Hormonal and metabolic effects of morning or evening dosing of the dipeptidyl peptidase IV inhibitor vildagliptin in patients with type 2 diabetes

British Journal of Clinical Pharmacology

Volumn 70, Issue 1, 2010, Pages 34-42

  He, Yan Ling ^a   Valencia, Jessica ^b   Zhang, Yiming ^b   Schwartz, Sherwyn L ^c   Ligueros Saylan, Monica ^b   Foley, James ^b   Dole, William P ^a  

^a NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH   (United States)

^b NOVARTIS PHARMA AG   (Switzerland)

^c Diabetes and Glandular Disease Clinic   (United States)

Author keywords

DPP 4; GLP 1; Pharmacokinetics; Type 2 diabetes; Vildagliptin

Indexed keywords

DIPEPTIDYL PEPTIDASE IV; GLUCAGON LIKE PEPTIDE 1; GLUCOSE; INSULIN; PLACEBO; VILDAGLIPTIN;

ADULT; AGED; AREA UNDER THE CURVE; ARTICLE; BLOOD SAMPLING; CLINICAL ARTICLE; CLINICAL TRIAL; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; CROSSOVER PROCEDURE; DIABETIC PATIENT; DOSAGE SCHEDULE COMPARISON; DOUBLE BLIND PROCEDURE; DRUG BLOOD LEVEL; DRUG DOSE REGIMEN; DRUG EFFECT; DRUG INDUCED HEADACHE; DRUG SAFETY; DRUG TOLERABILITY; ENZYME ACTIVITY; ENZYME INHIBITION; EVENING DOSAGE; FEMALE; GLUCOSE BLOOD LEVEL; HUMAN; INSULIN BLOOD LEVEL; MALE; MAXIMUM PLASMA CONCENTRATION; MORNING DOSAGE; NON INSULIN DEPENDENT DIABETES MELLITUS; PARAMETER; POSTPRANDIAL STATE; PRIORITY JOURNAL; RANDOMIZED CONTROLLED TRIAL; SORE THROAT; TIME TO MAXIMUM PLASMA CONCENTRATION; TREATMENT OUTCOME;

ADAMANTANE; ADOLESCENT; ADULT; AGED; BLOOD GLUCOSE; DIABETES MELLITUS, TYPE 2; DIPEPTIDYL-PEPTIDASE IV INHIBITORS; DOUBLE-BLIND METHOD; FEMALE; HUMANS; INSULIN; MALE; MIDDLE AGED; NITRILES; PYRROLIDINES; TIME FACTORS; TREATMENT OUTCOME; YOUNG ADULT;

EID: 77953503929     PISSN: 03065251     EISSN: 13652125     Source Type: Journal    
DOI: 10.1111/j.1365-2125.2010.03652.x     Document Type: Article

References (32)

1. Pratley RE, Salsali A. Inhibition of DPP-4: a new therapeutic approach for the treatment of type 2 diabetes. Curr Med Res Opin 2007 23 : 919 931.
2. Holst JJ, Deacon CF. Inhibition of the activity of dipeptidyl-peptidase IV as a treatment for type 2 diabetes. Diabetes 1998 47 : 1663 1670.
3. Kieffer TJ, Habener JF. The glucagon-like peptides. Endocr Rev 1999 20 : 876 913.
4. Gutniak M, Orskov C, Holst JJ, Ahren B, Efendic S. Antidiabetogenic 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.
5. Creutzfeldt WO, Kleine N, Willms B, Orskov C, Holst JJ, Nauck MA. Glucagonostatic actions and reduction of fasting hyperglycemia by exogenous glucagon-like peptide I (7-36) amide in type I diabetic patients. Diabetes Care 1996 19 : 580 586.
6. Naslund E, Bogefors J, Skogar S, Gryback P, Jacobsson H, Holst JJ, Hellstrom PM. GLP-1 slows solid gastric emptying and inhibits insulin, glucagon, and PYY release in humans. Am J Physiol 1999 277 : R910 6.
7. Gutzwiller JP, Drewe J, Goke B, Schmidt H, Rohrer B, Lareida J, Beglinger C. Glucagon-like peptide-1 promotes satiety and reduces food intake in patients with diabetes mellitus type 2. Am J Physiol 1999 276 : R1541 4.
8. Vilsboll T, Krarup T, Deacon CF, Madsbad S, Holst JJ. Reduced postprandial concentrations of intact biologically active glucagon-like peptide 1 in type 2 diabetic patients. Diabetes 2001 50 : 609 613.
9. Nauck MA, Heimesaat MM, Orskov C, Holst JJ, Ebert R, Creutzfeldt W. 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 : 301 307.
10. He YL, Wang Y, Bullock JM, Deacon CF, Holst JJ, Dunning BE, Ligueros-Saylan M, Foley JE. Pharmacodynamics of vildagliptin in patients with type 2 diabetes during OGTT. J Clin Pharmacol 2007 47 : 633 641. (Pubitemid 46632151)
11. He YL, Serra D, Wang Y, Campestrini J, Riviere GJ, Deacon CF, Holst JJ, Schwartz S, Nielsen JC, Ligueros-Saylan M. Pharmacokinetics and pharmacodynamics of vildagliptin in patients with type 2 diabetes mellitus. Clin Pharmacokinet 2007 46 : 577 588. (Pubitemid 47025358)
12. Villhauer EB, Brinkman JA, Naderi GB, Burkey BF, Dunning BE, Prasad K, Mangold BL, Russell ME, Hughes TE. 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 2789.
13. Vella A, Bock G, Giesler PD, Burton DB, Serra DB, Saylan LM, Dunning BE, Foley JE, Rizza RA, Camilleri M. Effects of dipeptidyl peptidase-4 inhibition on gastrointestinal function, meal appearance and glucose metabolism in type 2 diabetes. Diabetes 2007 56 : 1475 1480.
14. Pratley RE, Schweizer A, Rosenstock J, Foley JE, Banerji MA, Pi-Sunyer FX, Mills D, Dejager S. Robust improvements in fasting and prandial measures of beta-cell function with vildagliptin in drug-naive patients: analysis of pooled vildagliptin monotherapy database. Diabetes Obes Metab 2008 10 : 931 938.
15. Pratley RE, Jauffret-Kamel S, Galbreath E, Holmes D. Twelve-week monotherapy with the DPP-4 inhibitor vildagliptin improves glycemic control in subjects with type 2 diabetes. Horm Metab Res 2006 38 : 423 428.
16. Pi-Sunyer FX, 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 : 132 138. (Pubitemid 46240373)
17. Pan C, Yang W, Barona JP, Wang Y, Niggli M, Mohideen P, Wang Y, Foley JE. Comparison of vildagliptin and acarbose monotherapy in patients with type 2 diabetes: a 24-week, double-blind, randomized trial. Diabet Med 2008 25 : 435 441.
18. Scherbaum WA, Schweizer A, Mari A, Nilsson PM, Lalanne G, Jauffret S, Foley JE. Efficacy and tolerability of vildagliptin in drug-naive patients with type 2 diabetes and mild hyperglycaemia. Diabetes Obes Metab 2008 10 : 675 682.
19. Garber AJ, Foley JE, Banerji MA, Ebeling P, Gudbjornsdottir S, Camisasca RP, Couturier A, Baron MA. Effects of vildagliptin on glucose control in patients with type 2 diabetes inadequately controlled with a sulphonylurea. Diabetes Obes Metab 2008 10 : 1047 1056.
20. Bosi E, Camisasca RP, Collober C, Rochotte E, Garber AJ. Effects of vildagliptin on glucose control over 24 weeks in patients with type 2 diabetes inadequately controlled with metformin. Diabetes Care 2007 30 : 890 895.
21. Fonseca V, Baron MA, Shao Q, Dejager S. Sustained efficacy and reduced hypoglycemia during one year of treatment with vildagliptin added to insulin in patients with type 2 diabetes mellitus. Horm Metab Res 2008 40 : 427 430.
22. Ahren B, Landin-Olsson M, Jansson PA, Svensson M, Holmes D, Schweizer A. 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.
23. 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 : 692 698.
24. Mari A, Sallas WM, He YL, Watson C, Ligueros-Saylan M, Dunning BE, Deacon CF, Holst JJ, Foley JE. Vildagliptin, a dipeptidyl peptidase-IV inhibitor, improves model-assessed beta-cell function in patients with type 2 diabetes. J Clin Endocrinol Metab 2005 90 : 4888 4894.
25. Kim D, Wang L, Beconi M, Eiermann GJ, Fisher MH, He H, Hickey GJ, Kowalchick JE, Leiting B, Lyons K, Marsilio F, McCann ME, Patel RA, Petrov A, Scapin G, Patel SB, Roy RS, Wu JK, Wyvratt MJ, Zhang BB, Zhu L, Thornberry NA, Weber AE. (2R)-4-oxo-4-[3-(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 2005 48 : 141 151.
26. Balas B, Baig MR, Watson C, Dunning BE, Ligueros-Saylan M, Wang Y, He YL, Darland C, Holst JJ, Deacon CF, Cusi K, Mari A, Foley JE, DeFronzo RA. 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.
27. He YL, Ligueros-Saylan M, Sunkara G, Sabo R, Zhao C, Wang Y, Campestrini J, Pommier F, Dole K, Marion A, Dole WP, Howard D. Vildagliptin, a novel dipeptidyl peptidase IV inhibitor, has no pharmacokinetic interactions with the antihypertensive agents amlodipine, valsartan, and ramipril in healthy subjects. J Clin Pharmacol 2008 48 : 85 95.
28. Serra D, He YL, Bullock J, Riviere GJ, Balez S, Schwartz S, Wang Y, Ligueros-Saylan M, Jarugula V, Dole WP. Evaluation of pharmacokinetic and pharmacodynamic interaction between the dipeptidyl peptidase IV inhibitor vildagliptin, glyburide and pioglitazone in patients with type 2 diabetes. Int J Clin Pharmacol Ther 2008 46 : 349 364. (Pubitemid 352005928)
29. He YL, Barilla D, Ligueros-Saylan M, Riviere GJ, Campestrini J, Pratapa P. The pharmacokinetics and DPP-4 inhibition of LAF237 in healthy volunteers. J Clin Pharmacol 2004 44 : 1212.
30. Sunkara G, Sabo R, Wang Y, He YL, Campestrini J, Howard D, Dole WP. Dose proportionality and the effect of food on vildagliptin, a novel dipeptidyl peptidase IV inhibitor, in healthy volunteers. J Clin Pharmacol 2007 47 : 1152 1158.
31. DeFronzo RA, Ferrannini E, Simonson DC. Fasting hyperglycemia in non-insulin-dependent diabetes mellitus: contributions of excessive hepatic glucose production and impaired tissue glucose uptake. Metabolism 1989 38 : 387 395.
32. Balschun D, Schuh J. Dipeptidyl-peptidase IV (DP IV): rhythmic changes of serum activity in mice. Pharmazie 1983 38 : 424.