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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 isavuconazole and the routes of excretion and the extent of metabolism of 14C-labeled prodrug BAL8557.
Subjects will be admitted to and stay in a clinical research unit for 23 days. On Day 1, they will receive a single oral dose of BAL8557 and throughout the study period the excretion and metabolism of the study drug will be monitored.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| 14C-labeled prodrug isavuconazonium sulfate | Experimental | single dose |
|
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| 14C-labeled prodrug isavuconazonium sulfate | Drug | oral |
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| 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) | Pre-dose and 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, 168, 216, 264, 312, 360, 408, 456, and 504 hours after radioactive dose. If subjects are not discharged on Day 22, blood will be collected at 576 and 648 hours after dosing | |
| Radioactivity in whole blood and in plasma: AUC from time of dosing to the last quantifiable concentration (AUClast) | Pre-dose and 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, 168, 216, 264, 312, 360, 408, 456, and 504 hours after radioactive dose. If subjects are not discharged on Day 22, blood will be collected at 576 and 648 hours after dosing | |
| Radioactivity in whole blood and in plasma: Maximum concentration (Cmax) | Pre-dose and 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, 168, 216, 264, 312, 360, 408, 456, and 504 hours after radioactive dose. If subjects are not discharged on Day 22, blood will be collected at 576 and 648 hours after dosing | |
| Radioactivity in whole blood and in plasma: Time to Attain Cmax (tmax) | Pre-dose and 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, 168, 216, 264, 312, 360, 408, 456, and 504 hours after radioactive dose. If subjects are not discharged on Day 22, blood will be collected at 576 and 648 hours after dosing | |
| Radioactivity in whole blood and in plasma: Apparent terminal elimination half-life (t1/2) | Pre-dose and 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, 168, 216, 264, 312, 360, 408, 456, and 504 hours after radioactive dose. If subjects are not discharged on Day 22, blood will be collected at 576 and 648 hours after dosing | |
| Radioactivity in emesis (if applicable) | After study drug administration Days 1 up through 29 |
| Measure | Description | Time Frame |
|---|---|---|
| Pharmacokinetic profile of isavuconazole in plasma: AUCinf, AUClast, Cmax, tmax, Apparent body clearance after dosing (CL/F), Apparent volume of distribution (Vz/F), t1/2 | Pre-dose and 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, 168, 216, 264, 312, 360, 408, 456, and 504 hours after radioactive dose. If subjects are not discharged on Day 22, blood will be collected at 576 and 648 hours after dosing |
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Inclusion Criteria:
Exclusion Criteria:
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| Name | Affiliation | Role |
|---|---|---|
| Medical Director | Astellas Pharma Global Development, Inc. | Study Director |
| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| Covance | Madison | Wisconsin | 53704 | United States |
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| Radioactivity ratio blood/plasma | Day 1 |
| Excretion ratio and cumulative excretion of radioactivity in urine | Pre-dose and after dosing collection times: 0 to 6, 6 to 12, 12 to 24, and in 24 hour intervals up to 504 hours after radioactive dose. If subjects are not discharged on Day 22, sample collection will continue in 24 hour intervals until discharge |
| Excretion ratio and cumulative excretion of radioactivity in feces | Pre-dose and after dosing in 24 hour intervals up to 504 hours after radioactive dose. If subjects are not discharged on Day 22, sample collection will continue in 24 hour intervals until the day of discharge |
| Pharmacokinetic Profile of isavuconazole in urine: Ae, Ae%, CLR | Amount excreted (Ae), Percent of unchanged drug excreted into the urine (Ae%), Renal clearance (CLR) | Pre-dose and 0 to 6, 6 to 12, 12 to 24, in 24 hour intervals up to 504 hours after radioactive dose. If subjects are not discharged on Day 22, sample collection will continue in 24 hour intervals until day of discharge |
| Metabolic profile of isavuconazole and possible metabolites in plasma, urine, and feces | 8, 24,72, 144, and 312 hours after dosing. If subjects are not discharged on Day 22, samples will be taken at 504 hours after dosing |