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This is a study to evaluate the safety, tolerability, and pharmacokinetics of single oral doses of TS-142 compared to placebo and of a single repeated dose compared to placebo in healthy volunteers. This Phase I study is composed of two parts; Part A (Single Ascending Dose) and Part B (Repeated Dose). The study employs a randomized, double-blind, placebo-controlled, parallel group design to evaluate the single and repeat-dose safety and pharmacokinetics of TS-142 in healthy participants.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| Part A: Cohort 1: TS-142 10 mg | Experimental | Single dose of TS-142 10 mg or placebo in a fasted condition |
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| Part A: Cohort 2: TS-142 30 mg | Experimental | Single dose of TS-142 30 mg or placebo in a fasted condition. |
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| Part B: Cohort 4: TS-142 20 mg | Experimental | Daily doses of 20 mg TS-142 or placebo for 7 days before bedtime. |
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| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| TS-142 | Drug | TS-142 tablets |
|
| Measure | Description | Time Frame |
|---|---|---|
| Incidence and severity of Adverse Events | Part A: Day 1 to Day 10; Part B: Day 1 to Day 16 | |
| TS-142 Plasma Pharmacokinetic Profile - Cmax | Maximum plasma concentration | Part A: Day 1 predose and at multiple time points (up to 48 hours) postdose; Part B: Day 1 predose and at multiple time points (up to 12 hours) postdose, Day 2 to Day 6 predose, Day 7 predose and at multiple time points (up to 48 hours) postdose |
| TS-142 Plasma Pharmacokinetic Profile - Tmax | Time to maximum plasma concentration | Part A: Day 1 predose and at multiple time points (up to 48 hours) postdose; Part B: Day 1 predose and at multiple time points (up to 12 hours) postdose, Day 2 to Day 6 predose, Day 7 predose and at multiple time points (up to 48 hours) postdose |
| TS-142 Plasma Pharmacokinetic Profile - AUC(0-∞) | Area Under the Concentration vs. Time Curve from Time Zero to Infinity | Part A: Day 1 predose and at multiple time points (up to 48 hours) postdose; Part B: Day 1 predose and at multiple time points (up to 12 hours) postdose, Day 2 to Day 6 predose, Day 7 predose and at multiple time points (up to 48 hours) postdose |
| TS-142 Plasma Pharmacokinetic Profile - AUC(0-last) | Area Under the Concentration vs. Time Curve from Time Zero to Last Measurable Concentration | Part A: Day 1 predose and at multiple time points (up to 48 hours) postdose; Part B: Day 1 predose and at multiple time points (up to 12 hours) postdose, Day 2 to Day 6 predose, Day 7 predose and at multiple time points (up to 48 hours) postdose |
| TS-142 Plasma Pharmacokinetic Profile - AUC(0-tau) |
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Inclusion Criteria:
Exclusion Criteria:
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| Name | Affiliation | Role |
|---|---|---|
| Taisho Director | Taisho Pharmaceutical R&D Inc. | Study Director |
| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| PPD Phase I unit | Austin | Texas | 78744 | United States |
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| ID | Term |
|---|---|
| C000723815 | TS-142 |
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| TS-142 Placebo | Drug | TS-142 matching placebo tablets |
|
Area Under the Concentration vs. Time Curve over a Dosing Interval
| Part A: Day 1 predose and at multiple time points (up to 48 hours) postdose; Part B: Day 1 predose and at multiple time points (up to 12 hours) postdose, Day 2 to Day 6 predose, Day 7 predose and at multiple time points (up to 48 hours) postdose |
| TS-142 Plasma Pharmacokinetic Profile - %AUCex | Percentage of the area extrapolated for calculation of AUC(0-∞) | Part A: Day 1 predose and at multiple time points (up to 48 hours) postdose; Part B: Day 1 predose and at multiple time points (up to 12 hours) postdose, Day 2 to Day 6 predose, Day 7 predose and at multiple time points (up to 48 hours) postdose |
| TS-142 Plasma Pharmacokinetic Profile - λz | Elimination rate constant | Part A: Day 1 predose and at multiple time points (up to 48 hours) postdose; Part B: Day 1 predose and at multiple time points (up to 12 hours) postdose, Day 2 to Day 6 predose, Day 7 predose and at multiple time points (up to 48 hours) postdose |
| TS-142 Plasma Pharmacokinetic Profile - t1/2 | Apparent terminal half-life | Part A: Day 1 predose and at multiple time points (up to 48 hours) postdose; Part B: Day 1 predose and at multiple time points (up to 12 hours) postdose, Day 2 to Day 6 predose, Day 7 predose and at multiple time points (up to 48 hours) postdose |
| TS-142 Plasma Pharmacokinetic Profile - CL/F | Apparent oral clearance | Part A: Day 1 predose and at multiple time points (up to 48 hours) postdose; Part B: Day 1 predose and at multiple time points (up to 12 hours) postdose, Day 2 to Day 6 predose, Day 7 predose and at multiple time points (up to 48 hours) postdose |
| TS-142 Plasma Pharmacokinetic Profile - Vd,z/F | Volumes of distribution | Part A: Day 1 predose and at multiple time points (up to 48 hours) postdose; Part B: Day 1 predose and at multiple time points (up to 12 hours) postdose, Day 2 to Day 6 predose, Day 7 predose and at multiple time points (up to 48 hours) postdose |
| TS-142 Urine Pharmacokinetic Profile - Ae | Amount excreted in urine | Part A: Day 1 predose and pooled for multiple intervals (up to 48 hours) postdose |
| TS-142 Urine Pharmacokinetic Profile - Fe% | Percent of dose excreted in urine | Part A: Day 1 predose and pooled for multiple intervals (up to 48 hours) postdose |
| TS-142 Urine Pharmacokinetic Profile - CLr | Renal clearance | Part A: Day 1 predose and pooled for multiple intervals (up to 48 hours) postdose |