The objective of the current study is to investigate safety, tolerability, and pharmacokinetics of BI 201335 ZW following administration of single rising doses from 5 mg to 1500 mg. In addition Two stage intra-subject bioavailability comparison of 600 mg BI 201335 ZW as a liquid formulation given with and without food.
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
TREATMENT
Masking
DOUBLE
Enrollment
8
Number of patients with abnormal findings in physical examination
Time frame: Baseline, day 3 of each treatment period, within 8 days after last administration
Number of patients with clinically significant changes in vital signs
Time frame: Baseline, day 1-3 of each treatment period, within 8 days after last administration
Number of patients with clinically significant changes in 12-lead ECG (electrocardiogram)
Time frame: Baseline, day 1, 2 in treatment period, within 8 days after last administration
Number of patients with abnormal changes in laboratory parameters
Time frame: Baseline, day 1-3 of each treatment period, within 8 days after last administration
Number of patients with adverse events
Time frame: up to 13 days
Assessment of tolerability by investigator on a 4-point scale
Time frame: on day 3 of each treatment period
Cmax (maximum concentration of the analyte in plasma)
Time frame: pre-dose and 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12, 15, 24, 30, 36 and 48 hours post-dose
tmax (time from dosing to maximum concentration)
Time frame: pre-dose and 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12, 15, 24, 30, 36 and 48 hours post-dose
AUC0-∞ (area under the concentration time curve of the analyte in plasma over the time interval from 0 extrapolated to infinity)
Time frame: pre-dose and 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12, 15, 24, 30, 36 and 48 hours post-dose
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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 last quantifiable data point)
Time frame: pre-dose and 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12, 15, 24, 30, 36 and 48 hours post-dose
λz (terminal elimination rate constant in plasma)
Time frame: pre-dose and 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12, 15, 24, 30, 36 and 48 hours post-dose
t1/2 (terminal half-life of the analyte in plasma)
Time frame: pre-dose and 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12, 15, 24, 30, 36 and 48 hours post-dose
MRTpo (Mean residence time of the analyte in the body after oral administration)
Time frame: pre-dose and 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12, 15, 24, 30, 36 and 48 hours post-dose
CL/F (apparent clearance of the analyte in the plasma after oral administration)
Time frame: pre-dose and 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12, 15, 24, 30, 36 and 48 hours post-dose
Vz/F (apparent volume of distribution during the terminal phase λz following an oral dose)
Time frame: pre-dose and 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12, 15, 24, 30, 36 and 48 hours post-dose