A Study to Assess Absolute Bioavailability (ABA) of TAK-831 and to Characterize Mass Balance, Pharmacokinetics (PK), Metabolism, and Excretion of [14C] TAK-831 in Male Healthy Participants

Overview

The purpose of this study is to determine ABA of TAK-831 following a single microdose intravenous administration of 50 microgram (mcg) (approximately 1 microcurie [mcCi]) [14C] TAK-831 and a single oral administration of 500 milligram (mg) TAK-831 tablets in Period 1, and to assess the mass balance, characterize the PK of TAK-831 in plasma and urine, and total radioactivity concentration equivalents in plasma and whole blood following a single oral suspension dose of 500 mg (approximately 100 mcCi) [14C]TAK-831 in Period 2.

Full Title of Study: “A Phase 1 Study to Assess Absolute Bioavailability of TAK-831 and to Characterize Mass Balance, Pharmacokinetics, Metabolism, and Excretion of [14C]TAK-831 in Male Healthy Subjects”

Study Type

  • Study Type: Interventional
  • Study Design
    • Allocation: N/A
    • Intervention Model: Single Group Assignment
    • Primary Purpose: Other
    • Masking: None (Open Label)
  • Study Primary Completion Date: April 4, 2020

Detailed Description

The drug being tested in this study is called TAK-831. The study will determine ABA in Period 1, and the absorption, metabolism, excretion, and mass balance of TAK-831 after single oral administration in Period 2 in healthy adult male participants, by collecting plasma, urine, and feces samples for drug concentration analysis, and plasma, whole blood, urine, and fecal samples for total radioactivity analysis and metabolic profiling.

The study will enroll approximately 6 participants. The study is designed to consist of 2 periods: Period 1 (ABA study period) and Period 2 (absorption, distribution, metabolism, and elimination [ADME] study period). In Period 1 (ABA study period), all participants will receive single unlabeled oral dose of TAK-831 as tablet and microdose of 50 mcg (approximately 1 mcCi) [14C]TAK-831 as intravenous infusion, followed by a washout period of at least 7 days before the dose in Period 2. In Period 2 (ADME study period), all participants will receive a single dose of 500 mg (approximately 100 mcCi) [14C]TAK-831 as an oral suspension.

This single center trial will be conducted in the United States. The overall time to participate in this study is approximately 65 days including screening period. Participants will be contacted approximately 30 days after the last dose of study drug for a follow-up assessment.

Interventions

  • Drug: TAK-831 Oral Tablet
    • TAK-831 tablet.
  • Drug: [14C]TAK-831 Intravenous Infusion
    • [14C]TAK-831 intravenous infusion.
  • Drug: [14C]TAK-831 Oral Suspension
    • [14C]TAK-831 oral suspension.

Arms, Groups and Cohorts

  • Experimental: TAK-831 500 mg + [14C]TAK-831 50 mcg + [14C]TAK-831 500 mg
    • TAK-831 500 mg, tablet, orally, once on Day 1, followed by [14C]TAK-831 50 mcg (approximately 1 mcCi), infusion, intravenously, once on Day 1 of Period 1, followed by a washout period of at least 7 days, further followed by [14C]TAK-831 500 mg (approximately 100 mcCi), suspension, orally, once under fasted state on Day 1 of Period 2.

Clinical Trial Outcome Measures

Primary Measures

  • Period 1: Percent Absolute Bioavailability (%F) for TAK-831
    • Time Frame: Day 1 pre-dose and at multiple time points (up to 96.5 hours) post-dose
  • Period 2: Percentage of Total Radioactivity Recovered in Urine (Cum%Dose[UR]) and Feces (Cum%Dose[Fe]) Relative to the Administered Radioactive Dose (Combined Cum%Dose)
    • Time Frame: Day 1 pre-dose and at multiple time points (up to 672 hours) post-dose
  • Period 2, Ae(UR): Cumulative Amount of Total Radioactivity Excreted in Urine
    • Time Frame: Day 1 pre-dose and at multiple time points (up to 672 hours) post-dose
  • Period 2, Ae(Fe): Cumulative Amount of Total Radioactivity Excreted in Feces
    • Time Frame: Day 1 pre-dose and at multiple time points (up to 672 hours) post-dose
  • Period 2: Percentage of Administered Radioactive Dose Excreted in Urine (%Dose[UR]) and Feces (%Dose[Fe])
    • Time Frame: Day 1 pre-dose and at multiple time points (up to 672 hours) post-dose
  • Period 2, Cmax: Maximum Observed Plasma Concentration for TAK-831
    • Time Frame: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose
  • Period 2, Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for TAK-831
    • Time Frame: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose
  • Period 2, t(1/2): Terminal Disposition Phase Half-life of TAK-831
    • Time Frame: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose
  • Period 2, AUC∞: Area Under the Plasma Concentration-time Curve from Time 0 to Infinity for TAK-831
    • Time Frame: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose
  • Period 2, AUClast: Area Under the Plasma Concentration-time Curve From Time 0 to the Time of the Last Quantifiable Concentration for TAK-831
    • Time Frame: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose
  • Period 2, Cmax: Maximum Observed Plasma and Whole Blood Radioactivity Concentration for [14C]TAK-831
    • Time Frame: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose
  • Period 2, Tmax: Time to Reach the Maximum Plasma and Whole Blood Radioactivity Concentration (Cmax) for [14C]TAK-831
    • Time Frame: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose
  • Period 2, t(1/2): Terminal Disposition Phase Half-life of Plasma and Whole Blood Radioactivity Concentration for [14C]TAK-831
    • Time Frame: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose
  • Period 2, AUC∞: Area Under the Plasma and Whole Blood Radioactivity Concentration-time Curve from Time 0 to Infinity for [14C]TAK-831
    • Time Frame: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose
  • Period 2, AUClast: Area Under the Plasma and Whole Blood Radioactivity Concentration-time Curve from Time 0 to Last Quantifiable Concentration for [14C]TAK-831
    • Time Frame: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose
  • Period 2, CLR: Renal Clearance for TAK-831 in Urine
    • Time Frame: Day 1 pre-dose and at multiple time points (up to 672 hours) post-dose

Secondary Measures

  • Period 1: Ceoi: Plasma Concentration at the end of Infusion for [14C]TAK-831
    • Time Frame: Day 1 pre-dose and at multiple time points (up to 95 hours) post-dose
  • Period 1, Cmax: Maximum Observed Plasma Concentration for TAK-831 After Oral Administration
    • Time Frame: Day 1 pre-dose and at multiple time points (up to 96.5 hours) post-dose
  • Period 1, Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for TAK-831 After Oral Administration
    • Time Frame: Day 1 pre-dose and at multiple time points (up to 96.5 hours) post-dose
  • Period 1, AUC∞: Area under the Plasma Concentration-time Curve from Time 0 to Infinity for TAK-831 and [14C]TAK-831
    • Time Frame: Day 1 pre-dose and at multiple time points (up to 96.5 hours) post-dose
  • Period 1, AUClast: Area under the Plasma Concentration-time Curve from Time 0 to Last Quantifiable Concentration for TAK-831 and [14C]TAK-831
    • Time Frame: Day 1 pre-dose and at multiple time points (up to 96.5 hours) post-dose
  • Period 1: t(1/2) : Terminal Disposition Half-life for TAK-831 and [14C]TAK-831
    • Time Frame: Day 1 pre-dose and at multiple time points (up to 96.5 hours) post-dose
  • Number of Participants Reporting one or More Treatment-emergent Adverse Events (TEAEs)
    • Time Frame: Baseline up to 30 days after last dose of study drug in Period 2 (Day 38)
  • Number of Participants with TEAEs Related to Electrocardiogram (ECG)
    • Time Frame: Baseline up to 30 days after last dose of study drug in Period 2 (Day 38)
  • Number of Participants with TEAEs Related to Vital Signs
    • Time Frame: Baseline up to 30 days after last dose of study drug in Period 2 (Day 38)
  • Number of Participants with TEAEs Categorized into Investigations System Organ Class (SOC) Related to Laboratory Values
    • Time Frame: Baseline up to 30 days after last dose of study drug in Period 2 (Day 38)

Participating in This Clinical Trial

Inclusion Criteria

1. Weighs at least 45 kilogram (kg) and body mass index (BMI) greater than or equal to (>=) 18.0 and less than (˂) 32.0 kilogram per square meter (kg/m^2) at screening.

Exclusion Criteria

1. Seated blood pressure is less than 90/40 millimeter of mercury (mmHg) or greater than 140/90 mmHg at screening.

2. Seated heart rate is lower than 40 beats per minute (bpm) or higher than 99 bpm at screening.

3. Estimated creatinine clearance <80 milliliter per minute (mL/min) at screening.

4. Has tattoo(s) or scarring at or near the site of intravenous infusion or any other condition which may interfere with infusion site examination, in the opinion of the Investigator.

5. Has infrequent bowel movements (less than approximately once per day) within 30 days prior to first dosing.

6. Has received radiolabeled substances or has been exposed to radiation sources within 12 months of first dosing or is likely to receive radiation exposure or radioisotopes within 12 months of first dosing such that participation in this study would increase their total exposure beyond the recommended levels considered safe (that is weighted annual limit recommended by the International Commission on Radiological Protection [ICRP] of 3000 milli roentgen equivalent man [mrem]).

7. Has been on a diet incompatible with the on-study diet, in the opinion of the Investigator or designee, within the 30 days prior to the first dosing and throughout the study.

8. Donation of blood or significant blood loss within 56 days prior to the first dosing.

9. Plasma donation within 7 days prior to the first dosing.

Gender Eligibility: Male

Minimum Age: 19 Years

Maximum Age: 55 Years

Are Healthy Volunteers Accepted: Accepts Healthy Volunteers

Investigator Details

  • Lead Sponsor
    • Takeda
  • Provider of Information About this Clinical Study
    • Sponsor
  • Overall Official(s)
    • Medical Director, Study Director, Takeda

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