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Clinical trial information and results are updated daily from ClinicalTrials.gov. The latest data update was conducted on 01/16/2021.

First-in-Human Study With Single and Multiple Doses of TS-161 in Healthy Participants

Clinicaltrials.gov identifier NCT03919409

Recruitment Status Completed

First Posted April 18, 2019

Last update posted February 28, 2020

Study Description

Brief summary:

This is a Phase 1, first-in-human study involving single and multiple oral doses of TS-161 in healthy male and female participants. The safety, tolerability, pharmacokinetics and pharmacodynamics of TS-161 will be evaluated. The study includes 3 parts; Part A (single ascending dose: Cohorts 1 to 5) , Part B (single dose, cerebrospinal fluid [CSF] collection: Cohort 6), and Part C (multiple ascending dose: Cohorts 7 to 9). Participants will be assigned to one of the 9 Cohorts.

  • Condition or Disease:Healthy Volunteers
  • Intervention/Treatment: Drug: TS-161
    Drug: TS-161 Placebo
  • Phase: Phase 1
Detailed Description

N/A

Study Design
  • Study Type: Interventional
  • Actual Enrollment: 70 participants
  • Allocation: Randomized
  • Intervention Model: Parallel Assignment
  • Masking: Double (Participant, Investigator)
  • Primary Purpose: Treatment
  • Official Title: A Randomized, Double-blind, Placebo-controlled, Single and Multiple Ascending Dose Study to Evaluate the Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of TS-161 Administered Orally to Healthy Male and Female Participants
  • Actual Study Start Date: June 2019
  • Actual Primary Completion Date: February 2020
  • Actual Study Completion Date: February 2020
Arms and interventions
Arm Intervention/treatment
Experimental: Part A: Cohort 1: TS-161 15 mg
Single dose of TS-161 15 mg or placebo in a fasted condition.
Drug: TS-161
TS-161 capsules

Drug: TS-161 Placebo
TS-161 matching placebo capsules
Experimental: Part A: Cohort 2: TS-161 50 mg
Single dose of TS-161 50 mg or placebo which will be dosed first in a fasted condition, and then in a fed condition, with a washout period in between 2 dosing. Although planned, all subsequent dose levels after Cohort 1 will be determined based on the results from the preceding cohorts.
Drug: TS-161
TS-161 capsules

Drug: TS-161 Placebo
TS-161 matching placebo capsules
Experimental: Part A: Cohort 3: TS-161 100 mg
Single dose of TS-161 100 mg or placebo in a fasted condition. Although planned, all subsequent dose levels after Cohort 1 will be determined based on the results from the preceding cohorts.
Drug: TS-161
TS-161 capsules

Drug: TS-161 Placebo
TS-161 matching placebo capsules
Experimental: Part A: Cohort 4: TS-161 200 mg
Single dose of TS-161 200 mg or placebo in a fasted condition. Although planned, all subsequent dose levels after Cohort 1 will be determined based on the results from the preceding cohorts.
Drug: TS-161
TS-161 capsules

Drug: TS-161 Placebo
TS-161 matching placebo capsules
Experimental: Part A: Cohort 5: TS-161 400 mg
Single dose of TS-161 400 mg or placebo in a fasted condition. Although planned, all subsequent dose levels after Cohort 1 will be determined based on the results from the preceding cohorts.
Drug: TS-161
TS-161 capsules

Drug: TS-161 Placebo
TS-161 matching placebo capsules
Experimental: Part B: Cohort 6: TS-161 TBD
Single dose of TS-161 in a fasted condition. The dose level will be determined based on the results from the preceding cohorts.
Drug: TS-161
TS-161 capsules
Experimental: Part C: Cohort 7: TS-161 TBD
Daily doses of TS-161 or placebo for 10 days in a fed condition. The dose level will be determined based on the results from the preceding cohorts.
Drug: TS-161
TS-161 capsules

Drug: TS-161 Placebo
TS-161 matching placebo capsules
Experimental: Part C: Cohort 8: TS-161 TBD
Daily doses of TS-161 or placebo for 10 days in a fed condition. The dose level will be determined based on the results from the preceding cohorts.
Drug: TS-161
TS-161 capsules

Drug: TS-161 Placebo
TS-161 matching placebo capsules
Experimental: Part C: Cohort 9: TS-161 TBD
Daily doses of TS-161 or placebo for 10 days in a fed condition. The dose level will be determined based on the results from the preceding cohorts.
Drug: TS-161
TS-161 capsules

Drug: TS-161 Placebo
TS-161 matching placebo capsules
Outcome Measures
  • Primary Outcome Measures: 1. Incidence and severity of Adverse Events [ Time Frame: Parts A and B: Day 1 to Day 8; Part C: Day 1 to Day 17 ]
  • 2. TS-161 Plasma Pharmacokinetic Profile - Cmax [ Time Frame: Parts A and B: Day 1 predose and at multiple time points (up to 48 hours) postdose; Part C: Day 1 predose and at multiple time points (up to 12 hours) postdose, Day 2 to Day 9 predose, Day 10 predose and at multiple time points (up to 48 hours) postdose ]
    Maximum plasma concentration
  • 3. TS-161 Plasma Pharmacokinetic Profile - Tmax [ Time Frame: Parts A and B: Day 1 predose and at multiple time points (up to 48 hours) postdose; Part C: Day 1 predose and at multiple time points (up to 12 hours) postdose, Day 2 to Day 9 predose, Day 10 predose and at multiple time points (up to 48 hours) postdose ]
    Time to maximum plasma concentration
  • 4. TS-161 Plasma Pharmacokinetic Profile - AUC(0-last) [ Time Frame: Parts A and B: Day 1 predose and at multiple time points (up to 48 hours) postdose ]
    Area under the plasma concentration versus time curve from time zero to last measurable concentration
  • 5. TS-161 Plasma Pharmacokinetic Profile - AUC(0-tau) [ Time Frame: Part C: Day 1 predose and at multiple time points (up to 12 hours) postdose, Day 2 to Day 9 predose, Day 10 predose and at multiple time points (up to 48 hours) postdose ]
    Area under the plasma concentration versus time curve over a dosing interval
  • 6. TS-161 Plasma Pharmacokinetic Profile - T1/2 [ Time Frame: Parts A and B: Day 1 predose and at multiple time points (up to 48 hours) postdose; Part C: Day 1 predose and at multiple time points (up to 12 hours) postdose, Day 2 to Day 9 predose, Day 10 predose and at multiple time points (up to 48 hours) postdose ]
    Apparent terminal elimination half-life
  • 7. TS-161 Plasma Pharmacokinetic Profile - CL/F [ Time Frame: Parts A and B: Day 1 predose and at multiple time points (up to 48 hours) postdose; Part C: Day 1 predose and at multiple time points (up to 12 hours) postdose, Day 2 to Day 9 predose, Day 10 predose and at multiple time points (up to 48 hours) postdose ]
    Apparent clearance following oral administration
  • 8. TS-161 Plasma Pharmacokinetic Profile - Vd,z/F [ Time Frame: Parts A and B: Day 1 predose and at multiple time points (up to 48 hours) postdose; Part C: Day 1 predose and at multiple time points (up to 12 hours) postdose, Day 2 to Day 9 predose, Day 10 predose and at multiple time points (up to 48 hours) postdose ]
    Apparent volume of distribution following oral administration
  • 9. TS-161 Urine Pharmacokinetic Profile - Ae [ Time Frame: Part A: Day 1 predose and pooled for multiple intervals (up to 48 hours) postdose; Part C: Day 1 predose and pooled for multiple intervals (up to 48 hours after last dose) postdose ]
    Amount excreted in urine
  • 10. TS-161 Urine Pharmacokinetic Profile - Fe% [ Time Frame: Part A: Day 1 predose and pooled for multiple intervals (up to 48 hours) postdose; Part C: Day 1 predose and pooled for multiple intervals (up to 48 hours after last dose) postdose ]
    Percent of dose excreted in urine
  • 11. TS-161 Urine Pharmacokinetic Profile - CLr [ Time Frame: Part A: Day 1 predose and pooled for multiple intervals (up to 48 hours) postdose; Part C: Day 1 predose and pooled for multiple intervals (up to 48 hours after last dose) postdose ]
    Renal Clearance
  • Secondary Outcome Measures: 1. TS-161 CSF Pharmacokinetic Profile - Cmax [ Time Frame: Part B: Day 1 predose and at multiple time points (up to 24 hours) postdose ]
    Maximum CSF concentration
  • 2. TS-161 CSF Pharmacokinetic Profile - Tmax [ Time Frame: Part B: Day 1 predose and at multiple time points (up to 24 hours) postdose ]
    Time to maximum CSF concentration
  • 3. TS-161 CSF Pharmacokinetic Profile - AUC(0-last) [ Time Frame: Part B: Day 1 predose and at multiple time points (up to 24 hours) postdose ]
    Area under the CSF concentration versus time curve from time zero to last
  • 4. TS-161 CSF Pharmacokinetic Profile - T1/2 [ Time Frame: Part B: Day 1 predose and at multiple time points (up to 24 hours) postdose ]
    Apparent terminal elimination half-life
  • 5. Changes from baseline in relative and absolute powers of the delta, theta, alpha, beta and gamma bands using quantitative electroencephalogram (qEEG) compared to placebo [ Time Frame: Part A: predose and at multiple time points (up to 8 hours) postdose ]
Eligibility Criteria
  • Ages Eligible for Study: 18 to 55 Years (Adult)
  • Sexes Eligible for Study: All
  • Accepts Healthy Volunteers: Yes
Criteria

Inclusion Criteria:

- Healthy adult male and female participants between 18 and 55 years of age, inclusive

- Body weight ≥ 45 kg

- Body Mass Index (BMI) 18 - 30 kg/m^2, inclusive

Exclusion Criteria:

- Significant history or presence of medical disorders or condition capable of
significantly affecting the absorption, metabolism, or elimination of drugs

- History or presence of psychiatric or neurologic disease or condition

- History of seizures

- Abnormal EEG observed at screening

- Abnormal blood pressure

- Breast cancer within the past 10 years, or any other malignancies within the past 5
years

- Clinically significant abnormal results in electrocardiogram, blood and urine test

- History or presence of liver disease

- Participants using medication or supplements within 14 days prior to dosing

- Use of N-methyl-D-aspartate (NMDA) receptor modulators (example: dextromethorphan,
ketamine, amantadine, memantine) within 90 days of screening

- Loss of blood or blood products in excess of 450 mL within 60 days prior to screening

- Used any investigational drug within 60 days prior to screening

- Recent history of alcohol or drug abuse

- Any participant who currently uses or has used tobacco products or nicotine-containing
products (cigarettes, pipes, e-cigarettes, nicotine patches, etc.) for one month or
more prior to screening

Exclusion Criteria for Part B only:

- Significant abnormalities in lumbar spine

- History of clinically significant back pain, back pathology, and/or back injury

- History of migraines, and/or frequent, severe headaches

- History or presence of significant active bleeding or coagulation disorder or use of
non-steroidal anti-inflammatory drugs or other drugs that affect coagulation or
platelet function within 14 days prior to lumbar catheter insertion

- Allergy to lidocaine (Xylocaine®) or related drugs

- History of adverse reaction to lumbar puncture or epidural procedure

Contacts and Locations
Contacts
Locations

United States, California
PAREXEL - Early Phase Clinical Unit-Los Angeles
Glendale

Sponsors and Collaborators

Taisho Pharmaceutical R&D Inc.

Investigators

Study Director: Taisho Director Taisho Pharmaceutical R&D Inc.

More Information
  • Responsible Party: Taisho Pharmaceutical R&D Inc.
  • ClinicalTrials.gov Identifier: NCT03919409 History of Changes
  • Other Study ID Numbers: TS161-US101
  • First Posted: April 18, 2019 Key Record Dates
  • Last Update Posted: February 28, 2020
  • Last Verified: February 2020
  • Individual Participant
    Data (IPD) Sharing
    Statement:
  • Plan to Share IPD: No
  • Studies a U.S. FDA-regulated Drug Product: Yes
  • Studies a U.S. FDA-regulated Device Product: No
  • Keywords provided by Taisho Pharmaceutical R&D Inc.: TS-161
    CSF
    first-in-human