Study to investigate safety, tolerability, and pharmacokinetics of single rising peroral doses of BI 1744 CL.
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
TREATMENT
Masking
SINGLE
Enrollment
24
Number of patients with abnormal findings in physical examination
Time frame: Baseline, day 17
Number of patients with clinically significant changes in vital signs (blood pressure (BP), pulse rate (PR), respiration rate (RR), oral body temperature)
Time frame: Baseline, up to day 17
Number of patients with clinically relevant abnormal findings in 12-lead electrocardiogram (ECG)
Time frame: Baseline, up to day 17
Number of patients with clinically significant changes in clinical laboratory tests
Time frame: Baseline, up to day 17
Number of patients with Adverse events (AEs)
Time frame: 5 weeks
Assessment of tolerability by investigator on a 4-point scale
Time frame: Day 17
Cmax (maximum measured concentration of the analyte in plasma)
Time frame: pre-dose and 15, 30, 45 min, 1, 2, 3, 4, 6, 8, 10, 12, 24, 36 and 48 hours after drug administration
tmax (time from dosing to maximum measured concentration of the analyte in plasma)
Time frame: pre-dose and 15, 30, 45 min, 1, 2, 3, 4, 6, 8, 10, 12, 24, 36 and 48 hours after drug administration
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 15, 30, 45 min, 1, 2, 3, 4, 6, 8, 10, 12, 24, 36 and 48 hours after drug administration
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%AUCtz-∞ (the percentage of the AUC0-∞ that is obtained by extrapolation)
Time frame: pre-dose and 15, 30, 45 min, 1, 2, 3, 4, 6, 8, 10, 12, 24, 36 and 48 hours after drug administration
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: pre-dose and 15, 30, 45 min, 1, 2, 3, 4, 6, 8, 10, 12, 24, 36 and 48 hours after drug administration
λz (terminal rate constant in plasma)
Time frame: pre-dose and 15, 30, 45 min, 1, 2, 3, 4, 6, 8, 10, 12, 24, 36 and 48 hours after drug administration
t1/2 (terminal half-life of the analyte in plasma)
Time frame: pre-dose and 15, 30, 45 min, 1, 2, 3, 4, 6, 8, 10, 12, 24, 36 and 48 hours after drug administration
MRTpo (mean residence time of the analyte in the body after peroral administration)
Time frame: pre-dose and 15, 30, 45 min, 1, 2, 3, 4, 6, 8, 10, 12, 24, 36 and 48 hours after drug administration
CL/F (apparent clearance of the analyte in plasma after peroral administration, will not be calculated for metabolites)
Time frame: pre-dose and 15, 30, 45 min, 1, 2, 3, 4, 6, 8, 10, 12, 24, 36 and 48 hours after drug administration
Vz/F (apparent volume of distribution during the terminal phase λz following a peroral dose, will not be calculated for metabolites)
Time frame: pre-dose and 15, 30, 45 min, 1, 2, 3, 4, 6, 8, 10, 12, 24, 36 and 48 hours after drug administration
Aet1-t2 (amount of analyte eliminated in urine from the time point t1 to time point t2)
Time frame: pre-dose and 0-4, 4-8, 8-12, 12-24, 24-48 h after drug administration
fet1-t2 (fraction of analyte eliminated in urine from time point t1 to time point t2)
Time frame: pre-dose and 0-4, 4-8, 8-12, 12-24, 24-48 h after drug administration
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, 4-8, 8-12, 12-24, 24-48 h after drug administration