Incretin-based therapies in type 2 diabetes: A review of clinical results

Diabetes Research and Clinical Practice

Volumn 82, Issue SUPPL. 2, 2008, Pages

  Bosi, Emanuele ^a   Lucotti, Pietro ^a   Setola, Emanuela ^a   Monti, Lucilla ^a   Piatti, Pier Marco ^a  

^a SAN RAFFAELE HOSPITAL   (Italy)

Author keywords

Diabetes mellitus; DPP 4 inhibitors; Exenatide; GLP 1 analogues; Sitagliptin; Vidagliptin

Indexed keywords

2,4 THIAZOLIDINEDIONE DERIVATIVE; ACARBOSE; EXENDIN 4; GLIMEPIRIDE; GLIPIZIDE; GLUCAGON LIKE PEPTIDE 1; HEMOGLOBIN A1C; INCRETIN; INSULIN; INSULIN ASPART; INSULIN GLARGINE; METFORMIN; PIOGLITAZONE; ROSIGLITAZONE; SAXAGLIPTIN; SITAGLIPTIN; SULFONYLUREA; VILDAGLIPTIN;

ABSENCE OF SIDE EFFECTS; ARTICLE; DRUG EFFICACY; DRUG HALF LIFE; DRUG MECHANISM; DRUG RECEPTOR BINDING; DRUG SAFETY; GASTROINTESTINAL SYMPTOM; GLUCOSE BLOOD LEVEL; HUMAN; NAUSEA; NON INSULIN DEPENDENT DIABETES MELLITUS;

ADAMANTANE; CLINICAL TRIALS AS TOPIC; DIABETES MELLITUS, TYPE 2; DIPEPTIDYL-PEPTIDASE IV INHIBITORS; GLUCAGON-LIKE PEPTIDE 1; HUMANS; INCRETINS; NITRILES; PEPTIDES; PYRAZINES; PYRROLIDINES; TRIAZOLES; VENOMS;

EID: 56949086428     PISSN: 01688227     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.diabres.2008.10.003     Document Type: Article

References (65)

1. Resnick H.E., Foster G.L., Bardsley J., and Ratner R.E. Achievement of American Diabetes Association clinical practice recommendations among US adults with diabetes, 1999-2002: the National Health and Nutrition Examination Survey. Diabetes Care 29 (2006) 531-537
2. 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 352 (9131) (1998) 837-853.
3. Kahn S.E., Haffner S., Heise M.A., Herman W.H., Holman R.R., Jones N.P., et al. ADOPT Study Group. Glycemic durability of rosiglitazone, metformin, or glyburide monotherapy. N. Engl. J. Med. 355 (2006) 2427-2443
4. Nathan D.M., Buse J.B., Davidson M.B., Heine R.J., Holman R.R., Sherwin R., et al. Professional Practice Committee, American Diabetes Association; European Association for the Study of Diabetes. Management of hyperglycaemia 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 29 (2006) 1963-1972
5. UKPDS Group, Overview of six years' therapy of type 2 diabetes-a progressive disease UKPDS 16, Diabetes 44 (1995) 1249-1258.
6. Wajchenberg B.L. Beta-cell failure in diabetes and preservation by clinical treatment. Endocrinol. Rev. 28 (2007) 187-218
7. Weyer C., Bogardus C., Mott D.M., and Pratley R.E. The natural history of insulin secretory dysfunction and insulin resistance in the pathogenesis of type 2 diabetes mellitus. J. Clin. Invest. 104 (1999) 787-794
8. Poitout V., and Robertson R.P. Glucolipotoxicity: fuel excess and beta-cell dysfunction. Endocrinol. Rev. 29 (2008) 351-366
9. Haataja L., Gurlo T., Huang C.J., and Butler P.C. Islet amyloid in type 2 diabetes, and the toxic oligomer hypothesis. Endocrinol. Rev. 29 (2008) 303-316
10. Donath M.Y., Størling J., Berchtold L.A., Billestrup N., and Mandrup-Poulsen T. Cytokines and beta-cell biology: from concept to clinical translation. Endocrinol. Rev. 29 (2008) 334-350
11. Abdul-Ghani M., and DeFronzo R.A. Fasting hyperglycemia impairs glucose- but not insulin-mediated suppression of glucagon secretion. J. Clin. Endocrinol. Metab. 92 (2007) 1778-1784
12. Holst J.J., and Gromada J. Role of incretin hormones in the regulation of insulin secretion in diabetic and nondiabetic humans. Am. J. Physiol. Endocrinol. Metab. 287 (2004) E199-206
13. Creutzfeldt W. The incretin concept today. Diabetologia 16 (1979) 75-85
14. Nauck M., Stockmann F., Ebert R., and Creutzfeldt W. Reduced incretin effect in type 2 (non-insulin-dependent) diabetes. Diabetologia 29 (1986) 46-52
15. Holst J.J. The physiology of glucagon-like peptide 1. Physiol. Rev. 87 (2007) 1409-1439
16. Toft-Nielsen M.B., Damholt M.B., Madsbad S., Hilsted L.M., Hughes T.E., Michelsen B.K., et al. Determinants of the impaired secretion of glucagon-like peptide-1 in type 2 diabetic patients. J. Clin. Endocrinol. Metab. 86 (2001) 3717-3723
17. Drucker D.J., and Nauck M.A. The incretin system: glucagon-like peptide-1 receptor agonists and dipeptidyl peptidase-4 inhibitors in type 2 diabetes. Lancet 368 (2006) 1696-1705
18. Rachman J., Barrow B.A., Levy J.C., and Turner R.C. Near-normalisation of diurnal glucose concentrations by continuous administration of glucagon-like peptide-1 (GLP-1) in subjects with NIDDM. Diabetologia 40 (1997) 205-211
19. Zander M., Madsbad S., Madsen J., and Holst J.J. 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 359 (2002) 824-830
20. Deacon C.F., Nauck M.A., Toft-Nielsen M., Pridal L., Willms B., and Holst J.J. 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
21. Amori R.E., Lau J., and Pittas A.G. Efficacy and safety of incretin therapy in type 2 diabetes: systematic review and meta-analysis. JAMA 298 (2007) 194-206
22. Nielsen L.L., and Baron A.D. Pharmacology of exenatide (synthetic exendin-4) for the treatment of type 2 diabetes. Curr. Opin. Invest. Drugs 4 (2003) 401-405
23. Buse J.B., Henry R.R., Han J., Kim D.D., Fineman M.S., and Baron A.D. Effects of exenatide (exendin-4) on glycemic control over 30 weeks in sulfonylurea-treated patients with type 2 diabetes. Diabetes Care 27 (2004) 2628-2635
24. DeFronzo R.A., Ratner R.E., Han J., Kim D.D., Fineman M.S., and Baron A.D. Effects of exenatide (exendin-4) on glycemic control and weight over 30 weeks in metformin-treated patients with type 2 diabetes. Diabetes Care 28 (2005) 1092-1100
25. Kendall D.M., Riddle M.C., Rosenstock J., Zhuang D., Kim D.D., Fineman M.S., 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 28 (2005) 1083-1091
26. Zinman B., Hoogwerf B.J., Duran-Garcia S., Milton D.R., Giaconia J.M., Kim D.D., et al. The effect of adding exenatide to a thiazolidinedione in suboptimally controlled type 2 diabetes: a randomized trial. Ann. Intern. Med. 146 (2007) 477-485
27. Heine R.J., Van Gaal L.F., Johns D., Mihm M.J., Widel M.H., and Brodows R.G. Exenatide versus insulin glargine in patients with suboptimally controlled type 2 diabetes: a randomized trial. Ann. Intern. Med. 143 (2005) 559-569
28. Nauck M.A., Duran S., Kim D., Johns D., Northrup J., Festa A., 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 50 (2007) 259-267
29. Klonoff D.C., Buse J.B., Nielsen L.L., Guan X., Bowlus C.L., Holcombe J.H., 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. 24 (2008) 275-286
30. Kim D., Macconell L., Zhuang D., Kothare P.A., Trautmann M., Fineman M., 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 30 (2007) 1487-1493
31. Kim D., Wang L., Beconi M., Eiermann G.J., Fisher M.H., He H., et al. (trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine: a potent, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes. J. Med. Chem. 48 (2005) 141-151
32. Villhauer E.B., Brinkman J.A., Naderi G.B., Burkey B.F., Dunning B.E., Prasad K., et al. 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
33. Augeri D.J., Robl J.A., Betebenner D.A., Magnin D.R., Khanna A., Robertson J.G., 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. 48 (2005) 5025-5037
34. Feng J., Zhang Z., Wallace M.B., Stafford J.A., Kaldor S.W., Kassel D.B., et al. Discovery of alogliptin: a potent, selective, bioavailable, and efficacious inhibitor of dipeptidyl peptidase IV. J. Med. Chem. 50 (2007) 2297-2300
35. Aschner P., Kipnes M.S., Lunceford J.K., Sanchez M., Mickel C., and Williams-Herman D.E. 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
36. Raz I., Hanefeld M., Xu L., Caria C., Williams-Herman D., and Khatami H. Efficacy and safety of the dipeptidyl peptidase-4 inhibitor sitagliptin as monotherapy in patients with type 2 diabetes mellitus. Diabetologia 49 (2006) 2564-2571
37. Scott R., Wu M., Sanchez M., and Stein P. Efficacy and tolerability of the dipeptidyl peptidase-4 inhibitor sitagliptin as monotherapy over 12 weeks in patients with type 2 diabetes. Int. J. Clin. Pract. 61 (2007) 171-180
38. Hanefeld M., Herman G.A., Wu M., Mickel C., and Sanchez M. Once-daily sitagliptin, a dipeptidyl peptidase-4 inhibitor, for the treatment of patients with type 2 diabetes. Curr. Med. Res. Opin. 23 (2007) 1329-1339
39. Charbonnel B., Karasik A., Liu J., Wu M., and 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 29 (2006) 2638-2643
40. Rosenstock J., Brazg R., Andryuk P.J., Lu K., and 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. 28 (2006) 1556-1568
41. Hermansen K., Kipnes M., Luo E., Fanurik D., Khatami H., and Stein P. Efficacy and safety of the dipeptidyl peptidase-4 inhibitor, sitagliptin, in patients with type 2 diabetes mellitus inadequately controlled on glimepiride alone or on glimepiride and metformin. Diabetes Obes. Metab. 9 (2007) 733-745
42. Raz I., Chen Y., Wu M., Hussain S., Kaufman K.D., Amatruda J.M., et al. Efficacy and safety of sitagliptin added to ongoing metformin therapy in patients with type 2 diabetes. Curr. Med. Res. Opin. 24 (2008) 537-550
43. Scott R., Loeys T., Davies M.J., and Engel S.S. Efficacy and safety of sitagliptin when added to ongoing metformin therapy in patients with type 2 diabetes. Diabetes Obes. Metab. 10 (2008) 959-969
44. Nauck M.A., Meininger G., Sheng D., Terranella L., and Stein P.P. 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
45. Goldstein B.J., Feinglos M.N., Lunceford J.K., Johnson J., and Williams-Herman D.E. 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
46. Ristic S., Byiers S., Foley J., and Holmes D. Improved glycaemic control with dipeptidyl peptidase-4 inhibition in patients with type 2 diabetes: vildagliptin (LAF237) dose response. Diabetes Obes. Metab. 7 (2005) 692-698
47. Pratley R.E., Jauffret-Kamel S., Galbreath E., and Holmes D. Twelve-week monotherapy with the DPP-4 inhibitor vildagliptin improves glycemic control in subjects with type 2 diabetes. Horm. Metab. Res. 38 (2006) 423-428
48. Pi-Sunyer F.X., Schweizer A., Mills D., and Dejager S. Efficacy and tolerability of vildagliptin monotherapy in drug-naive patients with type 2 diabetes. Diabetes Res. Clin. Pract. 74 (2006) 132-138
49. Dejager S., Razac S., Foley J.E., and Schweizer A. Vildagliptin in drug-naive patients with type 2 diabetes: a 24-week, double-blind, randomized, placebo-controlled, multiple-dose study. Horm. Metab. Res. 39 (2007) 218-223
50. Scherbaum W.A., Schweizer A., Mari A., Nilsson P.M., Lalanne G., Jauffret S., et al. Efficacy and tolerability of vildagliptin in drug-naïve patients with type 2 diabetes and mild hyperglycaemia. Diabetes Obes. Metab. 10 (2008) 675-682
51. Ahrén B., Gomis R., Standl E., Mills D., and Schweizer A. Twelve- and 52-week efficacy of the dipeptidyl peptidase IV inhibitor LAF237 in metformin-treated patients with type 2 diabetes. Diabetes Care 272 (2004) 874-880
52. Garber A.J., Schweizer A., Baron M.A., Rochotte E., and Dejager S. 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
53. Bosi E., Camisasca R.P., Collober C., Rochotte E., and Garber A.J. 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
54. Fonseca V., Schweizer A., Albrecht D., Baron M.A., Chang I., and Dejager S. Addition of vildagliptin to insulin improves glycaemic control in type 2 diabetes. Diabetologia 50 (2007) 1148-1155
55. Garber A.J., Foley J.E., Banerjj M.A., Ebeling P., Gudbjornsdottir S., Camisasca R.P., et al. Effects of vildagliptin on glucose control in patients with type 2 diabetes inadequately controlled with a sulphonylurea. Diabetes Obes. Metab. (2008) February 18, Epub ahead of print
56. Rosenstock J., Baron M.A., Dejager S., Mills D., and Schweizer A. Comparison of vildagliptin and rosiglitazone monotherapy in patients with type 2 diabetes: a 24-week, double-blind, randomized trial. Diabetes Care 30 (2007) 217-223
57. Schweizer A., Couturier A., Foley J.E., and Dejager S. Comparison between vildagliptin and metformin to sustain reductions in HbA1c over 1 year in drug-naive patients with type 2 diabetes. Diabet. Med. 9 (2007) 955-961
58. Pan C., Yang W., Barbona J.P., Wang Y., Niggli M., Mohideen P., et al. Comparison of vildagliptin and acarbose monotherapy in patients with Type 2 diabetes: a 24-week, double-blind, randomized trial. Diabet. Med. 10 (2008) 435-441
59. Bolli G., Dotta F., Rochotte E., and Cohen S.E. Efficacy and tolerability of vildagliptin vs. pioglitazone when added to metformin: a 24-week, randomized, double-blind study. Diabetes Obes. Metab. 9 (2008) 82-90
60. Rosenstock J., Baron M.A., Camisasca R.P., Cressier F., Couturier A., and Dejager S. Efficacy and tolerability of initial combination therapy with vildagliptin and pioglitazone compared with component monotherapy in patients with type 2 diabetes. Diabetes Obes. Metab. 9 (2007) 175-185
61. Scherbaum W.A., Schweizer A., Mari A., Nilsson P.M., Lalanne G., Wang Y., 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) March 18, Epub ahead of print
62. Rosenstock J., Foley J.E., Rendell M., Landin-Olsson M., Holst J.J., Deacon C.F., et al. Effects of the dipeptidyl-peptidase-IV inhibitor Vildagliptin on incretin hormones, islet function, and postprandial glicemia in subjects with impaired glucose tolerance. Diabetes Care 31 (2008) 30-35
63. Utzschneider K.M., Tong J., Montgomery B., Udayasankar J., Gerchman F., Marcovina S.M., et al. The dipeptidyl peptidase-4 inhibitor vildagliptin improves beta-cell function and insulin sensitivity in subjects with impaired fasting glucose. Diabetes Care 31 (2008) 108-113
64. Farilla L., Bulotta A., Hirshberg B., Li Calzi S., Khoury N., et al. Glucagon-like peptide 1 inhibits cell apoptosis and improves glucose responsiveness of freshly isolated human islets. Endocrinology 144 (2003) 5149-5158
65. Farilla L., Hui H., Bertolotto C., Kang E., Bulotta A., Di Mario U., et al. Glucagon-like peptide-1 promotes islet cell growth and inhibits apoptosis in Zucker diabetic rats. Endocrinology 143 (2002) 4397-4408