To assess the safety, tolerance and pharmacokinetics of 5 mg to 2400 mg BILN 2061 ZW 1. In rising single doses 2. With and without a 64 g fat breakfast at one selected dose
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
TREATMENT
Masking
DOUBLE
Enrollment
103
Number of patients with clinically relevant changes in vital signs (systolic and diastolic blood pressure, pulse rate)
Time frame: Pre-dose, up to 48 hours after drug administration
Changes from baseline in laboratory tests
Time frame: Pre-dose and 48 hours after drug administration
Number of patients with clinically relevant changes in 12-lead ECG
Time frame: Pre-dose, up to 48 hours after drug administration
Changes from baseline in physical examination
Time frame: Pre-dose and 48 hours after drug administration
Number of patients with adverse events
Time frame: Up to 48 hours after drug administration
Global assessment of tolerability by the investigator on a 4-point scale
Time frame: Up to 48 hours after drug administration
Maximum concentration of the analyte in plasma after a single dose administration (Cmax)
Time frame: up to 48 hours after drug administration
Area under the concentration-time curve of the analyte in plasma from time 0 to infinity (AUC0-infinity)
Time frame: up to 48 hours after drug administration
Time to reach Cmax following a single dose administration (tmax)
Time frame: up to 48 hours after drug administration
Elimination half-life of the analyte in plasma (t1/2)
Time frame: up to 48 hours after drug administration
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Total oral clearance of the analyte from plasma after oral administration, divided by F (bioavailability factor) (CL/F)
Time frame: up to 48 hours after drug administration
Total mean residence time of the analyte in plasma (MRT)
Time frame: up to 48 hours after drug administration
Apparent volume of distribution during the terminal elimination phase (Vz/F)
Time frame: up to 48 hours after drug administration
Amount of intact drug excreted in urine (Au)
Time frame: up to 48 hours after drug administration