Pharmacokinetics and pharmacodynamics of vildagliptin in patients with type 2 diabetes mellitus.

Research output: Contribution to journalJournal articleResearchpeer-review

Standard

Pharmacokinetics and pharmacodynamics of vildagliptin in patients with type 2 diabetes mellitus. / He, Yan-Ling; Serra, Denise; Wang, Yibin; Campestrini, Joelle; Riviere, Gilles-Jacques; Deacon, Carolyn F; Holst, Jens J; Schwartz, Sherwyn; Nielsen, Jace C; Ligueros-Saylan, Monica.

In: Clinical Pharmacokinetics, Vol. 46, No. 7, 2007, p. 577-88.

Research output: Contribution to journalJournal articleResearchpeer-review

Harvard

He, Y-L, Serra, D, Wang, Y, Campestrini, J, Riviere, G-J, Deacon, CF, Holst, JJ, Schwartz, S, Nielsen, JC & Ligueros-Saylan, M 2007, 'Pharmacokinetics and pharmacodynamics of vildagliptin in patients with type 2 diabetes mellitus.', Clinical Pharmacokinetics, vol. 46, no. 7, pp. 577-88.

APA

He, Y-L., Serra, D., Wang, Y., Campestrini, J., Riviere, G-J., Deacon, C. F., ... Ligueros-Saylan, M. (2007). Pharmacokinetics and pharmacodynamics of vildagliptin in patients with type 2 diabetes mellitus. Clinical Pharmacokinetics, 46(7), 577-88.

Vancouver

He Y-L, Serra D, Wang Y, Campestrini J, Riviere G-J, Deacon CF et al. Pharmacokinetics and pharmacodynamics of vildagliptin in patients with type 2 diabetes mellitus. Clinical Pharmacokinetics. 2007;46(7):577-88.

Author

He, Yan-Ling ; Serra, Denise ; Wang, Yibin ; Campestrini, Joelle ; Riviere, Gilles-Jacques ; Deacon, Carolyn F ; Holst, Jens J ; Schwartz, Sherwyn ; Nielsen, Jace C ; Ligueros-Saylan, Monica. / Pharmacokinetics and pharmacodynamics of vildagliptin in patients with type 2 diabetes mellitus. In: Clinical Pharmacokinetics. 2007 ; Vol. 46, No. 7. pp. 577-88.

Bibtex

@article{71886770ab4911ddb5e9000ea68e967b,
title = "Pharmacokinetics and pharmacodynamics of vildagliptin in patients with type 2 diabetes mellitus.",
abstract = "BACKGROUND: Vildagliptin is a dipeptidyl peptidase IV (DPP-4) inhibitor currently under development for the treatment of type 2 diabetes mellitus. OBJECTIVES: To assess the pharmacokinetic and pharmacodynamic characteristics and tolerability of vildagliptin at doses of 10 mg, 25 mg and 100 mg twice daily following oral administration in patients with type 2 diabetes. METHODS: Thirteen patients with type 2 diabetes were enrolled in this randomised, double-blind, double-dummy, placebo-controlled, four-period, crossover study. Patients received vildagliptin 10 mg, 25 mg and 100 mg as well as placebo twice daily for 28 days. RESULTS: Vildagliptin was absorbed rapidly (median time to reach maximum concentration 1 hour) and had a mean terminal elimination half-life ranging from 1.32 to 2.43 hours. The peak concentration and total exposure increased in an approximately dose-proportional manner. Vildagliptin inhibited DPP-4 (>90{\%}) at all doses and demonstrated a dose-dependent effect on the duration of inhibition. The areas under the plasma concentration-time curves of glucagon-like peptide-1 (GLP-1) [p < 0.001] and glucose-dependent insulinotropic peptide (GIP) [p < 0.001] were increased whereas postprandial glucagon was significantly reduced at the 25 mg (p = 0.006) and 100mg (p = 0.005) doses compared with placebo. As compared with placebo treatment, mean plasma glucose concentrations were decreased by 1.4 mmol/L with the vildagliptin 25 mg dosing regimen and by 2.5 mmol/L with the 100 mg dosing regimen, corresponding to a 10{\%} and 19{\%} reduction, respectively. Vildagliptin was generally well tolerated. CONCLUSION: Vildagliptin is likely to be a useful therapy for patients with type 2 diabetes based on the inhibition of DPP-4 and the subsequent increase in incretin hormones, GLP-1 and GIP, and the decrease in glucose and glucagon levels.",
author = "Yan-Ling He and Denise Serra and Yibin Wang and Joelle Campestrini and Gilles-Jacques Riviere and Deacon, {Carolyn F} and Holst, {Jens J} and Sherwyn Schwartz and Nielsen, {Jace C} and Monica Ligueros-Saylan",
note = "Keywords: Adamantane; Administration, Oral; Adult; Aged; Area Under Curve; Blood Glucose; Cross-Over Studies; Diabetes Mellitus, Type 2; Dose-Response Relationship, Drug; Double-Blind Method; Drug Administration Schedule; Female; Gastric Inhibitory Polypeptide; Glucagon-Like Peptide 1; Half-Life; Humans; Hypoglycemic Agents; Male; Middle Aged; Nausea; Nitriles; Pyrrolidines; Treatment Outcome; Vomiting",
year = "2007",
language = "English",
volume = "46",
pages = "577--88",
journal = "Clinical Pharmacokinetics",
issn = "0312-5963",
publisher = "Adis International Ltd",
number = "7",

}

RIS

TY - JOUR

T1 - Pharmacokinetics and pharmacodynamics of vildagliptin in patients with type 2 diabetes mellitus.

AU - He, Yan-Ling

AU - Serra, Denise

AU - Wang, Yibin

AU - Campestrini, Joelle

AU - Riviere, Gilles-Jacques

AU - Deacon, Carolyn F

AU - Holst, Jens J

AU - Schwartz, Sherwyn

AU - Nielsen, Jace C

AU - Ligueros-Saylan, Monica

N1 - Keywords: Adamantane; Administration, Oral; Adult; Aged; Area Under Curve; Blood Glucose; Cross-Over Studies; Diabetes Mellitus, Type 2; Dose-Response Relationship, Drug; Double-Blind Method; Drug Administration Schedule; Female; Gastric Inhibitory Polypeptide; Glucagon-Like Peptide 1; Half-Life; Humans; Hypoglycemic Agents; Male; Middle Aged; Nausea; Nitriles; Pyrrolidines; Treatment Outcome; Vomiting

PY - 2007

Y1 - 2007

N2 - BACKGROUND: Vildagliptin is a dipeptidyl peptidase IV (DPP-4) inhibitor currently under development for the treatment of type 2 diabetes mellitus. OBJECTIVES: To assess the pharmacokinetic and pharmacodynamic characteristics and tolerability of vildagliptin at doses of 10 mg, 25 mg and 100 mg twice daily following oral administration in patients with type 2 diabetes. METHODS: Thirteen patients with type 2 diabetes were enrolled in this randomised, double-blind, double-dummy, placebo-controlled, four-period, crossover study. Patients received vildagliptin 10 mg, 25 mg and 100 mg as well as placebo twice daily for 28 days. RESULTS: Vildagliptin was absorbed rapidly (median time to reach maximum concentration 1 hour) and had a mean terminal elimination half-life ranging from 1.32 to 2.43 hours. The peak concentration and total exposure increased in an approximately dose-proportional manner. Vildagliptin inhibited DPP-4 (>90%) at all doses and demonstrated a dose-dependent effect on the duration of inhibition. The areas under the plasma concentration-time curves of glucagon-like peptide-1 (GLP-1) [p < 0.001] and glucose-dependent insulinotropic peptide (GIP) [p < 0.001] were increased whereas postprandial glucagon was significantly reduced at the 25 mg (p = 0.006) and 100mg (p = 0.005) doses compared with placebo. As compared with placebo treatment, mean plasma glucose concentrations were decreased by 1.4 mmol/L with the vildagliptin 25 mg dosing regimen and by 2.5 mmol/L with the 100 mg dosing regimen, corresponding to a 10% and 19% reduction, respectively. Vildagliptin was generally well tolerated. CONCLUSION: Vildagliptin is likely to be a useful therapy for patients with type 2 diabetes based on the inhibition of DPP-4 and the subsequent increase in incretin hormones, GLP-1 and GIP, and the decrease in glucose and glucagon levels.

AB - BACKGROUND: Vildagliptin is a dipeptidyl peptidase IV (DPP-4) inhibitor currently under development for the treatment of type 2 diabetes mellitus. OBJECTIVES: To assess the pharmacokinetic and pharmacodynamic characteristics and tolerability of vildagliptin at doses of 10 mg, 25 mg and 100 mg twice daily following oral administration in patients with type 2 diabetes. METHODS: Thirteen patients with type 2 diabetes were enrolled in this randomised, double-blind, double-dummy, placebo-controlled, four-period, crossover study. Patients received vildagliptin 10 mg, 25 mg and 100 mg as well as placebo twice daily for 28 days. RESULTS: Vildagliptin was absorbed rapidly (median time to reach maximum concentration 1 hour) and had a mean terminal elimination half-life ranging from 1.32 to 2.43 hours. The peak concentration and total exposure increased in an approximately dose-proportional manner. Vildagliptin inhibited DPP-4 (>90%) at all doses and demonstrated a dose-dependent effect on the duration of inhibition. The areas under the plasma concentration-time curves of glucagon-like peptide-1 (GLP-1) [p < 0.001] and glucose-dependent insulinotropic peptide (GIP) [p < 0.001] were increased whereas postprandial glucagon was significantly reduced at the 25 mg (p = 0.006) and 100mg (p = 0.005) doses compared with placebo. As compared with placebo treatment, mean plasma glucose concentrations were decreased by 1.4 mmol/L with the vildagliptin 25 mg dosing regimen and by 2.5 mmol/L with the 100 mg dosing regimen, corresponding to a 10% and 19% reduction, respectively. Vildagliptin was generally well tolerated. CONCLUSION: Vildagliptin is likely to be a useful therapy for patients with type 2 diabetes based on the inhibition of DPP-4 and the subsequent increase in incretin hormones, GLP-1 and GIP, and the decrease in glucose and glucagon levels.

M3 - Journal article

C2 - 17596103

VL - 46

SP - 577

EP - 588

JO - Clinical Pharmacokinetics

JF - Clinical Pharmacokinetics

SN - 0312-5963

IS - 7

ER -

ID: 8416909