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To assess the absorption of 30 mg Lefradafiban in two formulations, each under physiological conditions and with 40 mg Pantoprazole
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| Lefradafiban tablet with pantoprazole | Experimental |
| |
| Lefradafiban tablet | Active Comparator |
| |
| Lefradafiban double chamber sachet with pantoprazole | Experimental |
| |
| Lefradafiban double chamber sachet | Active Comparator |
|
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| Lefradafiban tablet | Drug |
| ||
| Lefradafiban double chamber sachet |
| Measure | Description | Time Frame |
|---|---|---|
| Area under the concentration-time curve of the analyte in plasma at steady state, 13th dosing interval (AUCss,13) | Up to 168 hours after first drug administration | |
| Maximum concentration of the analyte in plasma at steady state, 13th dosing interval (Cmax,ss,13) | Up to 168 hours after first drug administration | |
| Pre-dose concentration of the analyte in plasma at steady state, 13th dosing interval (Cpre,ss,13) | Up to 168 hours after first drug administration | |
| Amount of the analyte eliminated unchanged in the urine per dosing interval i expressed as percent of applied dose and corrected for molecular weight differences (Ae% (i=1,...,13)) | Up to 168 hours after first drug administration |
| Measure | Description | Time Frame |
|---|---|---|
| Pre-dose concentration of the analyte in plasma for the i-th dosing interval (Cpre,i (i=1,4,7,10,11,12)) | Up to 90 hours after first drug administration | |
| Plasma concentration of the analyte at 2 hours post-dose for the i-th dosing interval (C2h,i (i=10,11,12)) |
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Inclusion Criteria:
Exclusion Criteria:
Use of any drugs which might influence the results of the trial within 10 days prior to administration or during the trial
Intake of drugs with a long half-life (> 24 hours) within 1 month prior to administration
Participation in another trial with an investigational drug within 2 months prior to administration or during the trial
Drug abuse
Alcohol abuse (> 60 g/day)
Smoker (> 10 cigarettes or 3 cigars or 3 pipes/day) or inability to refrain from smoking on study days
Excessive physical activities within 5 days prior to administration or during the trial
Blood donation within 1 month prior to administration or during the trial
History or current gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immunological, hormonal disorders
Chronic or relevant acute infections
Diseases of the central nervous system (such as epilepsy) or psychiatric disorders
History of
Recent surgical procedures
Thrombocytes < 150000/µ
Any finding of the medical examination (including blood pressure, pulse rate and ECG) deviating from normal and of clinical relevance
Any laboratory value outside the clinically accepted reference range
Other disease or abnormality of clinical relevance
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| Drug |
|
| Pantoprazole | Drug |
|
| Up to 98 hours after first drug administration |
| Terminal half life of the analyte in plasma (t1/2) | Up to 168 hours after first drug administration |
| Percent swing of peak/trough concentrations of the analyte in plasma for the i-th dosing interval (%Swingi) | Calculated: (C2h,i - Cpre,i) / Cpre,i * 100% (i=10,11,12) | Up to 168 hours after first drug administration |
| Percent peak-trough fluctuation for the 13th dosing interval (%PTF13) | Calculated: (Cmax,ss,13 - Cpre,ss,13) * 8h / AUCss,13 * 100%) | Up to 168 hours after first drug administration |
| Percent fluctuation of area under the plasma concentration-time curve (AUCfluc,13) | Calculated: (AUCabove,13 - AUCbelow,13) / AUCabove,13 | Up to 168 hours after first drug administration |
| Fibrinogen receptor occupancy levels | Up to 168 hours after first drug administration |
| Number of patients with clinically relevant findings in laboratory tests | up to 168 hours after first drug administration |
| Number of patients with clinically relevant findings in vital signs | systolic and diastolic blood pressure, pulse rate | up to day 8 after first drug administration |
| Number of patients with adverse events | Up to 3 days after last drug administration |
| ID | Term |
|---|---|
| C107918 | lefradafiban |
| D000077402 | Pantoprazole |
| ID | Term |
|---|---|
| D053799 | 2-Pyridinylmethylsulfinylbenzimidazoles |
| D013454 | Sulfoxides |
| D013457 | Sulfur Compounds |
| D009930 | Organic Chemicals |
| D011725 | Pyridines |
| D006573 | Heterocyclic Compounds, 1-Ring |
| D006571 | Heterocyclic Compounds |
| D001562 | Benzimidazoles |
| D006574 | Heterocyclic Compounds, 2-Ring |
| D000072471 | Heterocyclic Compounds, Fused-Ring |
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