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

• Published in: Clinical therapeutics Vol. 28; no. 1; pp. 55 - 72
• Main Authors: Bergman, Arthur J., Stevens, Catherine, Zhou, YanYan, Yi, Bingming, Laethem, Martine, De Smet, Marina, Snyder, Karen, Hilliard, Deborah, Tanaka, Wesley, Zeng, Wei, Tanen, Michael, Wang, Amy Q., Chen, Li, Winchell, Gregory, Davies, Michael J., Ramael, Steven, Wagner, John A., Herman, Gary A.
• Format: Journal Article
• Language: English
• Published: Belle Mead, NJ EM Inc USA 2006; Excerpta Medica; Elsevier Limited
• Subjects: Administration, Oral; Adolescent; Adult; antihyperglycemic agents; Biological and medical sciences; Blood Glucose - drug effects; Blood Glucose - metabolism; Diabetes; Diabetes Mellitus, Type 2 - blood; Diabetes Mellitus, Type 2 - drug therapy; Diabetes. Impaired glucose tolerance; Dipeptidyl Peptidase 4 - blood; Dipeptidyl Peptidase 4 - drug effects; dipeptidyl peptidase-IVinhibitor; Dose-Response Relationship, Drug; Double-Blind Method; DPP-IV; Drug dosages; Endocrine pancreas. Apud cells (diseases); Endocrinopathies; Enzyme-Linked Immunosorbent Assay; Etiopathogenesis. Screening. Investigations. Target tissue resistance; Follow-Up Studies; Glucagon; Glucagon-Like Peptide 1 - blood; Glucose; Humans; incretins; Insulin-Like Growth Factor Binding Protein 3 - blood; Insulin-Like Growth Factor I - metabolism; Male; Medical sciences; Metabolism; Metabolites; Middle Aged; MK-0431; Pharmacokinetics; Pharmacology. Drug treatments; Polypeptides; Pyrazines - administration & dosage; Pyrazines - pharmacokinetics; Reference Values; sitagliptin; Sitagliptin Phosphate; Triazoles - administration & dosage; Triazoles - pharmacokinetics; type 2 diabetes; incretins; sitagliptin; type 2 diabetes; DPP-IV; antihyperglycemic agents; MK-0431; dipeptidyl peptidase-IVinhibitor; Endocrinopathy; Type 2 diabetes; Dipeptidyl-peptidase IV; Human; dipeptidyl peptidase- IV inhibitor; Healthy subject; Enzyme; Oral administration; Metabolic diseases; Biological activity; Multiple dose; Peptidases; Hypoglycemic agent; Randomization; Placebo; Double blind study; Hydrolases; Inhibitor; Pharmacokinetics

Dipeptidyl peptidase-IV (DPP-IV) inhibitorsrepresent a new class of oral antihyperglycemic agents. Sitagliptin is an orally active and selective DPP-IV inhibitor currently in Phase III development for the treatment of type 2 diabetes mellitus. The aim of this study was to assess the pharmacokinetic...