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This is an open-label, single-center, single-sequence study to evaluate the concomitant effects of the potent CYP3A inhibitor itraconazole on the single-dose pharmakokinetics, safety and tolerability of oral TS-142 in healthy subjects.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| Subjects receiving TS-142 and itraconazole | Experimental | Eligible subjects will receive a single dose of 5 mg TS-142 on Day 1. Subjects will also receive twice-a-day of 200 mg itraconazole on Day 3 and an once-daily single dose of 200 mg itraconazole from Day 4 to Day 7 and single dose of 1 mg TS-142 on Day 6. |
|
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| TS-142 | Drug | TS-142 will be given as 1 mg per capsule administered orally with water. |
|
| Measure | Description | Time Frame |
|---|---|---|
| Cmax | Maximum observed concentration of unchanged form of TS-142 and its metabolite in plasma. | Sampling at pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 9, 12, 18, 24, 48 hours post-dose of TS-142 on Day 1 or Day 6, in addition, at 96, 144, 192, 240 hours post-dose of TS-142 on Day 6. |
| Measure | Description | Time Frame |
|---|---|---|
| AUC(0-last) | Area under the concentration-time curve from time zero to time of the last quantifiable concentration of TS-142 and its metabolite in plasma. | Sampling at pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 9, 12, 18, 24, 48 hours post-dose of TS-142 on Day 1 or Day 6, in addition, at 96, 144, 192, 240 hours post-dose of TS-142 on Day 6. |
| Measure | Description | Time Frame |
|---|---|---|
| AUC(0-infinity) | Area under the concentration-time curve from time zero extrapolated to infinite time of TS-142 and its metabolite in plasma. | Sampling at pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 9, 12, 18, 24, 48 hours post-dose of TS-142 on Day 1 or Day 6, in addition, at 96, 144, 192, 240 hours post-dose of TS-142 on Day 6. |
Inclusion Criteria:
Exclusion Criteria:
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| Name | Affiliation | Role |
|---|---|---|
| Taisho Director | Taisho Pharmaceutical Co., Ltd. | Study Director |
| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| Taisho Pharmaceutical Co., Ltd selected site | Tokyo | Japan |
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| ID | Term |
|---|---|
| C000723815 | TS-142 |
| D017964 | Itraconazole |
| ID | Term |
|---|---|
| D014230 | Triazoles |
| D001393 | Azoles |
| D006573 | Heterocyclic Compounds, 1-Ring |
| D006571 | Heterocyclic Compounds |
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| Itraconazole | Drug | Itraconazole will given as 50 mg per capsule administered orally with water. |
|
| Tmax |
Time to Cmax of TS-142 and its metabolite in plasma. |
| Sampling at pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 9, 12, 18, 24, 48 hours post-dose of TS-142 on Day 1 or Day 6, in addition, at 96, 144, 192, 240 hours post-dose of TS-142 on Day 6. |
| T1/2 | Terminal phase half-life of TS-142 and its metabolite in plasma. | Sampling at pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 9, 12, 18, 24, 48 hours post-dose of TS-142 on Day 1 or Day 6, in addition, at 96, 144, 192, 240 hours post-dose of TS-142 on Day 6. |
| Vz/F | Apparent Volume of Distribution During Terminal Phase of TS-142 and its metabolite in plasma. | Sampling at pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 9, 12, 18, 24, 48 hours post-dose of TS-142 on Day 1 or Day 6, in addition, at 96, 144, 192, 240 hours post-dose of TS-142 on Day 6. |
| CL/F | Apparent Oral Clearance of TS-142 and its metabolite in plasma. | Sampling at pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 9, 12, 18, 24, 48 hours post-dose of TS-142 on Day 1 or Day 6, in addition, at 96, 144, 192, 240 hours post-dose of TS-142 on Day 6. |
| λz | terminal elimination rate constant of TS-142 and its metabolite in plasma. | Sampling at pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 9, 12, 18, 24, 48 hours post-dose of TS-142 on Day 1 or Day 6, in addition, at 96, 144, 192, 240 hours post-dose of TS-142 on Day 6. |
| AUC(0-24h) | Area under the concentration-time curve from time zero to time 24 h of TS-142 and its metabolite in plasma. | Sampling at pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 9, 12, 18, 24, 48 hours post-dose of TS-142 on Day 1 or Day 6, in addition, at 96, 144, 192, 240 hours post-dose of TS-142 on Day 6. |
| D010879 |
| Piperazines |