The objective of this trial was to investigate safety, tolerability, and pharmacokinetics of BI 201335 ZW after administration of single rising doses from 40 mg to 480 mg of BI 201335 NA in healthy Japanese male volunteers.
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
TREATMENT
Masking
DOUBLE
Enrollment
50
Number of patients with abnormal findings in physical examination
Time frame: Baseline and within 7 days after last trial procedure
Number of patients with clinically significant changes in vital signs (blood pressure, pulse rate)
Time frame: Baseline, pre-dose and 1, 2, 3, 4, 6, 8, 12, 24, 48, 72 and 96 hours post-dose and day 12
Number of patients with abnormal findings in 12-lead electrocardiography (ECG)
Time frame: Baseline, pre-dose and 1, 2, 4, 6, 8, 24, 48, 72 and 96 hours post-dose and day 12
Number of patients with abnormal changes in laboratory tests (haematology, clinical chemistry, and urinalysis)
Time frame: Baseline, pre-dose and 24, 48, 72 and 96 hours post-dose and day 12
Number of patients with adverse events
Time frame: up to day 12
Assessment of tolerability by the investigator on a 4-point scale
Time frame: day 12 (within 7 days after last trial procedure)
Cmax (maximum concentration of the analyte in plasma)
Time frame: pre-dose and 1, 2, 3, 4, 6, 8, 10, 12, 16, 24, 36, 48, 72 and 96 hours post-dose
tmax (time from dosing to maximum concentration of the analyte in plasma)
Time frame: pre-dose and 1, 2, 3, 4, 6, 8, 10, 12, 16, 24, 36, 48, 72 and 96 hours post-dose
AUC0-∞ (area under the concentration time curve of the analyte in plasma over the time interval from 0 extrapolated to infinity)
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Time frame: pre-dose and 1, 2, 3, 4, 6, 8, 10, 12, 16, 24, 36, 48, 72 and 96 hours post-dose
AUC0-tz (area under the concentration-time curve of the analyte in plasma over the time interval from 0 to the last quantifiable data point)
Time frame: pre-dose and 1, 2, 3, 4, 6, 8, 10, 12, 16, 24, 36, 48, 72 and 96 hours post-dose
λz (terminal elimination rate constant in plasma)
Time frame: pre-dose and 1, 2, 3, 4, 6, 8, 10, 12, 16, 24, 36, 48, 72 and 96 hours post-dose
t1/2 (terminal half-life of the analyte in plasma)
Time frame: pre-dose and 1, 2, 3, 4, 6, 8, 10, 12, 16, 24, 36, 48, 72 and 96 hours post-dose
MRTpo (mean residence time of the analyte in the body after po administration)
Time frame: pre-dose and 1, 2, 3, 4, 6, 8, 10, 12, 16, 24, 36, 48, 72 and 96 hours post-dose
CL/F (apparent clearance of the analyte in the plasma after oral administration)
Time frame: pre-dose and 1, 2, 3, 4, 6, 8, 10, 12, 16, 24, 36, 48, 72 and 96 hours post-dose
Vz/F (apparent volume of distribution during the terminal phase λz following an oral administration)
Time frame: pre-dose and 1, 2, 3, 4, 6, 8, 10, 12, 16, 24, 36, 48, 72 and 96 hours post-dose
Aet1-t2 (amount of analyte that is eliminated in urine from the time point t1 to time point t2)
Time frame: 0-4, 4-12, 12-24, 24-48, 48-72 and 72-96 hours post-dose
fet1-t2 (fraction of analyte eliminated in urine from time point t1 to time point t2)
Time frame: 0-4, 4-12, 12-24, 24-48, 48-72 and 72-96 hours post-dose
CLR,t1-t2 (renal clearance of the analyte from the time point t1 until the time point t2)
Time frame: 0-4, 4-12, 12-24, 24-48, 48-72 and 72-96 hours post-dose