The objective of the current study was to investigate safety, tolerability, pharmacokinetics and pharmacodynamics of BI 1356 BS.
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
TREATMENT
Masking
DOUBLE
Enrollment
64
Number of patients with adverse events
Time frame: up to 30 days
Number of patients with abnormal findings in physical examination
Time frame: Screening, up to 16 days after drug administration
Number of patients with clinically significant changes in vital signs (blood pressure [BP], heart rate [HR])
Time frame: Screening, up to 16 days after drug administration
Number of patients with clinically significant changes in 12-lead electrocardiogram (ECG)
Time frame: Screening, up to 16 days after drug administration
Number of patients with abnormal changes in laboratory parameters
Time frame: Screening, up to 16 days after drug administration
Assessment of tolerability by investigator on a 4-point scale
Time frame: up to 16 days after drug administration
Cmax (maximum concentration of the analyte in plasma)
Time frame: predose, up to 192 h following drug administration
tmax (time from dosing to maximum concentration)
Time frame: predose, up to 192 h following 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: predose, up to 192 h following drug administration
%AUCtz-∞ (the percentage of the AUC0-∞ that is obtained by extrapolation)
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Time frame: predose, up to 192 h following 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: predose, up to 192 h following drug administration
λz (terminal rate constant in plasma)
Time frame: predose, up to 192 h following drug administration
t1/2 (terminal half-life of the analyte in plasma)
Time frame: predose, up to 192 h following drug administration
MRTpo (mean residence time of the analyte in the body after po administration)
Time frame: predose, up to 192 h following drug administration
CL/F (total clearance of the analyte in the plasma after extravascular administration)
Time frame: predose, up to 192 h following drug administration
Vz/F (apparent volume of distribution during the terminal phase λz following an extravascular dose)
Time frame: predose, up to 192 h following drug administration
Aet1-t2 (amount of analyte that is eliminated in urine from the time point t1 to time point t2)
Time frame: up to 120 h following drug administration
fet1-t2 (fraction of analyte eliminated in urine from time point t1 to time point t2)
Time frame: up to 120 h following drug administration
CLR,t1-t2 (renal clearance of the analyte from the time point t1 until the time point t2)
Time frame: up to 120 h following drug administration
Changes of Dipeptidyl-Peptidase IV (DPP-IV) activity in plasma
Time frame: predose, up to 96 h following drug administration