Evaluation of pharmacokinetic parameters and dipeptidyl peptidase-4 inhibition following single doses of sitagliptin in healthy, young Japanese males

British Journal of Clinical Pharmacology

Volumn 71, Issue 3, 2011, Pages 429-436

  Herman, Gary A ^a   Mistry, Goutam C ^a   Yi, Bingming ^a   Bergman, Arthur J ^a   Wang, Amy Q ^a   Zeng, Wei ^a   Chen, Li ^a   Snyder, Karen ^a   Ruckle, Jon L ^b   Larson, Patrick J ^a   Davies, Michael J ^a   Langdon, Ronald B ^a   Gottesdiener, Keith M ^a   Wagner, John A ^a  

^a Radiant Research ^*

^b MERCK RESEARCH LABORATORIES   (United States)

Author keywords

DPP 4 inhibitor; MK 0431; Race

Indexed keywords

DIPEPTIDYL PEPTIDASE IV; PLACEBO; SITAGLIPTIN;

ADULT; ARTICLE; DROWSINESS; DRUG BLOOD LEVEL; DRUG DOSE INCREASE; DRUG EXCRETION; DRUG HALF LIFE; DRUG SAFETY; DRUG TOLERABILITY; DRUG URINE LEVEL; DRUG WITHDRAWAL; ENZYME INHIBITION; HEADACHE; HUMAN; HUMAN EXPERIMENT; HYPOGLYCEMIA; JAPANESE; MALE; NON INSULIN DEPENDENT DIABETES MELLITUS; NORMAL HUMAN; PRIORITY JOURNAL; SINGLE DRUG DOSE; SOMNOLENCE;

ADMINISTRATION, ORAL; ADULT; ASIAN CONTINENTAL ANCESTRY GROUP; DIABETES MELLITUS, TYPE 2; DIPEPTIDYL-PEPTIDASE IV INHIBITORS; DOSE-RESPONSE RELATIONSHIP, DRUG; DOUBLE-BLIND METHOD; HUMANS; HYPOGLYCEMIC AGENTS; MALE; MIDDLE AGED; PYRAZINES; RESEARCH DESIGN; STATISTICS AS TOPIC; TRIAZOLES; YOUNG ADULT;

EID: 79251623618     PISSN: 03065251     EISSN: 13652125     Source Type: Journal    
DOI: 10.1111/j.1365-2125.2010.03852.x     Document Type: Article

References (27)

1. Herman GA, Stein PP, Thornberry NA, Wagner JA. Dipeptidyl peptidase-4 inhibitors for the treatment of type 2 diabetes: focus on sitagliptin. Clin Pharmacol Ther 2007; 81: 761-7.
2. Herman GA, Bergman A, Stevens C, Kotey P, Yi B, Zhao P, Dietrich B, Golor G, Schrodter A, Keymeulen B, Lasseter KC, Kipnes MS, Snyder K, Hilliard D, Tanen M, Cilissen C, De Smet M, de Lepeleire I, Van Dyck K, Wang AQ, Zeng W, Davies MJ, Tanaka W, Holst JJ, Deacon CF, Gottesdiener KM, Wagner JA. Effect of single oral doses of sitagliptin, a dipeptidyl peptidase-4 inhibitor, on incretin and plasma glucose levels following an oral glucose tolerance test in patients with type 2 diabetes. J Clin Endocrinol Metab 2006; 91: 4612-9.
3. Drucker DJ, Nauck MA. The incretin system: glucagon-like peptide-1 receptor agonists and dipeptidyl peptidase-4 inhibitors in type 2 diabetes. Lancet 2006; 368: 1696-705.
4. Karasik A, Aschner P, Katzeff H, Davies MJ, Stein PP. Sitagliptin, a DPP-4 inhibitor for the treatment of patients with type 2 diabetes: a review of recent clinical trials. Curr Med Res Opin 2008; 24: 489-96.
5. Lyseng-Williamson KA. Sitagliptin. Drugs 2007; 67: 587-97.
6. Herman GA, Stevens C, Van Dyck K, Bergman A, Yi B, De Smet M, Snyder K, Hilliard D, Tanen M, Tanaka W, Wang AQ, Zeng W, Musson D, Winchell G, Davies MJ, Ramael S, Gottesdiener KM, Wagner JA. Pharmacokinetics and pharmacodynamics of single doses of sitagliptin, an inhibitor of dipeptidyl peptidase-IV, in healthy subjects. Clin Pharmacol Ther 2005; 78: 675-88.
7. Bergman AJ, Stevens C, Zhou YY, Yi B, Laethem M, De Smet M, Snyder K, Hilliard D, Tanaka W, Zeng W, Tanen M, Wang AQ, Chen L, Winchell G, Davies MJ, Ramael S, Wagner JA, Herman GA. 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 2006; 28: 55-72.
8. Herman GA, Bergman A, Liu F, Stevens C, Wang AQ, Zeng W, Chen L, Snyder K, Hilliard D, Tanen M, Tanaka W, Meehan AG, Lasseter K, Dilzer S, Blum R, Wagner JA. Pharmacokinetics and pharmacodynamic effects of the oral DPP-4 inhibitor sitagliptin in middle-aged obese subjects. J Clin Pharmacol 2006; 46: 876-86.
9. Vincent SH, Reed JR, Bergman AJ, Elmore CS, Zhu B, Xu S, Ebel D, Larson P, Zeng W, Chen L, Dilzer S, Lasseter K, Gottesdiener K, Wagner JA, Herman GA. Metabolism and excretion of the dipeptidyl peptidase 4 inhibitor [14C]sitagliptin in humans. Drug Metab Dispos 2007; 35: 533-8.
10. Bergman AJ, Cote J, Yi B, Marbury T, Swan SK, Smith W, Gottesdiener K, Wagner J, Herman GA. Effect of renal insufficiency on the pharmacokinetics of sitagliptin, a dipeptidyl peptidase-4 inhibitor. Diabetes Care 2007; 30: 1862-4.
11. Chu XY, Bleasby K, Yabut J, Cai X, Chan GH, Hafey MJ, Xu S, Bergman AJ, Braun MP, Dean DC, Evers R. Transport of the dipeptidyl peptidase-4 inhibitor sitagliptin by human organic anion transporter 3, organic anion transporting polypeptide 4C1, and multidrug resistance P-glycoprotein. J Pharmacol Exp Ther 2007; 321: 673-83.
12. Ieiri I, Takane H, Hirota T, Otsubo K, Higuchi S. Genetic polymorphisms of drug transporters: pharmacokinetic and pharmacodynamic consequences in pharmacotherapy. Expert Opin Drug Metab Toxicol 2006; 2: 651-74.
13. Sissung TM, Baum CE, Kirkland CT, Gao R, Gardner ER, Figg WD. Pharmacogenetics of membrane transporters: an update on current approaches. Mol Biotechnol 2010; 44: 152-67.
14. Zeng W, Musson DG, Fisher AL, Wang AQ. Determination of MK-0431 in human plasma using high turbulence liquid chromatography online extraction and tandem mass spectrometry. Rapid Commun Mass Spectrom 2006; 20: 1169-75.
15. Zeng W, Musson DG, Fisher AL, Chen L, Schwartz MS, Woolf EJ, Wang AQ. Determination of sitagliptin in human urine and hemodialysate using turbulent flow online extraction and tandem mass spectrometry. J Pharm Biomed Anal 2008; 46: 534-42.
16. 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: 141-51.
17. Segel IH. Enzyme Kinetics: Behavior and Analysis of Rapid Equilibrium and Steady-State Enzyme Systems. New York: Wiley-Interscience, 1975.
18. Alba M, Sheng D, Guan Y, Williams-Herman D, Larson P, Sachs JR, Thornberry N, Herman G, Kaufman KD, Goldstein BJ. Sitagliptin 100mg daily effect on DPP-4 inhibition and compound-specific glycemic improvement. Curr Med Res Opin 2009; 25: 2507-14.
19. Hartley HO. The modified Gauss-Newton method for the fitting of non-linear regression functions by least squares. Technometrics 1961; 3: 269-28.
20. Scott R, Wu M, Sanchez M, Stein PP. 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 2007; 61: 171-80.
21. Hanefeld M, Herman GA, Wu M, Mickel C, Sanchez M, Stein PP. Once-daily sitagliptin, a dipeptidyl peptidase-4 inhibitor, for the treatment of patients with type 2 diabetes. Curr Med Res Opin 2007; 23: 1329-39.
22. Raz I, Hanefeld M, Xu L, Caria C, Williams-Herman D, Khatami H. Efficacy and safety of the dipeptidyl peptidase-4 inhibitor sitagliptin as monotherapy in patients with type 2 diabetes mellitus. Diabetologia 2006; 49: 2564-71.
23. Aschner P, Kipnes MS, Lunceford JK, Sanchez M, Mickel C, Williams-Herman DE. Effect of the dipeptidyl peptidase-4 inhibitor sitagliptin as monotherapy on glycemic control in patients with type 2 diabetes. Diabetes Care 2006; 29: 2632-7.
24. Williams-Herman D, Engel SS, Round E, Johnson J, Golm GT, Guo H, Musser B, Davies MJ, Kaufman KD, Goldstein BJ. Safety and tolerability of sitagliptin in clinical studies: a pooled analysis of data from 10246 patients with type 2 diabetes. BMC Endocr Disord 2010; 10: 7.
25. Baggio LL, Drucker DJ. Biology of incretins: GLP-1 and GIP. Gastroenterology 2007; 132: 2131-57.
26. Myers RP, Shaffer EA, Beck PL. Gallbladder polyps: epidemiology, natural history and management. Can J Gastroenterol 2002; 16: 187-94.
27. Aragon G, Younossi ZM. When and how to evaluate mildly elevated liver enzymes in apparently healthy patients. Cleve Clin J Med 2010; 77: 195-204.