Clinical Trial to Investigate the Pharmacokinetics/Pharmacodynamics of Sitagliptin

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

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

Conditions
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Diabetes Mellitus

Intervention / Treatment
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* Drug: Sitagliptin


Participation Criteria
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Eligibility Criteria
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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

Ages Eligible for Study
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Minimum Age: 20 Years
Maximum Age: 50 Years

Sexes Eligible for Study
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Male

Accepts Healthy Volunteers
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Accepts Healthy Volunteers

Study Plan
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How is the study designed?
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Design Details

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


Arms and Interventions

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

What is the study measuring?
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Primary Outcome Measures

| Outcome Measure | Measure Description | 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 |