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| Name | Class |
|---|---|
| Basilea Pharmaceutica International Ltd | INDUSTRY |
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The purpose of this study is to evaluate the pharmacokinetics of 14C-labeled cleavage product (BAL8728), in particular the routes of excretion and extent ot metabolism of the cleavage product following administration of a single intravenous dose of pyridinylmethyl-14C-labeled prodrug isavuconazonium sulfate (BAL8557). In addition, identify the metabolic profile of BAL8728 in human plasma, urine and/or feces after a single intravenous dose of pyridinylmethyl-14C-labeled BAL8557 and evaluate the pharmacokinetics of BAL8728 and BAL4815. Safety and tolerability after a single intravenous dose of pyridinylmethyl-14C-labeled isavuconazonium sulfate will also be evaluated.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| Pyridinylmethyl-14C-labeled isavuconazonium sulfate | Experimental | single dose |
|
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| Pyridinylmethyl-14C-labeled isavuconazonium sulfate | Drug | Intravenous |
|
| Measure | Description | Time Frame |
|---|---|---|
| Radioactivity in whole blood and in plasma: Area under the concentration-time curve (AUC) from time of dosing to infinity (AUCinf) | 20 time points up to Day 4. If Day 4 is not the end of the study, samples will be drawn once a day up to Day 9 | |
| Radioactivity in whole blood and in plasma: AUC from time of dosing to the last quantifiable concentration (AUClast) | 20 time points up to Day 4. If Day 4 is not the end of the study, samples will be drawn once a day up to Day 9 | |
| Radioactivity in whole blood and in plasma: Maximum concentration (Cmax) | 20 time points up to Day 4. If Day 4 is not the end of the study, samples will be drawn once a day up to Day 9 | |
| Radioactivity in whole blood and in plasma: Time to Attain Cmax (tmax) | 20 time points up to Day 4. If Day 4 is not the end of the study, samples will be drawn once a day up to Day 9 | |
| Radioactivity in whole blood and in plasma: Apparent terminal elimination half-life (t1/2) | 20 time points up to Day 4. If Day 4 is not the end of the study, samples will be drawn once a day up to Day 9 | |
| Radioactivity in emesis (if applicable) | After study drug administration up to Day 9 | |
| Radioactivity ratio blood/plasma | Day 1 | |
| Percent of dose and cumulative percent of dose of radioactivity recovered in urine | 7 time intervals up to Day 4. If Day 4 is not the end of the study, sample collection will continue in 24 hour intervals until discharge up to Day 9 |
| Measure | Description | Time Frame |
|---|---|---|
| Metabolic profile of BAL8728 and possible metabolites in plasma, urine, and feces | Up to 3 days (72 hours) after dosing |
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Inclusion Criteria:
Exclusion Criteria:
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| Name | Affiliation | Role |
|---|---|---|
| Medical Director | Astellas Pharma Global Development | Study Director |
| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| Covance | Madison | Wisconsin | 53704 | United States |
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| Percent of dose and cumulative percent dose of radioactivity recovered in feces | 4 time intervals up to Day 4. If Day 4 is not the end of the study, sample collection will continue in 24 hour intervals until discharge up to Day 9 |
| Pharmacokinetics of BAL8728 (cleavage product) in plasma: AUCinf | 20 time points up to Day 4. If Day 4 is not the end of the study, samples will be drawn once a day up to Day 9 |
| Pharmacokinetics of BAL8728 (cleavage product) in plasma: AUClast | 20 time points up to Day 4. If Day 4 is not the end of the study, samples will be drawn once a day up to Day 9 |
| Pharmacokinetics of BAL8728 (cleavage product) in plasma: Cmax | 20 time points up to Day 4. If Day 4 is not the end of the study, samples will be drawn once a day up to Day 9 |
| Pharmacokinetics of BAL8728 (cleavage product) in plasma: tmax | 20 time points up to Day 4. If Day 4 is not the end of the study, samples will be drawn once a day up to Day 9 |
| Pharmacokinetics of BAL8728 (cleavage product) in plasma: total body clearance after intravenous dosing (CLtot) | 20 time points up to Day 4. If Day 4 is not the end of the study, samples will be drawn once a day up to Day 9 |
| Pharmacokinetics of BAL8728 (cleavage product) in plasma: volume of distribution during terminal phase after intravenous dosing (Vz) | 20 time points up to Day 4. If Day 4 is not the end of the study, samples will be drawn once a day up to Day 9 |
| Pharmacokinetics of BAL8728 (cleavage product) in plasma: t 1/2 | 20 time points up to Day 4. If Day 4 is not the end of the study, samples will be drawn once a day up to Day 9 |
| Pharmacokinetics of BAL8728 (cleavage product) in urine: amount excreted (Ae) | 7 time intervals up to Day 4. If Day 4 is not the end of the study, sample collection will continue in 24 hour intervals until discharge up to Day 9 |
| Pharmacokinetics of BAL8728 (cleavage product) in urine: percent of unchanged drug excreted into the urine (Ae%) | 7 time intervals up to Day 4. If Day 4 is not the end of the study, sample collection will continue in 24 hour intervals until discharge up to Day 9 |
| Pharmacokinetics of BAL8728 (cleavage product) in urine: renal clearance (CLr) | 7 time intervals up to Day 4. If Day 4 is not the end of the study, sample collection will continue in 24 hour intervals until discharge up to Day 9 |
| Pharmacokinetics of BAL4815 (isavuconazole) in plasma: AUClast | 20 time points up to Day 4. If Day 4 is not the end of the study, samples will be drawn once a day up to Day 9 |
| Pharmacokinetics of BAL4815 (isavuconazole) in plasma: Cmax | 20 time points up to Day 4. If Day 4 is not the end of the study, samples will be drawn once a day up to Day 9 |
| Pharmacokinetics of BAL4815 (isavuconazole) in plasma: tmax | 20 time points up to Day 4. If Day 4 is not the end of the study, samples will be drawn once a day up to Day 9 |
| ID | Term |
|---|---|
| C508735 | isavuconazole |
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