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Study to assess the tolerability of an intravenous infusion of 0.5 and 1.0 mg (actual 0.8 mg) BIBT 986 BS per hour over 32 hours as well as pharmacokinetics and the effect on blood coagulation parameters
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| BIBT 986 BS - low | Experimental |
| |
| BIBT 986 BS - high | Experimental |
| |
| Placebo | Placebo Comparator |
|
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| BIBT 986 BS - low | Drug |
| ||
| BIBT 986 BS - high |
| Measure | Description | Time Frame |
|---|---|---|
| Cmax (maximum measured concentration of the analyte in plasma) | up to 48 hours post dose | |
| CT (concentration of the analyte at the end of drug infusion) | up to 48 hours post dose | |
| Css (steady state concentration of the analyte in plasma following a constant rate infusion) | up to 48 hours post dose | |
| Tmax (time from dosing to the maximum concentration of the analyte in plasma) | up to 48 hours post dose | |
| AUC0-∞ (Area under the concentration-time curve of the analyte in plasma over the time interval from 0 extrapolated to infinity after single dose administration) | up to 48 hours post dose | |
| t1/2 (Terminal half-life of the analyte in plasma after single dose administration) | up to 48 hours post dose | |
| AUC0-tz (Area under the concentration-time curve of the analyte in plasma over the time interval from 0 to the last quantifiable drug plasma concentration after single dose administration) | up to 48 hours post dose | |
| λz (terminal rate constant of the analyte in plasma) | up to 48 hours post dose | |
| MRTinf (mean residence time of the analyte in the body after intravenous infusion) | up to 48 hours post dose |
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Inclusion Criteria:
Exclusion Criteria:
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| Placebo | Drug |
|
| CL (Total clearance of the analyte in plasma following intravascular administration) | up to 48 hours post dose |
| Vss (Apparent volume of distribution at steady state following intravascular administration) | up to 48 hours post dose |
| Vz (apparent volume of distribution during the terminal phase λz following intravascular administration) | up to 48 hours post dose |
| Amount of parent drug eliminated in urine (Ae) | up to 48 hours post dose |
| Change in activated partial thromboplastin time (aPTT) | up to 48 hours post dose |
| Change in prothrombin time (PT) | up to 48 hours post dose |
| Change in ecarin clotting time (ECT) | up to 48 hours post dose |
| Change in thrombin time (TT) | up to 48 hours post dose |
| Number of subjects with adverse events | up to 4 days |
| Number of subjects with clinically significant changes in vital signs | Pulse rate, systolic & diastolic blood pressure | up to 4 days |
| Change in International Normalised Ratio (INR) | up to 48 hours post dose |
| Fraction of administered drug excreted unchanged in urine (fe) | up to 48 hours post dose |
| CLR (renal clearance of the analyte in plasma following intravascular administration) | up to 48 hours post dose |