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The primary objective of the study was to investigate the relative bioavailability and pharmacokinetics of 20 mg BIBW 2992 administered as film-coated immediate release tablet (final formulation, i.e. phase III/to-be-marketed formulation) to healthy subjects in comparison with the drinking solution and in comparison with the trial formulation II tablet, which was administered in phase II clinical trials and also partly in phase I trials.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| BIBW 2992 MA2, final formulation | Experimental |
| |
| BIBW 2992 MA2, trial formulation II | Experimental |
| |
| BIBW 2992 MA 2 drinking solution | Active Comparator |
|
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| BIBW 2992 MA2 | Drug | film-coated immediate release tablet - final formulation |
|
| Measure | Description | Time Frame |
|---|---|---|
| AUC0-∞ (area under the concentration-time curve of the analyte in plasma over the time interval from 0 extrapolated to infinity) | up to 96 hours after drug administration | |
| Cmax (maximum measured concentration of the analyte in plasma) | up to 96 hours after drug administration |
| Measure | Description | Time Frame |
|---|---|---|
| AUC (area under the concentration-time curve of the analyte in plasma) for several time points | up to 96 hours after drug administration | |
| %AUCtz-∞ (percentage of the AUCtz-∞ that is obtained by extrapolation from the last quantifiable data point to infinity) |
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Inclusion Criteria:
Exclusion Criteria:
Exclusion criteria specific for this study:
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| BIBW 2992 MA2 | Drug | film-coated immediate release tablet - trial formulation II |
|
| BIBW 2992 MA2 | Drug | powder for oral solution |
|
| up to 96 hours after drug administration |
| tmax (time from dosing to the maximum concentration of the analyte in plasma) | up to 96 hours after drug administration |
| λz (terminal rate constant in plasma) | up to 96 hours after drug administration |
| t1/2 (terminal half-life of the analyte in plasma) | up to 96 hours after drug administration |
| MRTpo (mean residence time of the analyte in the body after oral administration) | up to 96 hours after drug administration |
| CL/F (apparent clearance of the analyte in the plasma after extravascular administration) | up to 96 hours after drug administration |
| Vz/F (apparent volume of distribution during the terminal phase λz following an extravascular dose) | up to 96 hours after drug administration |
| Number of patients with adverse events | up to 88 days |
| Assessment of tolerability by the investigator on a 4-point scale | Day 5 of each treatment period |
| ID | Term |
|---|---|
| D000077716 | Afatinib |
| ID | Term |
|---|---|
| D000577 | Amides |
| D009930 | Organic Chemicals |
| D011799 | Quinazolines |
| D006574 | Heterocyclic Compounds, 2-Ring |
| D000072471 | Heterocyclic Compounds, Fused-Ring |
| D006571 | Heterocyclic Compounds |
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