The objective of this study was to investigate the safety, tolerability, and pharmacokinetics of BI 201335 NA following administration of single rising doses from 4 mg to 1200 mg. In addition, the food effect on the bioavailability of BI 201335 NA (480 mg) was investigated.
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
TREATMENT
Masking
SINGLE
Enrollment
74
Number of patients with abnormal findings in physical examination
Time frame: up to 12 days
Number of patients with clinically significant changes in vital signs (blood pressure, pulse rate)
Time frame: up to 12 days
Number of patients with abnormal findings in 12-lead ECG (electrocardiogram)
Time frame: up to 12 days
Number of patients with abnormal changes in laboratory tests (haematology, clinical chemistry and urinalysis)
Time frame: up to 12 days
Number of patients with adverse events
Time frame: up to 12 days
Assessment of tolerability by investigator on a 4-point scale
Time frame: within 7 days after last trial procedure
Cmax (maximum concentration of the analyte in plasma)
Time frame: Pre-dose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 30, 36, 48, 60, 72, 84, 96 hours post-dose
tmax (time from dosing to maximum concentration)
Time frame: Pre-dose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 30, 36, 48, 60, 72, 84, 96 hours post-dose
AUC0-infinity (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, 3, 4, 6, 8, 12, 16, 24, 30, 36, 48, 60, 72, 84, 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)
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Time frame: Pre-dose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 30, 36, 48, 60, 72, 84, 96 hours post-dose
λz (terminal elimination rate constant in plasma)
Time frame: Pre-dose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 30, 36, 48, 60, 72, 84, 96 hours post-dose
t1/2 (terminal half-life of the analyte in plasma)
Time frame: Pre-dose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 30, 36, 48, 60, 72, 84, 96 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, 3, 4, 6, 8, 12, 16, 24, 30, 36, 48, 60, 72, 84, 96 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, 3, 4, 6, 8, 12, 16, 24, 30, 36, 48, 60, 72, 84, 96 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, 3, 4, 6, 8, 12, 16, 24, 30, 36, 48, 60, 72, 84, 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: Pre-dose and 0-4, 4-12, 12-24, 24-48 hours post-dose in the single rising dose phase
fet1-t2 (fraction of analyte eliminated in urine from time point t1 to time point t2)
Time frame: Pre-dose and 0-4, 4-12, 12-24, 24-48 hours post-dose in the single rising dose phase
CLR,t1-t2 (renal clearance of the analyte from the time point t1 until the time point t2)
Time frame: Pre-dose and 0-4, 4-12, 12-24, 24-48 hours post-dose in the single rising dose phase