Phase 1
N=6
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
Healthy Volunteers
Bottom Line
View on ClinicalTrials.gov: NCT04234672 ↗Enrolled (actual)
6
Serious AEs
0.0%
Results posted
Apr 2021
Primary outcome: Primary: Period 1: Percent Absolute Bioavailability (%F) for TAK-831 — 17.34 percent absolute bioavailability
Study Design & Population
- Study type
- Interventional
- Phase
- Phase 1
- Interventions
- TAK-831 Oral Tablet (Drug); [14C]TAK-831 IV Infusion (Drug); [14C]TAK-831 Oral Suspension (Drug)
- Age
- Adult · 19+ yrs
- Sex
- Male
- Sponsor
- Neurocrine Biosciences
- Primary completion
- Apr 2020
Outcome Measures
| Outcome | Result | p-value |
|---|---|---|
| PRIMARY Period 1: Percent Absolute Bioavailability (%F) for TAK-831 |
17.34 | — |
| PRIMARY Period 2: Total Radioactivity Expressed as Cumulative Percentage of Dose of [14C]TAK-831 Eliminated in Urine and Feces Combined [Combined Cum%Dose] |
88.66 | — |
| PRIMARY Period 2: Total Radioactivity Expressed as Cumulative Amount of [14C]TAK-831 Eliminated in Urine and Feces Combined (Combined CumAe) |
472.7 | — |
| PRIMARY Period 2: Percentage of Administered Radioactive Dose of [14C]TAK-831 Excreted in Urine (Cum%Dose [UR]) |
27.50 | — |
| PRIMARY Period 2: Percentage of Administered Radioactive Dose of [14C]TAK-831 Excreted in Feces (Cum%Dose [Fe]) |
60.71 | — |
| PRIMARY Period 2: Cmax: Maximum Observed Plasma Concentration of TAK-831 |
1243 | — |
| PRIMARY Period 2: Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) of TAK-831 |
0.799 | — |
| PRIMARY Period 2: t(1/2)z: Terminal Disposition Phase Half-life of TAK-831 in Plasma |
10.314 | — |
| PRIMARY Period 2: AUCinf: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity of TAK-831 |
4198 | — |
| PRIMARY Period 2: AUClast: Area Under the Plasma Concentration-time Curve From Time 0 to the Time of the Last Quantifiable Concentration of TAK-831 |
4171 | — |
| PRIMARY Period 2: Cmax: Maximum Observed Plasma Radioactivity Concentration |
5878 | — |
| PRIMARY Period 2: Tmax: Time to Reach the Maximum Plasma Radioactivity Concentration (Cmax) |
2.005 | — |
| PRIMARY Period 2: t(1/2)z: Terminal Disposition Phase Half-life of Plasma Radioactivity Concentration |
3.162 | — |
| PRIMARY Period 2: AUCinf: Area Under the Plasma Radioactivity Concentration-time Curve From Time 0 to Infinity |
31010 | — |
| PRIMARY Period 2: AUClast: Area Under the Plasma Radioactivity Concentration-time Curve From Time 0 to Last Quantifiable Concentration |
28860 | — |
| PRIMARY Period 2: Cmax: Maximum Observed Whole Blood Radioactivity Concentration |
2881 | — |
| PRIMARY Period 2: Tmax: Time to Reach the Maximum Whole Blood Radioactivity Concentration (Cmax) |
2.001 | — |
| PRIMARY Period 2: t(1/2)z: Terminal Disposition Phase Half-life of Whole Blood Radioactivity Concentration |
2.580 | — |
| PRIMARY Period 2: AUCinf: Area Under the Whole Blood Radioactivity Concentration-time Curve From Time 0 to Infinity |
15180 | — |
| PRIMARY Period 2: AUClast: Area Under the Whole Blood Radioactivity Concentration-time Curve From Time 0 to Last Quantifiable Concentration |
13420 | — |
| PRIMARY Period 2: CLR: Renal Clearance for TAK-831 in Urine |
0.06547 | — |
| SECONDARY Period 1: Ceoi: Plasma Concentration at the End of Infusion for [14C]TAK-831 |
2903 | — |
| SECONDARY Period 1: Cmax: Maximum Observed Plasma Concentration for TAK-831 After Oral Administration |
1121 | — |
| SECONDARY Period 1: Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for TAK-831 After Oral Administration |
1.255 | — |
| SECONDARY Period 1: AUCinf: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for TAK-831 After Oral Administration |
3436 | — |
| SECONDARY Period 1: AUCinf: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for [14C]TAK-831 After IV Administration |
1992 | — |
| SECONDARY Period 1: AUClast: Area Under the Plasma Concentration-time Curve From Time 0 to Last Quantifiable Concentration for TAK-831 After Oral Administration |
3397 | — |
| SECONDARY Period 1: AUClast: Area Under the Plasma Concentration-time Curve From Time 0 to Last Quantifiable Concentration for [14C]TAK-831 After IV Administration |
1972 | — |
| SECONDARY Period 1: t(1/2)z: Terminal Disposition Half-life for TAK-831 After Oral and [14C]TAK-831 After IV Administration in Plasma |
12.278; 3.815 | — |
| SECONDARY Number of Participants Reporting One or More Treatment-emergent Adverse Events (TEAEs) |
0; 0; 2 | — |
| SECONDARY Number of Participants With TEAEs Related to Electrocardiogram (ECG) |
0; 0; 0 | — |
| SECONDARY Number of Participants With TEAEs Related to Vital Signs |
0; 0; 0 | — |
| SECONDARY Number of Participants With TEAEs Related to Laboratory Parameters |
0; 0; 0 | — |
Summary
The purpose of this study is to determine ABA of TAK-831 following a single microdose intravenous administration of 50 microgram (μg) (approximately 1 microcurie [μCi]) [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 μCi) [14C]TAK-831 in Period 2.
Eligibility Criteria
Inclusion Criteria
- 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
- Seated blood pressure is less than 90/40 millimeter of mercury (mmHg) or greater than 140/90 mmHg at screening.
- Seated heart rate is lower than 40 beats per minute (bpm) or higher than 99 bpm at screening.
- Estimated creatinine clearance <80 milliliter per minute (mL/min) at screening.
- 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.
- Has infrequent bowel movements (less than approximately once per day) within 30 days prior to first dosing.
- 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]).
- 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.
- Donation of blood or significant blood loss within 56 days prior to the first dosing.
- Plasma donation within 7 days prior to the first dosing.
Data sourced from ClinicalTrials.gov (NCT04234672). Outcome figures and adverse-event rates are extracted automatically from the registry's posted results and are provided for clinician reference, not as a substitute for the primary publication.