Study to evaluate the safety, tolerability, pharmacokinetics, and pharmacodynamics of BI 10773 administered to healthy Japanese male subjects with single rising oral doses (1, 5, 10, 25, and 100 mg).
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
TREATMENT
Masking
DOUBLE
Enrollment
48
Number of patients with adverse events
Time frame: Up to 7 days
Number of patients with abnormal changes in laboratory parameters
Time frame: Baseline, day 2-4 and day 7
Number of patients with clinically significant changes in vital signs (blood pressure, pulse rate, and body temperature)
Time frame: Baseline, day 1-4 and day 7
Number of patients with clinical significant changes in 12-lead ECG (electrocardiogram)
Time frame: Baseline, day 1-4 and day 7
Assessment of tolerability on a 4-point scale
Time frame: Day 4
Cmax (maximum concentration of the analyte in plasma)
Time frame: Before and 10, 20, 30, 45 minutes and 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 14, 24, 34, 48 72 hours after administration of study drug
tmax (time from dosing to maximum concentration)
Time frame: Before and 10, 20, 30, 45 minutes and 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 14, 24, 34, 48 72 hours after administration of study drug
AUC0-∞ (area under the concentration-time curve of the analyte in plasma over the time interval from 0 extrapolated to infinity)
Time frame: Before and 10, 20, 30, 45 minutes and 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 14, 24, 34, 48 72 hours after administration of study drug
%AUCtz-∞ (the percentage of the AUC0-∞ that is obtained by extrapolation)
Time frame: Before and 10, 20, 30, 45 minutes and 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 14, 24, 34, 48 72 hours after administration of study drug
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AUC0-tz (area under the concentration-time curve of the analyte in plasma over the time interval from 0 to the time of the last quantifiable data point)
Time frame: Before and 10, 20, 30, 45 minutes and 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 14, 24, 34, 48 72 hours after administration of study drug
λz (terminal rate constant in plasma)
Time frame: Before and 10, 20, 30, 45 minutes and 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 14, 24, 34, 48 72 hours after administration of study drug
t1/2 (terminal half-life of the analyte in plasma)
Time frame: Before and 10, 20, 30, 45 minutes and 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 14, 24, 34, 48 72 hours after administration of study drug
MRTpo (mean residence time of the analyte in the body after po administration)
Time frame: Before and 10, 20, 30, 45 minutes and 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 14, 24, 34, 48 72 hours after administration of study drug
CL/F (total clearance of the analyte in the plasma after extravascular administration)
Time frame: Before and 10, 20, 30, 45 minutes and 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 14, 24, 34, 48 72 hours after administration of study drug
Vz/F (apparent volume of distribution during the terminal phase λz following an extravascular dose)
Time frame: Before and 10, 20, 30, 45 minutes and 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 14, 24, 34, 48 72 hours after administration of study drug
Aet1-t2 (amount of analyte that is eliminated in urine from the time point t1 to time point t2)
Time frame: 2 hours before and 0-2, 2-4, 4-6, 6-8, 8-12, 12-24, 24-34, 34-48, and 48-72 hours after administration of study drug
fet1-t2 (fraction of analyte eliminated in urine from time point t1 to time point t2)
Time frame: 2 hours before and 0-2, 2-4, 4-6, 6-8, 8-12, 12-24, 24-34, 34-48, and 48-72 hours after administration of study drug
CLR,t1-t2 (renal clearance of the analyte from the time point t1 until the time point t2)
Time frame: 2 hours before and 0-2, 2-4, 4-6, 6-8, 8-12, 12-24, 24-34, 34-48, and 48-72 hours after administration of study drug