Safety, Tolerability and Pharmacokinetics of Single Doses of TS-134 in Healthy Volunteers
- Registration Number
- NCT03746067
- Lead Sponsor
- Taisho Pharmaceutical R&D Inc.
- Brief Summary
This is a Phase 1a study involving single oral dose of TS-134 in healthy male and female subjects. The safety, tolerability and pharmacokinetics of single dose of TS-134 will be evaluated.
- Detailed Description
Not available
Recruitment & Eligibility
- Status
- COMPLETED
- Sex
- All
- Target Recruitment
- 33
Inclusion Criteria
- Healthy adult male and female participants between 18 and 55 years of age
- Body weight greater than or equal to 45 kg
- Body Mass Index (BMI) greater than or equal to 18 and less than or equal to 30 kg/m^2
Exclusion Criteria
- Female participants who are pregnant, intend to become pregnant, or are breastfeeding
- Clinically significant abnormal physical examination, 12-lead electrocardiogram (ECG) OR cardiac telemetry prior to dosing.
- Significant history or presence of hepatic, renal, cardiovascular, pulmonary, gastrointestinal, hematological, locomotor, immunologic, ophthalmologic, metabolic or oncological disease.
- History or presence of psychiatric or neurologic disease or condition
- History of alcohol or drug abuse
- Any participant who currently uses or has used tobacco or tobacco-containing products for at least one month prior to screening
- Participated in strenuous exercise within 48 hours prior to study start (initial dosing) and/or are unwilling to avoid strenuous exercise at any time throughout the study.
Study & Design
- Study Type
- INTERVENTIONAL
- Study Design
- PARALLEL
- Arm && Interventions
Group Intervention Description Placebo Placebo Healthy adult subjects will be prospectively assigned to 1 of 4 cohorts. Within each cohort, 8 subjects will be randomized in a 3:1 ratio (6 active + 2 placebo) per cohort to receive TS-134 or placebo as a single oral dose solution. All cohorts will be dosed in a fasted state except for the 2nd and 4th (food effect) cohorts, which will be dosed first in a fasted state, and then in a fed state, in a single crossover design conducted with a washout between two periods. In the 3rd (CSF) cohort, the 8 subjects will receive one dose level of TS-134 as a single-blind dosing assignment; there will be no placebo dosing. TS-134 TS-134 Healthy adult subjects will be prospectively assigned to 1 of 4 cohorts. Within each cohort, 8 subjects will be randomized in a 3:1 ratio (6 active + 2 placebo) per cohort to receive TS-134 or placebo as a single oral dose solution. All cohorts will be dosed in a fasted state except for the 2nd and 4th (food effect) cohorts, which will be dosed first in a fasted state, and then in a fed state, in a single crossover design conducted with a washout between two periods. In the 3rd (CSF) cohort, 8 subjects will receive one dose level of TS-134 as a single-blind dosing assignment; there will be no placebo dosing.
- Primary Outcome Measures
Name Time Method TS-134 Plasma Pharmacokinetic Profile - tmax Day 1: predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12, 24, 36, 48 hours post-dose Time to maximum plasma concentration
TS-134 Plasma Pharmacokinetic Profile - t1/2 Day 1: predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12, 24, 36, 48 hours post-dose Apparent terminal elimination half-life
Incidence and severity of Adverse Events Day 1 to Day 7 TS-134 Plasma Pharmacokinetic Profile - Cmax Day 1: predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12, 24, 36, 48 hours post-dose Maximum plasma concentration
TS-134 Plasma Pharmacokinetic Profile - AUC(0-last) Day 1: predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12, 24, 36, 48 hours post-dose Area under the concentration vs. time curve from time zero to last measurable concentration
TS-134 Plasma Pharmacokinetic Profile - CL/F Day 1: predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12, 24, 36, 48 hours post-dose Apparent clearance following oral administration
TS-134 Plasma Pharmacokinetic Profile - Vd/F Day 1: predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12, 24, 36, 48 hours post-dose Apparent volumes of distribution following oral administration
- Secondary Outcome Measures
Name Time Method TS-134 CSF Pharmacokinetic Profile - tmax Day 1: predose, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 12, 24 hours post-dose Time to maximum CSF concentration
TS-134 CSF Pharmacokinetic Profile - t1/2 Day 1: predose, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 12, 24 hours post-dose Apparent terminal elimination half-life (CSF)
TS-134 CSF Pharmacokinetic Profile - CL/F Day 1: predose, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 12, 24 hours post-dose Apparent clearance (CSF) following oral administration
TS-134 CSF Pharmacokinetic Profile - Vd/F Day 1: predose, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 12, 24 hours post-dose Apparent volumes of distribution (CSF) following oral administration
TS-134 Cerebral Spinal Fluid (CSF) Pharmacokinetic Profile - Cmax Day 1: predose, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 12, 24 hours post-dose Maximum CSF concentration
TS-134 CSF Pharmacokinetic Profile - AUC(0-last) Day 1: predose, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 12, 24 hours post-dose Area under the CSF concentration vs. time curve from time zero to last measurable concentration
Trial Locations
- Locations (1)
PAREXEL - Early Phase Clinical Unit-Los Angeles
🇺🇸Glendale, California, United States