Inhibition of dipeptidyl peptidase-4 with vildagliptin: A potential new treatment for type 2 diabetes

British Journal of Diabetes and Vascular Disease

Volumn 6, Issue 4, 2006, Pages 150-156

  Pratley, Richard E ^a   Salsali, Afshin ^a   Matfin, Glenn ^b,c  

^a UNIVERSITY OF VERMONT COLLEGE OF MEDICINE   (United States)

^b NOVO NORDISK INC   (United States)

^c NEW YORK UNIVERSITY SCHOOL OF MEDICINE   (United States)

Author keywords

Diabetes; DPP 4; GIP; GLP 1; Incretin enhancer; Incretin hormone

Indexed keywords

DIPEPTIDYL PEPTIDASE IV; DIPEPTIDYL PEPTIDASE IV INHIBITOR; EXENDIN 4; GASTRIC INHIBITORY POLYPEPTIDE; GLIMEPIRIDE; GLUCAGON LIKE PEPTIDE 1; GLUCAGON LIKE PEPTIDE 1 [7-36] AMIDE; GLUCOSE; HEMOGLOBIN A1C; INCRETIN; INSULIN; METFORMIN; ORAL ANTIDIABETIC AGENT; PLACEBO; ROSIGLITAZONE; SITAGLIPTIN; VILDAGLIPTIN;

ARTICLE; BODY WEIGHT DISORDER; CLINICAL TRIAL; DIET THERAPY; DISEASE CONTROL; DRUG ABSORPTION; DRUG EXCRETION; DRUG HALF LIFE; DRUG POTENCY; DRUG SAFETY; DRUG STRUCTURE; DRUG TOLERABILITY; EDEMA; ENZYME INACTIVATION; ENZYME INHIBITION; EXERCISE; GASTROINTESTINAL DISEASE; HEART ARRHYTHMIA; HEART MUSCLE CONDUCTION DISTURBANCE; HUMAN; HYPERGLYCEMIA; HYPERTENSION; HYPOGLYCEMIA; MONOTHERAPY; MOUSE; NAUSEA AND VOMITING; NON INSULIN DEPENDENT DIABETES MELLITUS; NONHUMAN; RAT; TREATMENT DURATION; TREATMENT OUTCOME; WEIGHT GAIN; WEIGHT REDUCTION;

EID: 33748325702     PISSN: 14746514     EISSN: None     Source Type: Journal    
DOI: 10.1177/14746514060060040201     Document Type: Article

References (47)

1. Wild S, Roglic C, Green A et al. Global prevalence of diabetes: estimates for the year 2000 and projections for 2030. Diabetes 2004;27:1047-53.
2. Diabetes Control and Complications Trial (DCCT) Research Group. N Engl J Med 1993;329:977-86.
3. Turner RC. The UK Prospective Diabetes Study: A review. Diabetes Care 1998;21(suppl 3):C35-C38.
4. Ohkubo Y, Kishikawa H, Araki E et al. Intensive insulin therapy prevents the progression of diabetic microvascular complications in Japanese patients with non-insulin-dependent diabetes mellitus: a randomized prospective 6-year study. Diabetes Res Clin Pract 1995;28:103-17.
5. Koro CE, Bowlin SJ, Bourgeois N, Fedder DO. Glycemic control from 1988 to 2000 among U.S. adults diagnosed with type 2 diabetes: a preliminary report. Diabetes Care 2004;27:17-20.
6. Inzucchi SE. Oral antihyperglycemia therapy for type 2 diabetes: scientific review. J Am Med Assoc 2002;287:360-72.
7. UK Prospective Diabetes Study (UKPDS) Group. Lancet 1998;352:854-65.
8. Leahy JL. Pathogenesis of type 2 diabetes mellitus. Arch Med Res 2005; 36:197-209.
9. Pratley RE, Weyer C, Bogardus C. Metabolic abnormalities in the development of type 2 diabetes mellitus. In: Diabetes Mellitus: A Fundamental and Clinical Text, 2nd edition. LeRoith D, Taylor SI, Olefsky JM, editors; Lippincott Williams & Wilkins: Philadelphia; 1999, pp 548-557.
10. Weyer C, Bogardus C, Mott DM, Pratley RE. The natural history of insulin secretory dysfunction and insulin resistance in the pathogenesis of type 2 diabetes mellitus. J Clin Invest 1999;104:787-94.
11. Pratley RE, Weyer C. The role of impaired early insulin secretion in the pathogenesis of type 2 diabetes mellitus. Diabetologia 2001;44:929-45
12. Dunning BE, Foley JE, Ahren B. Alpha cell function in health and disease: influence of glucagon-like peptide-1. Diabetologia 2005;48:1700-13.
13. Butler AE, Janson J, Bonner-Weir S et al. Beta-cell deficit and increased beta-cell apoptosis in humans with type 2 diabetes. Diabetes 2003;52: 102-10.
14. Rachman J, Barrow BA, Levy JC, Turner RC. Near-normalisation of diurnal glucose concentrations by continuous administration of glucagon-like peptide-1 (GLP-1) in subjects with NIDDM. Diabetologia 1997;40: 205-11.
15. Nauck MA, Meier JJ. Glucagon-like peptide 1 (GLP-1) and its derivatives in the treatment of diabetes. Regul Pept 2005 124(suppl): 135-48.
16. Drucker DJ. Enhancing Incretin Action for the Treatment of Type 2 Diabetes. Diabetes Care 2003;26:2929-40.
17. Vilsbøll T, Krarup T, Deacon CF et al. Reduced postprandial concentrations of intact biologically active glucagon-like peptide 1 in type 2 diabetic patients. Diabetes 2001;50:609-13.
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;86:3717-23.
19. Nauck MA, Heimesaat MM, Ørskov C et al. 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;91:301-07.
20. 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;52:380-6.
21. Meier JJ, Gallwitz B, Kask B et al. Stimulation of insulin secretion by intravenous bolus injection and continuous infusion of gastric inhibitory polypeptide in patients with type 2 diabetes and healthy control subjects. Diabetes 2004;53(suppl 3):S220-4.
22. Irwin N, O'Harte FP, Gault VA et al. GIP(Lys16PAL) and GIP(Lys37PAL): novel long-acting acylated analogues of glucose-dependent insulinotropic polypeptide with improved antidiabetic potential. J Med Chem 2006;49:1047-54.
23. Egan JM, Meneilly GS, Habener JF, Elahi D. Glucagon-like peptide-1 augments insulin-mediated glucose uptake in the obese state. J Clin Endocrinol Metab 2002;87:3768-73.
24. Nauck MA, Niedereichholz U, Ettler R et al. Glucagon-like peptide 1 inhibition of gastric emptying outweighs its insulinotropic effects in healthy humans. Am J Physiol (Endocrinol Metab) 1997;273:E981-8.
25. Perfetti R, Hui H. The role of GLP-1 in the life and death of pancreatic beta cells. Horm Metab Res 2004;36:804-10.
26. Trumper A, Trumper K, Trusheim H, Arnold R, Goke B, Horsch D. Glucose-dependent insulinotropic polypeptide is a growth factor for beta (INS-1) cells by pleiotropic signaling. Mol Endocrinol 2001;15:1559-70.
27. Deacon CF, Nauck MA, Toft-Nielsen M-B et al. Both subcutaneously and intravenously administered glucagon-like peptide-1 are rapidly degraded from the amino-acid terminus in type 2 diabetic patients and in healthy subjects. Diabetes 1995;44:1126-31.
28. Mentlein R. Dipeptidyl-peptidase IV (CD26)-role in the inactivation of regulatory peptides. Regul Pept 1999;85:9-24.
29. Ahrén B: Exenatide: a novel treatment of type 2 diabetes. Therapy 2005; 2:207-22.
30. Buse JB, Henry RR, Han J et al. Effects of Exenatide (Exendin-4) on Glycemic Control Over 30 Weeks in Sulfonylurea-Treated Patients With Type 2 Diabetes. Diabetes Care 2004;27:2628-35.
31. Marguet D, Baggio L, Kobayashi T et al. Enhanced secretion and improved glucose tolerance in mice lacking CD26. Proc Natl Acad Sci USA 2000;97:6874-9.
32. Nagakura T, Yasuda N, Yamazaki K et al. Improved glucose tolerance via enhanced glucose-dependent insulin secretion in dipeptidyl peptidase IV-deficient Fischer rats. Biochem Biophys Res Commun 2001;284:501-06.
33. Villhauer EB, Brinkman JA, Naderi GB 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 2003;46:2774-89.
34. Lankas GR, Leiting B, Roy RS 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.
35. Ahren B. Vildagliptin: an inhibitor of dipeptidyl peptidase-4 with antidiabetic properties. Expert Opin Investig Drugs 2006;15:431-42.
36. Tran P, Yin H, Smith T, Fischer F: Disposition of (14C)LAF237 in rats and humans. Drug Metab Rev 2002;34:293.
37. He Y-L, Sabo R, Wang Y et al. The Influence of Hepatic Impairment on the Pharmacokinetics of Vildagliptin. Diabetes 2006;55(suppl 1):A469.
38. Ahren B, Landin-Olsson M, Jansson P-A 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: 2078-84.
39. 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.
40. Pratley R, Jauffret-Kamel S. Galbreath, E. Holmes D. Twelve-week monotherapy with the DPP-4 inhibitor LAF237 improves glycemic control in patients with type 2 diabetes (T2DM). In Press: Hormone and Metabolic Research 2006.
41. Degager S, Lebeaut A, Couturier A, Schweizer A. Sustained Reduction in HbA1c during One-Year Treatment With Vildagliptin in Patients with Type 2 Diabetes (T2DM). Diabetes 2006;55(suppl 1):A29.
42. 1C but Without Weight Gain In Drug-Naive Patients With Type 2 Diabetes (T2DM). Diabetes 2006;55(suppl 1): A133.
43. Ahren B, Gomis R, Standl E et al. Twelve- and 52-week efficacy of the dipeptidyl peptidase IV inhibitor LAF237 in metformin-treated patients with type 2 diabetes. Diabetes Care 2004;27:2874-80.
44. Garber A, Camisasca RP, Ehrsam E etal. Vildagliptin Added to Metformin Improves Glycemic Control and May Mitigate Metformin-Induced GI Side Effects in Patients with Type 2 Diabetes (T2DM) Diabetes 2006;55(suppl 1):A29.
45. Fonseca V, Dejager S, Albrecht S et al. Vildagliptin as Add-On to Insulin in Patients with Type 2 Diabetes (T2DM). Diabetes 2006;55(suppl 1):A111.
46. Nathwani A, Lebeaut A, Byiers S et al. Reduction In Blood Pressure In Patients Treated With Vildagliptin As Monotherapy or in Combination with Metformin for Type 2 Diabetes. Diabetes 2006;55(suppl 1):A113.
47. Matikainen N, Manttari S, Schweizer A et al. Vildagliptin Decreases Postprandial Chylomicron Triglycerides (TGs) in Drug-Naive Patients with Type 2 Diabetes (T2DM) Diabetes 2006;55(suppl 1):A125.