Study to evaluate the safety, tolerability, pharmacokinetics, and pharmacodynamics of BI 1356 BS (0.5 mg, 2.5 mg, and 10 mg) administered orally once daily for 28 days in Japanese patients with type 2 diabetes mellitus.
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
TREATMENT
Masking
DOUBLE
Enrollment
72
Global assessment of tolerability by the investigator on a 4-point scale (good, satisfactory, not satisfactory and bad)
Time frame: Day 43
Number of patients with adverse events
Time frame: Up to day 50
Number of patients with clinically relevant changes in vital signs (blood pressure, pulse rate)
Time frame: Up to day 50
Number of patients with clinically relevant changes in clinical laboratory tests (haematology, clinical chemistry, and urinalysis)
Time frame: Up to day 50
Maximum measured concentration of the analyte in plasma (Cmax) at different time points
Time frame: Up to day 43
Time from last dosing to the maximum concentration of the analyte in plasma (tmax) at different time points
Time frame: Up to day 43
Area under the concentration time curve of the analyte in plasma (AUC) at different time points
Time frame: Up to day 43
Amount of the analyte that is eliminated in urine (Ae) at different time points
Time frame: Up to day 43
Fraction of parent drug eliminated in urine (fe) at different time points
Time frame: Up to day 43
Renal clearance of the analyte (CLR) at different time points
Time frame: Up to day 43
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Minimum measured concentration of the analyte in plasma at steady state over a uniform dosing interval τ (Cmin,ss)
Time frame: After the last dose on day 28 up to day 43
Average concentration of the analyte in plasma at steady state (Cavg)
Time frame: After the last dose on day 28 up to day 43
Terminal half-life of the analyte in plasma at steady state (t1/2,ss)
Time frame: After the last dose on day 28 up to day 43
Terminal rate constant in plasma at steady state (λz,ss)
Time frame: After last dose on day 28 up to day 43
Mean residence time of the analyte in the body at steady state after oral administration (MRTpo,ss)
Time frame: After last dose on day 28 up to day 43
Apparent clearance of the analyte in plasma at steady state after extravascular multiple dose administration (CL/F,ss)
Time frame: After last dose on day 28 up to day 43
Apparent volume of distribution during the terminal phase λz at steady state following extravascular administration (Vz/F,ss)
Time frame: After last dose on day 28 up to day 43
Predose concentration of the analyte in plasma (Cpre) at different time points immediately before administration of the Nth dose
Time frame: Up to day 28
Calculation of accumulation ratio of the analyte in plasma based on Cmax (RA,Cmax)
Time frame: Up to day 43
Calculation of accumulation ratio of the analyte in plasma based on AUCτ (RA,AUCτ)
Time frame: Up to day 43
Minimum dipeptidyl peptidase IV (DPP-IV) activity (Emin) at different time points
Time frame: Up to day 43
Time to reach minimum DPP-IV activity (tmin) at different time points
Time frame: Up to day 43
DPP-IV activity at different time points
Time frame: Up to day 43