in obese candy-fed rats, whereas a dipeptidyl peptidase-IV inhibitor, vildagliptin, does not Diabetes 56 2007 8 15
39. S.J. Kim, C. Nian, D.J. Doudet, and C.H. McIntosh Inhibition of dipeptidyl peptidase IV with sitagliptin (MK0431) prolongs islet graft survival in streptozotocin-induced diabetic mice Diabetes 57 2008 1331 1339
40. A. Maida, T. Hansotia, C. Longuet, Y. Seino, and D.J. Drucker Differential importance of glucose-dependent insulinotropic polypeptide vs glucagon-like peptide 1 receptor signaling for beta cell survival in mice Gastroenterology 137 2009 2146 2157
41. J. Mu, A. Petrov, and G.J. Eiermann 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 623 2009 148 154
42. J. Mu, J. Woods, and Y.P. Zhou Chronic inhibition of dipeptidyl peptidase-4 with a sitagliptin analog preserves pancreatic beta-cell mass and function in a rodent model of type 2 diabetes Diabetes 55 2006 1695 1704
43. H.J. Mest, and R. Mentlein Dipeptidyl peptidase inhibitors as new drugs for the treatment of type 2 diabetes Diabetologia 48 2005 616 620
44. G. Flock, L.L. Baggio, C. Longuet, and D.J. Drucker Incretin receptors for glucagon-like peptide 1 and glucose-dependent insulinotropic polypeptide are essential for the sustained metabolic actions of vildagliptin in mice Diabetes 56 2007 3006 3013
45. G.A. Herman, C. Stevens, and K. Van Dyck Pharmacokinetics 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 78 2005 675 688
46. A.J. Bergman, C. Stevens, and Y. Zhou Pharmacokinetic and pharmacodynamic properties of multiple oral doses of sitagliptin, a dipeptidyl peptidase-IV inhibitor: a double-blind, randomized, placebo-controlled study in healthy male volunteers Clin Ther 28 2006 55 72
47. G.A. Herman, A. Bergman, and F. Liu Pharmacokinetics and pharmacodynamic effects of the oral DPP-4 inhibitor sitagliptin in middle-aged obese subjects J Clin Pharmacol 46 2006 876 886
48. E.B. Villhauer, J.A. Brinkman, and G.B. Naderi 1-[[(3-hydroxy-1- adamantyl)amino]acetyl]-2-cyano-(S)-pyrrolidine: a potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitor with antihyperglycemic properties J Med Chem 46 2003 2774 2789
49. Y.L. He, D. Serra, and Y. Wang Pharmacokinetics and pharmacodynamics of vildagliptin in patients with type 2 diabetes mellitus Clin Pharmacokinet 46 2007 577 588
50. Y.L. He, Y. Wang, and J.M. Bullock Pharmacodynamics of vildagliptin in patients with type 2 diabetes during OGTT J Clin Pharmacol 47 2007 633 641
51. D.J. Augeri, J.A. Robl, and D.A. Betebenner 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 48 2005 5025 5037
52. J. Feng, Z. Zhang, and M.B. Wallace Discovery of alogliptin: a potent, selective, bioavailable, and efficacious inhibitor of dipeptidyl peptidase IV J Med Chem 50 2007 2297 2300
53. P. Covington, R. Christopher, and M. Davenport Pharmacokinetic, pharmacodynamic, and tolerability profiles of the dipeptidyl peptidase-4 inhibitor alogliptin: a randomized, double-blind, placebo-controlled, multiple-dose study in adult patients with type 2 diabetes Clin Ther 30 2008 499 512
54. S. Huttner, E.U. Graefe-Mody, B. Withopf, A. Ring, and K.A. Dugi Safety, tolerability, pharmacokinetics, and pharmacodynamics of single oral doses of BI 1356, an inhibitor of dipeptidyl peptidase 4, in healthy male volunteers J Clin Pharmacol 48 2008 1171 1178
55. T. Heise, E.U. Graefe-Mody, S. Huttner, A. Ring, D. Trommeshauser, and K.A. Dugi Pharmacokinetics, pharmacodynamics and tolerability of multiple oral doses of linagliptin, a dipeptidyl peptidase-4 inhibitor in male type 2 diabetes patients Diabetes Obes Metab 11 2009 786 794
56. A.J. Bergman, J. Cote, and B. Yi Effect of renal insufficiency on the pharmacokinetics of sitagliptin, a dipeptidyl peptidase-4 inhibitor Diabetes Care 30 2007 1862 1864
57. S.H. Vincent, J.R. Reed, and A.J. Bergman Metabolism and excretion of the dipeptidyl peptidase 4 inhibitor [14C]sitagliptin in humans Drug Metab Dispos 35 2007 533 538
58. J.C. Chan, R. Scott, and J.C. Arjona Ferreira Safety and efficacy of sitagliptin in patients with type 2 diabetes and chronic renal insufficiency Diabetes Obes Metab 10 2008 545 555
59. U. Graefe-Mody, C. Friedrich, and A. Port Effect of renal impairment on the pharmacokinetics of the dipeptidyl peptidase-4 inhibitor linagliptin(*) Diabetes Obes Metab 13 2011 939 946
60. B. Ahren Clinical results of treating type 2 diabetic patients with sitagliptin, vildagliptin or saxagliptin - diabetes control and potential adverse events Best Pract Res Clin Endocrinol Metab 23 2009 487 498
61. G.R. Lankas, B. Leiting, and R.S. Roy Dipeptidyl peptidase IV inhibition for the treatment of type 2 diabetes: potential importance of selectivity over dipeptidyl peptidases 8 and 9 Diabetes 54 2005 2988 2994
62. B.F. Burkey, P.K. Hoffmann, U. Hassiepen, J. Trappe, M. Juedes, and J.E. Foley Adverse effects of dipeptidyl peptidases 8 and 9 inhibition in rodents revisited Diabetes Obes Metab 10 2008 1057 1061
63. P. Aschner, M.S. Kipnes, J.K. Lunceford, M. Sanchez, C. Mickel, and D.E. Williams-Herman Effect of the dipeptidyl peptidase-4 inhibitor sitagliptin as monotherapy on glycemic control in patients with type 2 diabetes Diabetes Care 29 2006 2632 2637
64. B.J. Goldstein, M.N. Feinglos, J.K. Lunceford, J. Johnson, and D.E. Williams-Herman Effect of initial combination therapy with sitagliptin, a dipeptidyl peptidase-4 inhibitor, and metformin on glycemic control in patients with type 2 diabetes Diabetes Care 30 2007 1979 1987
65. B. Charbonnel, A. Karasik, J. Liu, M. Wu, and G. Meininger 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 29 2006 2638 2643
66. J. Rosenstock, R. Brazg, P.J. Andryuk, K. Lu, and P. Stein 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 28 2006 1556 1568
67. M.A. Nauck, G. Meininger, D. Sheng, L. Terranella, and P.P. Stein 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 9 2007 194 205
68. T. Seck, M. Nauck, and D. Sheng Safety and efficacy of treatment with sitagliptin or glipizide in patients with type 2 diabetes inadequately controlled on metformin: a 2-year study Int J Clin Pract 64 2010 562 576
69. R.E. Pratley, M. Nauck, and T. Bailey Liraglutide versus sitagliptin for patients with type 2 diabetes who did not have adequate glycaemic control with metformin: a 26-week, randomised, parallel-group, open-label trial Lancet 375 2010 1447 1456
70. F.X. Pi-Sunyer, A. Schweizer, D. Mills, and S. Dejager Efficacy and tolerability of vildagliptin monotherapy in drug-naive patients with type 2 diabetes Diabetes Res Clin Pract 76 2007 132 138
71. E. Bosi, R.P. Camisasca, C. Collober, E. Rochotte, and A.J. Garber Effects of vildagliptin on glucose control over 24 weeks in patients with type 2 diabetes inadequately controlled with metformin Diabetes Care 30 2007 890 895
72. A.J. Garber, A. Schweizer, M.A. Baron, E. Rochotte, and S. Dejager Vildagliptin in combination with pioglitazone improves glycaemic control in patients with type 2 diabetes failing thiazolidinedione monotherapy: a randomized, placebo-controlled study Diabetes Obes Metab 9 2007 166 174
73. E. Ferrannini, V. Fonseca, and B. Zinman Fifty-two-week efficacy and safety of vildagliptin vs. glimepiride in patients with type 2 diabetes mellitus inadequately controlled on metformin monotherapy Diabetes Obes Metab 11 2009 157 166
74. S. Del Prato, A.H. Barnett, H. Huisman, D. Neubacher, H.J. Woerle, and K.A. Dugi Effect of linagliptin monotherapy on glycaemic control and markers of beta-cell function in patients with inadequately controlled type 2 diabetes: a randomized controlled trial Diabetes Obes Metab 13 2011 258 267
75. M.R. Taskinen, J. Rosenstock, and I. Tamminen Safety and efficacy of linagliptin as add-on therapy to metformin in patients with type 2 diabetes: a randomized, double-blind, placebo-controlled study Diabetes Obes Metab 13 2011 65 74
76. L. Sloan, J. Newman, C. Sauce, M. von Eynatten, S. Patel, and Woerle H.J. Safety Efficacy of linagliptin in type 2 diabetes patients with severe renal impairment Diabetes 60 2011 A114
77. R.A. DeFronzo, P.R. Fleck, C.A. Wilson, and Q. Mekki Efficacy and safety of the dipeptidyl peptidase-4 inhibitor alogliptin in patients with type 2 diabetes and inadequate glycemic control: a randomized, double-blind, placebo-controlled study Diabetes Care 31 2008 2315 2317
78. M.A. Nauck, G.C. Ellis, P.R. Fleck, C.A. Wilson, and Q. Mekki Efficacy and safety of adding the dipeptidyl peptidase-4 inhibitor alogliptin to metformin therapy in patients with type 2 diabetes inadequately controlled with metformin monotherapy: a multicentre, randomised, double-blind, placebo-controlled study Int J Clin Pract 63 2009 46 55
79. R.E. Pratley, M.S. Kipnes, P.R. Fleck, C. Wilson, and Q. Mekki Efficacy and safety of the dipeptidyl peptidase-4 inhibitor alogliptin in patients with type 2 diabetes inadequately controlled by glyburide monotherapy Diabetes Obes Metab 11 2009 167 176
80. J. Rosenstock, M.S. Rendell, J.L. Gross, P.R. Fleck, C.A. Wilson, and Q. Mekki Alogliptin added to insulin therapy in patients with type 2 diabetes reduces HbA(1C) without causing weight gain or increased hypoglycaemia Diabetes Obes Metab 11 2009 1145 1152
81. J. Rosenstock, S. Sankoh, and J.F. List Glucose-lowering activity of the dipeptidyl peptidase-4 inhibitor saxagliptin in drug-naive patients with type 2 diabetes Diabetes Obes Metab 10 2008 376 386
82. J. Rosenstock, C. Aguilar-Salinas, E. Klein, S. Nepal, J. List, and R. Chen Effect of saxagliptin monotherapy in treatment-naive patients with type 2 diabetes Curr Med Res Opin 25 2009 2401 2411
83. R.A. DeFronzo, M.N. Hissa, and A.J. Garber The efficacy and safety of saxagliptin when added to metformin therapy in patients with inadequately controlled type 2 diabetes with metformin alone Diabetes Care 32 2009 1649 1655
84. P. Hollander, J. Li, E. Allen, and R. Chen Saxagliptin added to a thiazolidinedione improves glycemic control in patients with type 2 diabetes and inadequate control on thiazolidinedione alone J Clin Endocrinol Metab 94 2009 4810 4819
85. A.R. Chacra, G.H. Tan, A. Apanovitch, S. Ravichandran, J. List, and R. Chen Saxagliptin added to a submaximal dose of sulphonylurea improves glycaemic control compared with uptitration of sulphonylurea in patients with type 2 diabetes: a randomised controlled trial Int J Clin Pract 63 2009 1395 1406
86. M. Nowicki, I. Rychlik, and H. Haller Saxagliptin improves glycaemic control and is well tolerated in patients with type 2 diabetes mellitus and renal impairment Diabetes Obes Metab 13 2011 523 532
87. A.J. Scheen, G. Charpentier, C.J. Ostgren, A. Hellqvist, and I. Gause-Nilsson Efficacy and safety of saxagliptin in combination with metformin compared with sitagliptin in combination with metformin in adult patients with type 2 diabetes mellitus Diabetes Metab Res Rev 26 2010 540 549
88. M. El Yacoubi, J.M. Vaugeois, and D. Marguet Behavioral characterization of CD26 deficient mice in animal tests of anxiety and antidepressant-like activity Behav Brain Res 171 2006 279 285
89. S. Yan, D. Marguet, J. Dobers, W. Reutter, and H. Fan Deficiency of CD26 results in a change of cytokine and immunoglobulin secretion after stimulation by pokeweed mitogen Eur J Immunol 33 2003 1519 1527
90. S.J. Kim, C. Nian, D.J. Doudet, and C.H. McIntosh Dipeptidyl peptidase IV inhibition with MK0431 improves islet graft survival in diabetic NOD mice partially via T-cell modulation Diabetes 58 2009 641 651
91. N.N. Ta, Y. Li, C.A. Schuyler, M.F. Lopes-Virella, and Y.D.P.P-4 Huang (CD26) inhibitor alogliptin inhibits TLR4-mediated ERK activation and ERK-dependent MMP-1 expression by U937 histiocytes Atherosclerosis 213 2010 429 435
92. K.W. Christopherson, G. Hangoc, C.R. Mantel, and H.E. Broxmeyer Modulation of hematopoietic stem cell homing and engraftment by CD26 Science 305 2004 1000 1003
93. M.A. Nauck, T. Vilsboll, B. Gallwitz, A. Garber, and S. Madsbad Incretin-based therapies: viewpoints on the way to consensus Diabetes Care 32 Suppl. 2 2009 S223 S231
94. L.A. Nikolaidis, S. Mankad, and G.G. Sokos Effects of glucagon-like peptide-1 in patients with acute myocardial infarction and left ventricular dysfunction after successful reperfusion Circulation 109 2004 962 965
95. M. Arakawa, T. Mita, and K. Azuma Inhibition of monocyte adhesion to endothelial cells and attenuation of atherosclerotic lesion by a glucagon-like peptide-1 receptor agonist, exendin-4 Diabetes 59 2010 1030 1037
96. R. Gros, X. You, and L.L. Baggio Cardiac function in mice lacking the glucagon-like peptide-1 receptor Endocrinology 144 2003 2242 2252
97. G.G. Sokos, L.A. Nikolaidis, S. Mankad, D. Elahi, and R.P. Shannon Glucagon-like peptide-1 infusion improves left ventricular ejection fraction and functional status in patients with chronic heart failure J Card Fail 12 2006 694 699
98. G.G. Sokos, H. Bolukoglu, and J. German Effect of glucagon-like peptide-1 (GLP-1) on glycemic control and left ventricular function in patients undergoing coronary artery bypass grafting Am J Cardiol 100 2007 824 829
99. J.H. Best, B.J. Hoogwerf, and W.H. Herman 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 34 2011 90 95
100. M. Halbirk, H. Norrelund, and N. Moller Cardiovascular and metabolic effects of 48-h glucagon-like peptide-1 infusion in compensated chronic patients with heart failure Am J Physiol Heart Circ Physiol 298 2010 H1096 H1102
101. P.A. Read, F.Z. Khan, P.M. Heck, S.P. Hoole, and D.P. Dutka DPP-4 inhibition by sitagliptin improves the myocardial response to dobutamine stress and mitigates stunning in a pilot study of patients with coronary artery disease Circ Cardiovasc Imaging 3 2010 195 201
102. M. Sauve, K. Ban, and M.A. Momen Genetic deletion or pharmacological inhibition of dipeptidyl peptidase-4 improves cardiovascular outcomes after myocardial infarction in mice Diabetes 59 2010 1063 1073
103. R. Frederich, J.H. Alexander, and F.T. Fiedorek A systematic assessment of cardiovascular outcomes in the saxagliptin drug development program for type 2 diabetes Postgrad Med 122 2010 16 27
104. M. Monami, I. Iacomelli, N. Marchionni, and E. Mannucci Dipeptidyl peptidase-4 inhibitors in type 2 diabetes: a meta-analysis of randomized clinical trials Nutr Metab Cardiovasc Dis 20 2010 224 235
105. M.A. Bethel, J. Green, R. Califf, and R. Holman Rationale and design of the Trial Evaluating Cardiovascular Outcomes with Sitagliptin (TECOS) ADA 2009 Poster 2152-PO
106. J. Rosenstock, N. Marx, and S.E. Kahn Rationale and design of the CAROLINA trial: an active comparator CARdiOvascular Outcome Study of the DPP-4 inhibitor LINAgliptin in patients with type 2 diabetes at high cardiovascular risk Diabetes 60 2011 A303
107. W.B. White, G.L. Bakris, and R.M. Bergenstal EXamination of cArdiovascular outcoMes with alogliptIN versus standard of carE in patients with type 2 diabetes mellitus and acute coronary syndrome (EXAMINE): a cardiovascular safety study of the dipeptidyl peptidase 4 inhibitor alogliptin in patients with type 2 diabetes with acute coronary syndrome Am Heart J 162 2011 620 626