Safety, Tolerability and Pharmacokinetics of Single Doses of TS-134 in Healthy Volunteers

NCT03746067 | Completed Phase 1 FDA Drug

• 1 other identifier: TS134-US101
• Study Type: interventional
• Target: 33
• Locations: 1 country
• Sites: 1

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.

Conditions

Healthy Volunteers

Keywords

TS-134, CSF

Outcome Measures

Primary Outcomes (7)

• Incidence and severity of Adverse Events

  Day 1 to Day 7

• TS-134 Plasma Pharmacokinetic Profile - Cmax

  Maximum plasma concentration

  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

• TS-134 Plasma Pharmacokinetic Profile - AUC(0-last)

  Area under the concentration vs. time curve from time zero to last measurable concentration

  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

• TS-134 Plasma Pharmacokinetic Profile - tmax

  Time to maximum plasma concentration

  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

• TS-134 Plasma Pharmacokinetic Profile - t1/2

  Apparent terminal elimination half-life

  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

• TS-134 Plasma Pharmacokinetic Profile - CL/F

  Apparent clearance following oral administration

  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

• TS-134 Plasma Pharmacokinetic Profile - Vd/F

  Apparent volumes of distribution following oral administration

  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

Secondary Outcomes (6)

• 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

• 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

• 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

• 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

• 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

Study Arms (2)

TS-134

EXPERIMENTAL

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.

Drug: TS-134

Placebo

PLACEBO COMPARATOR

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.

Drug: Placebo

Interventions

TS-134 DRUG

5 mg, 10 mg, or 20 mg oral solution

TS-134

Placebo DRUG

Matched Placebo oral solution

Placebo

Eligibility Criteria

• Age: 18 Years - 55 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• 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

You may not qualify if:

• 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.

Sponsors & Collaborators

• Taisho Pharmaceutical R&D Inc.: lead

Study Sites (1)

PAREXEL - Early Phase Clinical Unit-Los Angeles

Glendale, California, 91206, United States

Location

Study Officials

• Taisho Director

  Taisho Pharmaceutical R&D Inc.

  STUDY DIRECTOR

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: DOUBLE
• Who Masked: PARTICIPANT, INVESTIGATOR
• Masking Details: Double-blind
• Purpose: TREATMENT
• Intervention Model: PARALLEL
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: October 18, 2018
• First Posted: November 19, 2018
• Study Start: August 21, 2015
• Primary Completion: January 13, 2016
• Study Completion: January 13, 2016
• Last Updated: November 19, 2018

Record last verified: 2018-11

Data Sharing

• IPD Sharing: Will not share

Locations

US (1)