Investigation of pharmacodynamics (inhibition of oxidosqualene cyclase, MES as marker), effect on routine lipid profile parameters, safety and preliminary pharmacokinetics
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
TREATMENT
Masking
DOUBLE
Enrollment
60
Percentage changes in total-cholesterol
Time frame: Pre-dose, up to day 15
Percentage changes in low density lipoprotein (LDL) - cholesterol
Time frame: Pre-dose, up to day 15
Percentage changes in high density lipoprotein (HDL) - cholesterol
Time frame: Pre-dose, up to day 15
Percentage changes in apo-lipoprotein B
Time frame: Pre-dose, up to day 15
Percentage changes in lipoprotein (a)
Time frame: Pre-dose, up to day 15
Percentage changes in triglycerides
Time frame: Pre-dose, up to day 15
Maximum concentration of the analyte in plasma at different time points (Cmax)
Time frame: Up 336 hours after first drug administration
Time to reach maximum concentration of the analyte in plasma at different time points (tmax)
Time frame: Up 336 hours after first drug administration
Apparent terminal elimination half-life of the analyte in plasma (t1/2)
Time frame: Up 336 hours after first drug administration
Area under the concentration-time curve of the analyte in plasma at different time points (AUC)
Time frame: Up 336 hours after first drug administration
Total mean residence time of the analyte in the body (MRTtot)
Time frame: Up 336 hours after first drug administration
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Apparent clearance of the analyte in plasma after extravascular multiple dose administration (CL/f)
Time frame: Up 336 hours after first drug administration
Apparent volume of distribution of the analyte during the terminal phase (Vz/f)
Time frame: Up 336 hours after first drug administration
Terminal rate constant of the analyte in plasma (λz)
Time frame: Up 336 hours after first drug administration
Number of participants with clinically relevant changes from baseline in physical examination
Time frame: Pre-dose and day 15
Number of participants with clinically relevant changes from baseline in 12-lead ECG
Time frame: Pre-dose and day 15
Number of participants with clinically relevant changes from baseline in lens examination
Time frame: Pre-dose and day 15
Number of participants with clinically relevant changes in vital signs (blood pressure, pulse rate, body weight)
Time frame: Pre-dose, up to 324 hours after first drug administration
Number of participants with clinically relevant changes in laboratory parameters
Time frame: Pre-dose, up to 324 hours after first drug administration
Number of participants with adverse events
Time frame: Up to 1 day after last drug administration
Global clinical assessment by the investigator
Time frame: On day 15 after first drug administration
Monoepoxy-squalene (MES) plasma concentration at different time points
as surrogate marker for squalene inhibition
Time frame: Pre-dose, up to day 15