Update: Vildagliptin for the treatment of Type 2 diabetes

Expert Opinion on Investigational Drugs

Volumn 17, Issue 1, 2008, Pages 105-113

  Garber, Alan J ^a   Sharma, Morali D ^a  

^a BAYLOR COLLEGE OF MEDICINE   (United States)

Author keywords

DPP 4; Glycemic control; HbA1c; Type 2 diabetes; Vildagliptin

Indexed keywords

2,4 THIAZOLIDINEDIONE DERIVATIVE; GLIMEPIRIDE; GLUCAGON; GLUCOSE; HEMOGLOBIN A1C; INSULIN; METFORMIN; ORAL ANTIDIABETIC AGENT; PIOGLITAZONE; PLACEBO; ROSIGLITAZONE; SULFONYLUREA DERIVATIVE; VILDAGLIPTIN; ADAMANTANE; ANTIDIABETIC AGENT; DIPEPTIDYL PEPTIDASE IV INHIBITOR; DRUG DERIVATIVE; NITRILE; PYRROLIDINE DERIVATIVE;

ABDOMINAL PAIN; ADD ON THERAPY; ARTICLE; CLINICAL TRIAL; COMBINATION CHEMOTHERAPY; DIARRHEA; DIZZINESS; DOSAGE SCHEDULE COMPARISON; DOSE RESPONSE; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG DISTRIBUTION; DRUG DOSE COMPARISON; DRUG DOSE TITRATION; DRUG EFFICACY; DRUG EXCRETION; DRUG INDUCED HEADACHE; DRUG MEGADOSE; DRUG SAFETY; DRUG TOLERABILITY; DYSPEPSIA; ENZYME INHIBITION; FLATULENCE; GASTROINTESTINAL SYMPTOM; GLUCOSE BLOOD LEVEL; GLUCOSE METABOLISM; GLYCEMIC CONTROL; HEMOGLOBIN BLOOD LEVEL; HUMAN; HYPOGLYCEMIA; INSULIN RELEASE; LOW DRUG DOSE; MAXIMUM PLASMA CONCENTRATION; MONOTHERAPY; NAUSEA; NON INSULIN DEPENDENT DIABETES MELLITUS; NONHUMAN; PERIPHERAL EDEMA; POSTPRANDIAL STATE; RHINOPHARYNGITIS; SIDE EFFECT; SINGLE DRUG DOSE; TREATMENT DURATION; UPPER RESPIRATORY TRACT INFECTION; VOMITING; WEIGHT CHANGE; DRUG COMBINATION; ENZYMOLOGY; REVIEW; TREATMENT OUTCOME;

ADAMANTANE; CLINICAL TRIALS AS TOPIC; DIABETES MELLITUS, TYPE 2; DIPEPTIDYL-PEPTIDASE IV INHIBITORS; DRUG THERAPY, COMBINATION; HUMANS; HYPOGLYCEMIC AGENTS; NITRILES; PYRROLIDINES; TREATMENT OUTCOME;

EID: 38949208872     PISSN: 13543784     EISSN: None     Source Type: Journal    
DOI: 10.1517/13543784.17.1.105     Document Type: Article

References (45)

1. Nathan DM, Cleary PA, Backlund JY, et al. Intensive diabetes treatment and cardiovascular disease in patients with Type 1 diabetes. N Engl J Med 2005;353:2643-53
2. Diabetes Control and Complications Trial Research Group. The effect of intensive treatment of diabetes on the development and progression of long-term complications in insulin-dependent diabetes mellitus. N Engl J Med 1993;329:977-86
3. 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
4. United Kingdom Prospective Diabetes Study 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 1998;352:837-53
5. Saydah SH, Fradkin J, Cowie CC. Poor control of risk factors for vascular disease among adults with previously diagnosed diabetes. JAMA 2004;291:335-42
6. Koro CE, Bowlin SJ, Bourgeois N, Fedder DO. Glycemic control from 1988 to 2000 among US adults diagnosed with Type 2 diabetes: a preliminary report. Diabetes Care 2004;27:17-20
7. Müller WA, Faloona GR, Aguilar-Parada E, Unger RH. Abnormal alpha-cell function in diabetes. Response to carbohydrate and protein ingestion. N Engl J Med 1970;283:109-15
8. Nauck MA, Homberger E, Siegel EG, et al. Incretin effects of increasing glucose loads in man calculated from venous insulin and C-peptide responses. J Clin Endocrinol Metab 1986;63:492-8
9. Nauck M, Stockmann F, Ebert R, Creutzfeldt W. Reduced incretin effect in Type 2 (non-insulin-dependent) diabetes. Diabetologia 1986;29:46-52
10. Vilsbøll T, Holst JJ. Incretins, insulin secretion and Type 2 diabetes mellitus. Diabetologia 2004;47:357,66
11. Wheeler MB, Gelling RW, McIntosh CHS, et al. Functional expression of the rat pancreatic islet glucose-dependent insulinotropic polypeptide receptor: ligand binding and intracellular signaling properties. Endocrinology 1995;136:4629-39
12. Hvidberg A, Nielsen MT, Hilsted J, et al. Effect of glucagon-like peptide-1 (proglucagon 78 - 107 amide) on hepatic glucose production in healthy man. Metabolism 1994;43:104-8
13. Kreymann B, Ghatei MA, Williams G, Bloom SR. Glucagon-like peptide-1 7-36: a physiological incretin in man. Lancet 1987;2:1300-4
14. Farilla L, Bulorta A, Hirshberg B, et al. Glucagon-like peptide 1 inhibits cell apoptosis and improves glucose responsiveness of freshly isolated human islets. Endocrinology 2003; 144:5149-58
15. Ehses JA, Casilla VR, Doty T, et al. Glucose-dependent insulinotropic polypeptide promotes β-(INS-1) cell survival via cyclic adenosine monophosphate-mediated caspase-3 inhibition and regulation of p38 mitogen-activated protein kinase. Endocrinology 2003;144:4433-45
16. Nauck MA, Meier JJ. Glucagon-like peptide 1 and its derivatives in the treatment of diabetes. Regul Pept 2005;128:135-48.
17. Ahrén B. Vildagliptin: an inhibitor of dipeptidyl peptidase-4 with antidiabetic properties. Expert Opin Investig Drugs 2006;15:431-42
18. Brandt I, Joossens J, Chen X, 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;70:134-43
19. Mentlein R. Dipeptidyl-peptidase IV (CD26) - role in the inactivation of regulatory peptides. Regul Pept 1999;85:9-24
20. Tsu H, Chen X, Chen C-T, et al. 2-[3-[2-[(2S)-2-cyano-1-pyrrolidi, y]-2-oxoethylamino]-3-methyl-1-oxobutyl]-1,2,3,4-terrahydroisoquinoline: a potent, selective, and orally bioavailable dipeptide-derived inhibitor of dipeptidyl peptidase IV. J Med Chem 2006;49:373-80
21. Ristic S, Bates PC. Vildagliptin: a novel DPP-4 inhibitor with pancreatic islet enhancement activity for treatment of patients with Type 2 diabetes. Drugs Today (Barc) 2006;42:519-31
22. Burkey BF, Russell M, Wang K, et al. Vildagliptin displays slow tight-binding to dipeptidyl peptidase 9DPP)-4, but not DPP-8 or DPP-9 [Abstract 0788]. Diabetologia 2006;49(Suppl):477-8
23. He YL, Balch A, Campestrini J, et al. Pharmacokinetics and pharmacodynamics of the DPP-4 inhibitor, LAF237, in patients with Type 2 diabetes [Abstract]. Clin Pharmauol Ther 2005;77:56
24. He YL, Wang Y, Bullock JM, et al. Pharmacodynamics of vildagliptin in patients with Type 2 diabetes during OGTT. J Clin Pharmacol 2007;47:633-41
25. He YL, Sabo R, Picard F, et al. Lack of pharmacokinetic interaction between vildagliptin and metformin in patients with Type 2 diabetes [Abstract]. Clin Pharmacol Ther 2006;79:62
26. Barilla D, He Y, Balez S, et al. No pharmacokinetic interactions or acute clinical safety issues preclude combination of the DPP-4 inhibitor LAF237 with glyburide [Abstract]. Diabetes 2004;53(Suppl):470
27. 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 200;34:2774-89
28. 14C]LAF237 in rats and humans [Abstract 293]. Drug Metab Rev 2002;34(Suppl):147
29. He YL, Sabo R, Balez S, et al. Absolute bioavailability of vildagliptin in healthy subjects [Abstract]. Clin Pharmacol Ther 2006;79:38
30. He YL, Sabo R, Wang Y, et al. The influence of age, gender and BMI on the pharmacokinetics and pharmacodynamics of vildagliptin [Abstract]. Clin Pharmacol Ther 2006;79:63
31. Mari A, Sallas WM, He YL, et al. Vildagliptin, a dipeptidyl peptidase-IV inhibitor, improves model-assessed β-cell function in patients with Type 2 diabetes. J Clin Endocrinol Metab 2005;90:4888-94
32. Ahrén 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
33. Jones-Leone AR, Yu T, Barilla D, et al. Evidence for insulin independent suppression of glucagon secretion by LAF237 (Abstract 8001. Diabetologia 2004;47(Suppl):A289
34. Ahrén B, Mills D, Gomis R, 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
35. Balas B, Baig MR, Watson C, et al. The dipeptidyl peptidase IV inhibitor vildagliptin suppresses endogenous glucose production and enhances islet function after single-close administration in Type 2 diabetic patients. J Clin Endocrinol Metab 2007;92:1249-55
36. Pi-Sunyer FY, Schweizer A, Mills D, Dejager S. Efficacy and tolerability of vildagliptin monotherapy in drug-naive patients with Type 2 diabetes. Diabetes Res Clin Pract 2007;76:132-8
37. Dejager S, Razac S, Foley JE, 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 2007;39:218-23
38. Rosenstock J, Baron MA, Dejager S, et al. 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
39. 1c over one year in drug-naive patients with Type 2 diabetes. Diabet Med 2007;24(9):955-61
40. Bosi E, Camisasca R-P, Collober C, et al. 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
41. Garber AJ, Camisasca R-P, Jauffret S, Baron MA. Efficacy and tolerability of vildagliptin added to a sulfonylurea (SU) in patients with Type 2 diabetes (T2DM) [Abstract 501-P]. Diabetes 2007;56(Suppl):A134
42. Garber AJ, Schweizer A, Baron MA, et al. 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 2007;9:166-74
43. Fonseca V, Schweizer A, Albrecht D, et al. Addition of vildagliptin to insulin improves glycaemic control in Type 2 diabetes. Diabetologia 2007;50:1148-55
44. Rosenstock J, Baron MA, Camisasca R-P, et al. Efficacy and tolerability of initial combination therapy with vildagliptin and pioglitazone compared with component monotherapy in patients with Type 2 diabetes. Diabetes Obes Metab 2007;9:175-85
45. Nesto RW, Bell D, Bonow RO, et al. Thiazolidinedione use, fluid retention, and congestive heart failure: a consensus statement from the American Heart Association. Diabetes Care 2004;27:256-63