Clinical Trial to Investigate the Pharmacokinetics/Pharmacodynamics of Sitagliptin

Multiple-dose, Dose Escalation Study to Investigate the Pharmacokinetics/Pharmacodynamics of Sitagliptin in Healthy Male Volunteers

The purpose of this study is to investigate the pharmacokinetics and pharmacodynamics of sitagliptin in healthy volunteers.

Study Overview

• Status: Completed
• Conditions: Diabetes Mellitus
• Intervention / Treatment: Drug: Sitagliptin

• Study Type: Interventional
• Enrollment (Anticipated): 12
• Phase: Phase 1

Contacts and Locations

Study Locations

• Korea, Republic of
  • Seoul, Korea, Republic of, 110-744
    • Clinical Trials Center; Seoul National University Hospital

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 20 years to 50 years (Adult)
• Accepts Healthy Volunteers: Yes
• Genders Eligible for Study: Male

Description

Inclusion Criteria:

• Healthy male subjects aged 20 - 50 years
• A body mass index (BMI) in the range 17-28 kg/m2
• Fasting plasma glucose levels in the range 70-110 mg/dL
• Sufficient ability to understand the nature of the study and any hazards of participating in it
• Provide written informed consent after being fully informed about the study procedures

Exclusion Criteria:

• Presence or history of severe adverse reaction to any drug (e.g., sitagliptin) or a history of severe allergic disease
• Clinically relevant abnormal medical history that could interfere with the objectives of the study
• A subject who has the following screening laboratory test results; creatinine clearance (calculated by Cockcroft-Gault equation) < 80 mL/min
• History of gastrointestinal disease or surgery (except simple appendectomy or repair of hernia), which can influence the absorption of the study drug
• A subject whose SBP is over 150 mmHg or below 100 mmHg and DBP is over 95 mmHg or below 65 mmHg
• Presence or history of drug abuse
• Participation in other clinical trial within 2 months
• Use of a prescription medicine, herbal medicine within 2 weeks or over-the-counter medication within 1 week before first dose
• Blood donation during 2 months or apheresis during 1 month before the study
• Presence or history of alcohol abuse
• Users of nicotine-containing substances within the previous three months
• Use of grapefruit juice, alcohol or smoking during restriction period
• Subject judged not eligible for study participation by investigator

Study Plan

How is the study designed?

Design Details

• Allocation: Randomized
• Interventional Model: Crossover Assignment
• Masking: None (Open Label)

Number of Arms

3

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Other: Sitagliptin 25mg; Repeated administrations for 4 days	Drug: Sitagliptin; Dosage form: 25mg, 50mg ,100mg Amount: 25mg, 50mg, 100mg Frequency and duration: once a day, for 4 days, including 5 days washout periods
Other: Sitagliptin 50mg; Repeated administrations for 4 days	Drug: Sitagliptin; Dosage form: 25mg, 50mg ,100mg Amount: 25mg, 50mg, 100mg Frequency and duration: once a day, for 4 days, including 5 days washout periods
Other: Sitagliptin 100mg; Repeated administrations for 4 days	Drug: Sitagliptin; Dosage form: 25mg, 50mg ,100mg Amount: 25mg, 50mg, 100mg Frequency and duration: once a day, for 4 days, including 5 days washout periods

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Time Frame
To evaluate the pharmacokinetics after repeated administrations of sitagliptin 25, 50 and 100 mg	Pre-dose and 0.5, 1, 2, 4, 6, 8, 10, 12, 16, 24, 36, 48 hours after drug administration
To evaluate the pharmacodynamics (activity of Dipeptidyl peptidase-IV enzyme) after repeated administrations of sitagliptin 25, 50 and 100 mg	Pre-dose and 0.5, 1, 2, 4, 6, 8, 10, 12, 16, 24, 36, 48 hours after drug administration

Collaborators and Investigators

• Sponsor: Seoul National University Hospital
• Investigators: Principal Investigator: Kyung-Sang Yu, MD, PhD, Seoul National University College of Medicine and Hospital

Study record dates

Study Major Dates

• Study Start: December 1, 2008
• Primary Completion (Actual): September 1, 2009

Study Registration Dates

• First Submitted: August 14, 2009
• First Submitted That Met QC Criteria: August 14, 2009
• First Posted (Estimate): August 17, 2009

Study Record Updates

• Last Update Posted (Estimate): February 23, 2011
• Last Update Submitted That Met QC Criteria: February 19, 2011
• Last Verified: February 1, 2011

More Information

Terms related to this study

• Additional Relevant MeSH Terms: Hypoglycemic Agents; Physiological Effects of Drugs; Molecular Mechanisms of Pharmacological Action; Enzyme Inhibitors; Hormones; Hormones, Hormone Substitutes, and Hormone Antagonists; Protease Inhibitors; Incretins; Dipeptidyl-Peptidase IV Inhibitors; Sitagliptin Phosphate
• Other Study ID Numbers: SNUCPT09_Sitagliptin