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Study to evaluate the pharmacokinetics of Tipranavir and its metabolites including excretion and mass balance of parent compound and radioactivity at steady-state; to isolate, identify and quantify major metabolites of tipranavir in plasma, urine and feces
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| TPV/r followed by 14C-radiolabeled TPV | Experimental | Tipranavir/Ritonavir dosed to steady state followed by single-dose 14C-radiolabeled tipranavir co-administered with Tipranavir/Ritonavir |
|
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| 14C-Tipranavir | Drug |
| ||
| Tipranavir |
| Measure | Description | Time Frame |
|---|---|---|
| Radioactive levels of 14C-Tipranavir in plasma and blood | -10 minutes, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, and 12 hours after dose administration | |
| Radioactive erythrocyte-plasma partition ratio | -10 minutes, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, and 12 hours after dose administration | |
| Maximum measured concentration of the analyte in plasma (Cmax) | 14C-radiolabeled Tipranavir + Tipranavir | -10 minutes, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, and 12 hours after dose administration |
| Plasma concentration 12 hours after dosing (Cp12h) | 14C-radiolabeled Tipranavir + Tipranavir | -10 minutes, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, and 12 hours after dose administration |
| Area under plasma concentration time curve (AUC) | 14C-radiolabeled Tipranavir + Tipranavir | -10 minutes, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, and 12 hours after dose administration |
| Time of maximum concentration (Tmax) | 14C-radiolabeled Tipranavir + Tipranavir | -10 minutes, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, and 12 hours after dose administration |
| Apparent terminal half life (t1/2) | 14C-radiolabeled Tipranavir + Tipranavir | -10 minutes, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, and 12 hours after dose administration |
| Measure | Description | Time Frame |
|---|---|---|
| Number of subjects with adverse events | up to 15 days | |
| Number of subjects with abnormal changes in laboratory parameters | up to day 14 | |
| Number of subjects with clinically significant changes in Electrocardiogram (ECG) |
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Inclusion Criteria:
Exclusion Criteria:
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| ID | Term |
|---|---|
| C107201 | tipranavir |
| D019438 | Ritonavir |
| ID | Term |
|---|---|
| D013844 | Thiazoles |
| D013457 | Sulfur Compounds |
| D009930 | Organic Chemicals |
| D001393 | Azoles |
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|
| Ritonavir | Drug |
|
| Cumulative amount of 14C- radioactivity in Urine and feces |
| up to 15 days |
| Percent excretion in urine and feces | relative to total radioactivity administered | up to 15 days |
| Time needed to achieve steady-state as determined by tipranavir trough concentrations | up to 15 days |
| up to day 6 |
| D006573 |
| Heterocyclic Compounds, 1-Ring |
| D006571 | Heterocyclic Compounds |