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Safety, pharmacodynamics and pharmacokinetics of 0.25, 0.75, 2.0, 6.0, and 10 mg BIBB 1464 p.o once daily in a rising dose group-comparison (placebo controlled, double blind, randomized per dose level).
Relative Bioavailability of 0.75 mg or 2 mg or 6 mg ( tablet vs. solution, intraindividual comparison), preliminary assessment of food effects (interindividual comparison)
Two-stage Trial Design With Randomised Double Blind Placebo Controlled Rising Dose Phase and Subsequent Randomised, Open Parallel Group Phase).
MS (Tablet) in Healthy Male Subjects, Combined With Preliminary Evaluation of Relative Bioavailability and Effect of Food of the Dose of 0.75 mg or 2 mg or 6 mg (Two-stage Trial Design With Randomised Double Blind Placebo Controlled Rising Dose Phase and Subsequent Randomised, Open Parallel Group Phase).
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| BIBB 1464 MS single rising dose fed | Experimental |
| |
| BIBB 1464 MS tablet fasted | Experimental |
| |
| BIBB 1464 MS solution fasted | Active Comparator |
| |
| BIBB 1464 MS placebo | Placebo Comparator |
|
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| BIBB 1464 MS tablet | Drug |
| ||
| BIBB 1464 MS solution |
| Measure | Description | Time Frame |
|---|---|---|
| Maximum drug plasma concentration (Cmax) | Up to 38 hours after drug administration | |
| Time to reach the maximum concentration of the analyte in plasma (tmax) | Up to 38 hours after drug administration | |
| Total area under the plasma drug concentration-time curve (AUC) | Up to 38 hours after drug administration | |
| Apparent terminal half-life of the analyte in plasma (t1/2) | Up to 38 hours after drug administration | |
| Total plasma clearance divided by the systemic availability factor (CL/f) | Up to 38 hours after drug administration | |
| Dose normalized AUC0-38h ( NAUC0-38h) | Up to 38 h after drug administration | |
| Mean residence time, total (MRTtot) | Up to 38 hours after drug administration | |
| Number of patients with adverse events | Up to 72 hours after last drug administration | |
| Number of patients with clinical significant findings in vital signs | Up to 38 hours after drug administration | |
| Number of patients with clinical significant findings in electrocardiogram (ECG) |
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Inclusion Criteria:
Exclusion Criteria:
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| Drug |
|
| BIBB 1464 MS placebo | Drug |
|
| Standard dinner | Other |
|
| Up to 38 hours after drug administration |
| Number of patients with clinical significant findings in physical examination | Up to 38 hours after drug administration |
| Investigator assessed tolerability on a 4 point scale | Up to 38 hours after drug administration |
| Monoepoxysqualene (MES) plasma concentration | Up to 38 hours after drug administration |
| Amount of drug excreted in urine | Up to 38 h after drug administration |