Trial Outcomes & Findings for A Study to Evaluate the Mass Balance, Pharmacokinetics (PK), Metabolism and Excretion of TAK-954 Containing Microtracer ([14C]-TAK-954) in Healthy Male Participants (NCT NCT03500224)

NCT ID: NCT03500224

Last Updated: 2019-07-29

Results Overview

Recruitment status

COMPLETED

Study phase

PHASE1

Target enrollment

6 participants

Primary outcome timeframe

Day 1 pre-dose and at multiple time points (up to 264, 312, and 336 hours) post-dose

Results posted on

2019-07-29

Participant Flow

Participants took part in the study at 1 investigative site in the Netherlands from 30 April 2018 to 01 June 2018.

Healthy participants were enrolled to receive a single 60-minute intravenous infusion of 0.5 milligram (mg) TAK-954 containing a microtracer of \[14C\]-TAK-954.

Participant milestones

Participant milestones
Measure
[14C]-TAK-954 0.5 mg
\[14C\]-TAK-954 0.5 mg (containing approximately 1.5 µCi) of radioactive tracer administered as a 60-minute infusion, intravenously, once on Day 1.
Overall Study
STARTED
6
Overall Study
COMPLETED
4
Overall Study
NOT COMPLETED
2

Reasons for withdrawal

Reasons for withdrawal
Measure
[14C]-TAK-954 0.5 mg
\[14C\]-TAK-954 0.5 mg (containing approximately 1.5 µCi) of radioactive tracer administered as a 60-minute infusion, intravenously, once on Day 1.
Overall Study
Withdrawal by Subject
2

Baseline Characteristics

A Study to Evaluate the Mass Balance, Pharmacokinetics (PK), Metabolism and Excretion of TAK-954 Containing Microtracer ([14C]-TAK-954) in Healthy Male Participants

Baseline characteristics by cohort

Baseline characteristics by cohort
Measure
[14C]-TAK-954 0.5 mg
n=6 Participants
\[14C\]-TAK-954 0.5 mg (containing approximately 1.5 µCi) of radioactive tracer administered as a 60-minute infusion, intravenously, once on Day 1.
Age, Continuous
39.5 years
STANDARD_DEVIATION 13.98 • n=5 Participants
Sex: Female, Male
Female
0 Participants
n=5 Participants
Sex: Female, Male
Male
6 Participants
n=5 Participants
Ethnicity (NIH/OMB)
Hispanic or Latino
0 Participants
n=5 Participants
Ethnicity (NIH/OMB)
Not Hispanic or Latino
6 Participants
n=5 Participants
Ethnicity (NIH/OMB)
Unknown or Not Reported
0 Participants
n=5 Participants
Race (NIH/OMB)
American Indian or Alaska Native
0 Participants
n=5 Participants
Race (NIH/OMB)
Asian
1 Participants
n=5 Participants
Race (NIH/OMB)
Native Hawaiian or Other Pacific Islander
0 Participants
n=5 Participants
Race (NIH/OMB)
Black or African American
0 Participants
n=5 Participants
Race (NIH/OMB)
White
5 Participants
n=5 Participants
Race (NIH/OMB)
More than one race
0 Participants
n=5 Participants
Race (NIH/OMB)
Unknown or Not Reported
0 Participants
n=5 Participants
Region of Enrollment
Netherlands
6 Participants
n=5 Participants
Weight
76.37 kilogram (kg)
STANDARD_DEVIATION 8.694 • n=5 Participants
Height
177.2 centimeter (cm)
STANDARD_DEVIATION 7.78 • n=5 Participants
Body mass index
24.2 kilogram per square meter (kg/m^2)
STANDARD_DEVIATION 1.72 • n=5 Participants

PRIMARY outcome

Timeframe: Day 1 pre-dose and at multiple time points (up to 264, 312, and 336 hours) post-dose

Population: The pharmacokinetic (PK) analysis set included all the participants of safety analysis set with sufficient concentration data to facilitate the derivation of at least 1 PK parameter from the concentration time data. The PK analysis set where data at specified time points was available.

Outcome measures

Outcome measures
Measure
[14C]-TAK-954 0.5 mg
n=6 Participants
\[14C\]-TAK-954 0.5 mg (containing approximately 1.5 µCi) of radioactive tracer administered as a 60-minute infusion, intravenously, once on Day 1.
Cumulative Percentage of Administered Radioactivity Recovered in Urine
0 to 264 hours
55.4 percentage of radioactive dose
Standard Deviation 3.2
Cumulative Percentage of Administered Radioactivity Recovered in Urine
0 to 312 hours
56.8 percentage of radioactive dose
Standard Deviation 3.2
Cumulative Percentage of Administered Radioactivity Recovered in Urine
0 to 336 hours
55.1 percentage of radioactive dose
Standard Deviation 0.4

PRIMARY outcome

Timeframe: Day 1 pre-dose and at multiple time points (up to 264, 312, and 336 hours) post-dose

Population: The PK analysis set included all the participants of safety analysis set with sufficient concentration data to facilitate the derivation of at least 1 PK parameter from the concentration time data. The PK analysis set where data at specified time points was available.

Outcome measures

Outcome measures
Measure
[14C]-TAK-954 0.5 mg
n=6 Participants
\[14C\]-TAK-954 0.5 mg (containing approximately 1.5 µCi) of radioactive tracer administered as a 60-minute infusion, intravenously, once on Day 1.
Cumulative Percentage of Administered Radioactivity Recovered in Feces
0 to 264 hours
28.8 percentage of radioactive dose
Standard Deviation 2.5
Cumulative Percentage of Administered Radioactivity Recovered in Feces
0 to 312 hours
30.3 percentage of radioactive dose
Standard Deviation 2.5
Cumulative Percentage of Administered Radioactivity Recovered in Feces
0 to 336 hours
30.0 percentage of radioactive dose
Standard Deviation 3.5

PRIMARY outcome

Timeframe: Day 1 pre-dose and at multiple time points (up to 264, 312, and 336 hours) post-dose

Population: The PK analysis set included all the participants of safety analysis set with sufficient concentration data to facilitate the derivation of at least 1 PK parameter from the concentration time data. The PK analysis set where data at specified time points was available.

Outcome measures

Outcome measures
Measure
[14C]-TAK-954 0.5 mg
n=6 Participants
\[14C\]-TAK-954 0.5 mg (containing approximately 1.5 µCi) of radioactive tracer administered as a 60-minute infusion, intravenously, once on Day 1.
Cumulative Percentage of Radioactivity in Urine and Feces Combined
0 to 312 hours
87.0 percentage of radioactive dose
Standard Deviation 4.6
Cumulative Percentage of Radioactivity in Urine and Feces Combined
0 to 264 hours
84.1 percentage of radioactive dose
Standard Deviation 5.3
Cumulative Percentage of Radioactivity in Urine and Feces Combined
0 to 336 hours
85.1 percentage of radioactive dose
Standard Deviation 3.9

PRIMARY outcome

Timeframe: Day 1 pre-dose and at multiple time points (up to 168 hours) post-dose

Population: PK analysis set: All participants of safety set with sufficient data to facilitate at least 1 PK parameter from concentration time data. Single value is available for Metabolite (M) 16, M4, and M5 because they co-eluted under chromatographic conditions. Single sampling method used across participants, therefore there was no measure of dispersion.

Percentage of dose recovered for TAK-954 and its metabolites derived from 0-168 hour sampling was normalized for 100% recovery.

Outcome measures

Outcome measures
Measure
[14C]-TAK-954 0.5 mg
n=6 Participants
\[14C\]-TAK-954 0.5 mg (containing approximately 1.5 µCi) of radioactive tracer administered as a 60-minute infusion, intravenously, once on Day 1.
Normalized Recovery as Percentage of Dose for TAK-954 and TAK-954 Metabolites in Urine and Feces Combined
M4, M5, and M16
5.0 percentage of dose
Normalized Recovery as Percentage of Dose for TAK-954 and TAK-954 Metabolites in Urine and Feces Combined
M17
1.6 percentage of dose
Normalized Recovery as Percentage of Dose for TAK-954 and TAK-954 Metabolites in Urine and Feces Combined
M9
0.6 percentage of dose
Normalized Recovery as Percentage of Dose for TAK-954 and TAK-954 Metabolites in Urine and Feces Combined
M1
3.0 percentage of dose
Normalized Recovery as Percentage of Dose for TAK-954 and TAK-954 Metabolites in Urine and Feces Combined
M3
13.6 percentage of dose
Normalized Recovery as Percentage of Dose for TAK-954 and TAK-954 Metabolites in Urine and Feces Combined
M14
4.3 percentage of dose
Normalized Recovery as Percentage of Dose for TAK-954 and TAK-954 Metabolites in Urine and Feces Combined
M7
0.5 percentage of dose
Normalized Recovery as Percentage of Dose for TAK-954 and TAK-954 Metabolites in Urine and Feces Combined
M10
1.0 percentage of dose
Normalized Recovery as Percentage of Dose for TAK-954 and TAK-954 Metabolites in Urine and Feces Combined
TAK-954
58.0 percentage of dose

PRIMARY outcome

Timeframe: Day 1 pre-dose and at multiple time points (up to 168 hours) post-dose

Population: PK analysis set: All participants of safety set with sufficient data to facilitate at least 1 PK parameter from concentration time data. Single value is available for Metabolite (M) 16, M4, and M5 because they co-eluted under chromatographic conditions. Single sampling method used across participants, therefore there was no measure of dispersion.

Percentage of dose recovered for TAK-954 and its metabolites derived from 0-168 hour sampling was normalized for 100% recovery.

Outcome measures

Outcome measures
Measure
[14C]-TAK-954 0.5 mg
n=6 Participants
\[14C\]-TAK-954 0.5 mg (containing approximately 1.5 µCi) of radioactive tracer administered as a 60-minute infusion, intravenously, once on Day 1.
Normalized Recovery as Percentage of Dose for TAK-954 and TAK-954 Metabolites in Urine
M1
3.0 Percentage of dose
Normalized Recovery as Percentage of Dose for TAK-954 and TAK-954 Metabolites in Urine
M3
4.8 Percentage of dose
Normalized Recovery as Percentage of Dose for TAK-954 and TAK-954 Metabolites in Urine
M14
4.3 Percentage of dose
Normalized Recovery as Percentage of Dose for TAK-954 and TAK-954 Metabolites in Urine
M5, M4, and M16
1.6 Percentage of dose
Normalized Recovery as Percentage of Dose for TAK-954 and TAK-954 Metabolites in Urine
M17
0.8 Percentage of dose
Normalized Recovery as Percentage of Dose for TAK-954 and TAK-954 Metabolites in Urine
M9
0.6 Percentage of dose
Normalized Recovery as Percentage of Dose for TAK-954 and TAK-954 Metabolites in Urine
M10
0.5 Percentage of dose
Normalized Recovery as Percentage of Dose for TAK-954 and TAK-954 Metabolites in Urine
TAK-954
44.3 Percentage of dose

PRIMARY outcome

Timeframe: Day 1 pre-dose and at multiple time points (up to 168 hours) post-dose

Population: PK analysis set: All participants of safety set with sufficient data to facilitate at least 1 PK parameter from concentration time data. Single value is available for Metabolite (M) 16, M4, and M5 because they co-eluted under chromatographic conditions. Single sampling method used across participants, therefore there was no measure of dispersion.

Percentage of dose recovered for TAK-954 and its metabolites derived from 0-168 hour sampling was normalized for 100% recovery.

Outcome measures

Outcome measures
Measure
[14C]-TAK-954 0.5 mg
n=6 Participants
\[14C\]-TAK-954 0.5 mg (containing approximately 1.5 µCi) of radioactive tracer administered as a 60-minute infusion, intravenously, once on Day 1.
Normalized Recovery as Percentage of Dose for TAK-954 and TAK-954 Metabolites in Feces
M3
8.8 percentage of dose
Normalized Recovery as Percentage of Dose for TAK-954 and TAK-954 Metabolites in Feces
M5, M4, and M16
3.4 percentage of dose
Normalized Recovery as Percentage of Dose for TAK-954 and TAK-954 Metabolites in Feces
M17
0.8 percentage of dose
Normalized Recovery as Percentage of Dose for TAK-954 and TAK-954 Metabolites in Feces
M7
0.5 percentage of dose
Normalized Recovery as Percentage of Dose for TAK-954 and TAK-954 Metabolites in Feces
M10
0.5 percentage of dose
Normalized Recovery as Percentage of Dose for TAK-954 and TAK-954 Metabolites in Feces
TAK-954
13.7 percentage of dose

PRIMARY outcome

Timeframe: Day 1 pre-dose and at multiple time points (up to 168 hours) post-dose

Population: The PK analysis set included all the participants of safety analysis set with sufficient concentration data to facilitate the derivation of at least 1 PK parameter from the concentration time data. Data is reported for TAK-954. Data for metabolites are not reported because none exceeded greater than (\>) 6% of the total plasma radioactivity.

Outcome measures

Outcome measures
Measure
[14C]-TAK-954 0.5 mg
n=6 Participants
\[14C\]-TAK-954 0.5 mg (containing approximately 1.5 µCi) of radioactive tracer administered as a 60-minute infusion, intravenously, once on Day 1.
Mean Percent of Total Radioactivity in Plasma for TAK-954 and TAK-954 Metabolites
74.28 percentage of total radioactivity
Standard Deviation 8.18

PRIMARY outcome

Timeframe: Day 1 pre-dose and at multiple time points (up to 264, 312, and 336 hours) post-dose

Population: The PK analysis set included all the participants of safety analysis set with sufficient concentration data to facilitate the derivation of at least 1 PK parameter from the concentration time data. The PK analysis set where data at specified time points was available.

Outcome measures

Outcome measures
Measure
[14C]-TAK-954 0.5 mg
n=6 Participants
\[14C\]-TAK-954 0.5 mg (containing approximately 1.5 µCi) of radioactive tracer administered as a 60-minute infusion, intravenously, once on Day 1.
Cumulative Percentage of Dose Excreted in Urine for TAK-954
0 to 336 hours
27.35 percentage of dose
Standard Deviation 0.35
Cumulative Percentage of Dose Excreted in Urine for TAK-954
0 to 264 hours
31.33 percentage of dose
Standard Deviation 3.29
Cumulative Percentage of Dose Excreted in Urine for TAK-954
0 to 312 hours
29.73 percentage of dose
Standard Deviation 4.14

PRIMARY outcome

Timeframe: Day 1 pre-dose and at multiple time points (up to 168 hours) post-dose

Population: The PK analysis set included all the participants of safety analysis set with sufficient concentration data to facilitate the derivation of at least 1 PK parameter from the concentration time data. Single sampling method used across participants, therefore there was no measure of dispersion.

The cumulative percentage of dose excreted in feces as TAK-954 derived from 0-168 hour sampling was normalized for 100% recovery.

Outcome measures

Outcome measures
Measure
[14C]-TAK-954 0.5 mg
n=6 Participants
\[14C\]-TAK-954 0.5 mg (containing approximately 1.5 µCi) of radioactive tracer administered as a 60-minute infusion, intravenously, once on Day 1.
Cumulative Percentage of Dose Excreted in Feces for TAK-954
13.7 percentage of dose

PRIMARY outcome

Timeframe: Day 1 pre-dose and at multiple time points (up to 336 hours) post-dose

Population: The PK analysis set included all the participants of safety analysis set with sufficient concentration data to facilitate the derivation of at least 1 PK parameter from the concentration time data. The PK analysis set where data at specified time points was available.

Outcome measures

Outcome measures
Measure
[14C]-TAK-954 0.5 mg
n=6 Participants
\[14C\]-TAK-954 0.5 mg (containing approximately 1.5 µCi) of radioactive tracer administered as a 60-minute infusion, intravenously, once on Day 1.
Mean Concentration of Total Radioactivity in Whole Blood and Plasma [14C]-TAK-954
Whole Blood: 1.5 hour
2.88 nanogram equivalent/milliliter(ng eq/mL)
Standard Deviation 0.523
Mean Concentration of Total Radioactivity in Whole Blood and Plasma [14C]-TAK-954
Whole Blood: 2 hour
2.40 nanogram equivalent/milliliter(ng eq/mL)
Standard Deviation 0.418
Mean Concentration of Total Radioactivity in Whole Blood and Plasma [14C]-TAK-954
Whole Blood: 3 hour
2.05 nanogram equivalent/milliliter(ng eq/mL)
Standard Deviation 0.349
Mean Concentration of Total Radioactivity in Whole Blood and Plasma [14C]-TAK-954
Whole Blood: 312 hour
NA nanogram equivalent/milliliter(ng eq/mL)
Standard Deviation NA
Data were not reported because none of the values were above LLOQ.
Mean Concentration of Total Radioactivity in Whole Blood and Plasma [14C]-TAK-954
Whole Blood: 336 hour
NA nanogram equivalent/milliliter(ng eq/mL)
Standard Deviation NA
Data were not reported because none of the values were above LLOQ.
Mean Concentration of Total Radioactivity in Whole Blood and Plasma [14C]-TAK-954
Whole Blood: 0.00 minute
NA nanogram equivalent/milliliter(ng eq/mL)
Standard Deviation NA
Data were not reported because none of the values were above lower limit of quantification (LLOQ).
Mean Concentration of Total Radioactivity in Whole Blood and Plasma [14C]-TAK-954
Whole Blood: 0.50 minute
5.15 nanogram equivalent/milliliter(ng eq/mL)
Standard Deviation 0.908
Mean Concentration of Total Radioactivity in Whole Blood and Plasma [14C]-TAK-954
Whole Blood: 1 hour
5.87 nanogram equivalent/milliliter(ng eq/mL)
Standard Deviation 1.26
Mean Concentration of Total Radioactivity in Whole Blood and Plasma [14C]-TAK-954
Whole Blood: 4 hour
2.09 nanogram equivalent/milliliter(ng eq/mL)
Standard Deviation 0.407
Mean Concentration of Total Radioactivity in Whole Blood and Plasma [14C]-TAK-954
Whole Blood: 6 hour
1.79 nanogram equivalent/milliliter(ng eq/mL)
Standard Deviation 0.385
Mean Concentration of Total Radioactivity in Whole Blood and Plasma [14C]-TAK-954
Whole Blood: 12 hour
1.40 nanogram equivalent/milliliter(ng eq/mL)
Standard Deviation 0.217
Mean Concentration of Total Radioactivity in Whole Blood and Plasma [14C]-TAK-954
Whole Blood: 24 hour
0.923 nanogram equivalent/milliliter(ng eq/mL)
Standard Deviation 0.114
Mean Concentration of Total Radioactivity in Whole Blood and Plasma [14C]-TAK-954
Whole Blood: 36 hour
0.583 nanogram equivalent/milliliter(ng eq/mL)
Standard Deviation 0.0874
Mean Concentration of Total Radioactivity in Whole Blood and Plasma [14C]-TAK-954
Whole Blood: 72 hour
0.232 nanogram equivalent/milliliter(ng eq/mL)
Standard Deviation 0.0530
Mean Concentration of Total Radioactivity in Whole Blood and Plasma [14C]-TAK-954
Whole Blood: 96 hour
0.140 nanogram equivalent/milliliter(ng eq/mL)
Standard Deviation 0.0420
Mean Concentration of Total Radioactivity in Whole Blood and Plasma [14C]-TAK-954
Whole Blood: 120 hour
0.0953 nanogram equivalent/milliliter(ng eq/mL)
Standard Deviation 0.0292
Mean Concentration of Total Radioactivity in Whole Blood and Plasma [14C]-TAK-954
Whole Blood: 144 hour
0.0695 nanogram equivalent/milliliter(ng eq/mL)
Standard Deviation 0.0211
Mean Concentration of Total Radioactivity in Whole Blood and Plasma [14C]-TAK-954
Whole Blood: 168 hour
0.0449 nanogram equivalent/milliliter(ng eq/mL)
Standard Deviation 0.0363
Mean Concentration of Total Radioactivity in Whole Blood and Plasma [14C]-TAK-954
Whole Blood: 192 hour
0.0352 nanogram equivalent/milliliter(ng eq/mL)
Standard Deviation 0.0332
Mean Concentration of Total Radioactivity in Whole Blood and Plasma [14C]-TAK-954
Whole Blood: 216 hour
0.0268 nanogram equivalent/milliliter(ng eq/mL)
Standard Deviation 0.0301
Mean Concentration of Total Radioactivity in Whole Blood and Plasma [14C]-TAK-954
Whole Blood: 240 hour
0.0246 nanogram equivalent/milliliter(ng eq/mL)
Standard Deviation 0.0273
Mean Concentration of Total Radioactivity in Whole Blood and Plasma [14C]-TAK-954
Whole Blood: 264 hour
0.00940 nanogram equivalent/milliliter(ng eq/mL)
Standard Deviation 0.0230
Mean Concentration of Total Radioactivity in Whole Blood and Plasma [14C]-TAK-954
Whole Blood: 288 hour
NA nanogram equivalent/milliliter(ng eq/mL)
Standard Deviation NA
Data were not reported because none of the values were above LLOQ.
Mean Concentration of Total Radioactivity in Whole Blood and Plasma [14C]-TAK-954
Plasma: 0.00 minute
NA nanogram equivalent/milliliter(ng eq/mL)
Standard Deviation NA
Data were not reported because none of the values were above LLOQ.
Mean Concentration of Total Radioactivity in Whole Blood and Plasma [14C]-TAK-954
Plasma: 0.50 minute
5.74 nanogram equivalent/milliliter(ng eq/mL)
Standard Deviation 1.72
Mean Concentration of Total Radioactivity in Whole Blood and Plasma [14C]-TAK-954
Plasma: 1 hour
6.29 nanogram equivalent/milliliter(ng eq/mL)
Standard Deviation 1.22
Mean Concentration of Total Radioactivity in Whole Blood and Plasma [14C]-TAK-954
Plasma: 1.5 hour
3.06 nanogram equivalent/milliliter(ng eq/mL)
Standard Deviation 0.528
Mean Concentration of Total Radioactivity in Whole Blood and Plasma [14C]-TAK-954
Plasma: 2 hour
2.59 nanogram equivalent/milliliter(ng eq/mL)
Standard Deviation 0.566
Mean Concentration of Total Radioactivity in Whole Blood and Plasma [14C]-TAK-954
Plasma: 3 hour
2.27 nanogram equivalent/milliliter(ng eq/mL)
Standard Deviation 0.495
Mean Concentration of Total Radioactivity in Whole Blood and Plasma [14C]-TAK-954
Plasma: 4 hour
2.17 nanogram equivalent/milliliter(ng eq/mL)
Standard Deviation 0.437
Mean Concentration of Total Radioactivity in Whole Blood and Plasma [14C]-TAK-954
Plasma: 6 hour
1.77 nanogram equivalent/milliliter(ng eq/mL)
Standard Deviation 0.433
Mean Concentration of Total Radioactivity in Whole Blood and Plasma [14C]-TAK-954
Plasma: 12 hour
1.34 nanogram equivalent/milliliter(ng eq/mL)
Standard Deviation 0.209
Mean Concentration of Total Radioactivity in Whole Blood and Plasma [14C]-TAK-954
Plasma: 24 hour
0.983 nanogram equivalent/milliliter(ng eq/mL)
Standard Deviation 0.104
Mean Concentration of Total Radioactivity in Whole Blood and Plasma [14C]-TAK-954
Plasma: 36 hour
0.601 nanogram equivalent/milliliter(ng eq/mL)
Standard Deviation 0.0567
Mean Concentration of Total Radioactivity in Whole Blood and Plasma [14C]-TAK-954
Plasma: 48 hour
0.443 nanogram equivalent/milliliter(ng eq/mL)
Standard Deviation 0.0478
Mean Concentration of Total Radioactivity in Whole Blood and Plasma [14C]-TAK-954
Plasma: 72 hour
0.271 nanogram equivalent/milliliter(ng eq/mL)
Standard Deviation 0.0502
Mean Concentration of Total Radioactivity in Whole Blood and Plasma [14C]-TAK-954
Plasma: 96 hour
0.169 nanogram equivalent/milliliter(ng eq/mL)
Standard Deviation 0.0368
Mean Concentration of Total Radioactivity in Whole Blood and Plasma [14C]-TAK-954
Plasma: 120 hour
0.123 nanogram equivalent/milliliter(ng eq/mL)
Standard Deviation 0.0378
Mean Concentration of Total Radioactivity in Whole Blood and Plasma [14C]-TAK-954
Plasma: 144 hour
0.0907 nanogram equivalent/milliliter(ng eq/mL)
Standard Deviation 0.0276
Mean Concentration of Total Radioactivity in Whole Blood and Plasma [14C]-TAK-954
Plasma: 168 hour
0.0689 nanogram equivalent/milliliter(ng eq/mL)
Standard Deviation 0.0264
Mean Concentration of Total Radioactivity in Whole Blood and Plasma [14C]-TAK-954
Plasma: 192 hour
0.0552 nanogram equivalent/milliliter(ng eq/mL)
Standard Deviation 0.0163
Mean Concentration of Total Radioactivity in Whole Blood and Plasma [14C]-TAK-954
Plasma: 216 hour
0.0480 nanogram equivalent/milliliter(ng eq/mL)
Standard Deviation 0.0131
Mean Concentration of Total Radioactivity in Whole Blood and Plasma [14C]-TAK-954
Plasma: 240 hour
0.0486 nanogram equivalent/milliliter(ng eq/mL)
Standard Deviation 0.0175
Mean Concentration of Total Radioactivity in Whole Blood and Plasma [14C]-TAK-954
Plasma: 264 hour
0.0407 nanogram equivalent/milliliter(ng eq/mL)
Standard Deviation 0.0114
Mean Concentration of Total Radioactivity in Whole Blood and Plasma [14C]-TAK-954
Plasma: 288 hour
0.0429 nanogram equivalent/milliliter(ng eq/mL)
Standard Deviation 0.0166
Mean Concentration of Total Radioactivity in Whole Blood and Plasma [14C]-TAK-954
Plasma: 312 hour
0.0413 nanogram equivalent/milliliter(ng eq/mL)
Standard Deviation 0.00559
Mean Concentration of Total Radioactivity in Whole Blood and Plasma [14C]-TAK-954
Plasma: 336 hour
0.0349 nanogram equivalent/milliliter(ng eq/mL)
Standard Deviation 0.00700

PRIMARY outcome

Timeframe: Day 1 pre-dose and at multiple time points (up to 336 hours) post-dose

Population: The PK analysis set included all the participants of safety analysis set with sufficient concentration data to facilitate the derivation of at least 1 PK parameter from the concentration time data.

Outcome measures

Outcome measures
Measure
[14C]-TAK-954 0.5 mg
n=6 Participants
\[14C\]-TAK-954 0.5 mg (containing approximately 1.5 µCi) of radioactive tracer administered as a 60-minute infusion, intravenously, once on Day 1.
Cmax: Maximum Observed Plasma and Whole Blood Concentrations of Radioactivity for [14C]-TAK-954
Plasma
6.28 ng eq/mL
Interval 4.99 to 8.93
Cmax: Maximum Observed Plasma and Whole Blood Concentrations of Radioactivity for [14C]-TAK-954
Whole Blood
5.78 ng eq/mL
Interval 4.1 to 7.75

PRIMARY outcome

Timeframe: Day 1 pre-dose and at multiple time points (up to 336 hours) post-dose

Population: The PK analysis set included all the participants of safety analysis set with sufficient concentration data to facilitate the derivation of at least 1 PK parameter from the concentration time data. PK data for TAK-954 metabolite THRX913682 could not be evaluated since its plasma levels were less than (\<) lower limit of quantification.

Outcome measures

Outcome measures
Measure
[14C]-TAK-954 0.5 mg
n=6 Participants
\[14C\]-TAK-954 0.5 mg (containing approximately 1.5 µCi) of radioactive tracer administered as a 60-minute infusion, intravenously, once on Day 1.
Cmax: Maximum Observed Plasma Concentration for TAK-954 and TAK-954 Metabolites
TAK-954
5.91 nanogram per milliliter (ng/mL)
Interval 5.08 to 7.79
Cmax: Maximum Observed Plasma Concentration for TAK-954 and TAK-954 Metabolites
THRX-513466
0.0143 nanogram per milliliter (ng/mL)
Interval 0.00998 to 0.0182

PRIMARY outcome

Timeframe: Day 1 pre-dose and at multiple time points (up to 336 hours) post-dose

Population: The PK analysis set included all the participants of safety analysis set with sufficient concentration data to facilitate the derivation of at least 1 PK parameter from the concentration time data.

Outcome measures

Outcome measures
Measure
[14C]-TAK-954 0.5 mg
n=6 Participants
\[14C\]-TAK-954 0.5 mg (containing approximately 1.5 µCi) of radioactive tracer administered as a 60-minute infusion, intravenously, once on Day 1.
AUClast: Area Under the Plasma and Whole Blood Radioactivity-time Curve From Time 0 to the Time of the Last Quantifiable Radioactivity for [14C]-TAK-954
Plasma
83.6 h*ng eq/mL
Interval 74.4 to 89.5
AUClast: Area Under the Plasma and Whole Blood Radioactivity-time Curve From Time 0 to the Time of the Last Quantifiable Radioactivity for [14C]-TAK-954
Whole Blood
75.4 h*ng eq/mL
Interval 64.9 to 87.1

PRIMARY outcome

Timeframe: Day 1 pre-dose and at multiple time points (up to 336 hours) post-dose

Population: The PK analysis set included all the participants of safety analysis set with sufficient concentration data to facilitate the derivation of at least 1 PK parameter from the concentration time data. PK data for TAK-954 metabolite THRX913682 could not be evaluated since its plasma levels were \< lower limit of quantification.

Outcome measures

Outcome measures
Measure
[14C]-TAK-954 0.5 mg
n=6 Participants
\[14C\]-TAK-954 0.5 mg (containing approximately 1.5 µCi) of radioactive tracer administered as a 60-minute infusion, intravenously, once on Day 1.
AUClast: Area Under the Plasma Concentration-time Curve From Time 0 to the Time of the Last Quantifiable Concentration for TAK-954 and TAK-954 Metabolites
TAK-954
55.4 hour*nanogram per milliliter (h*ng/mL)
Interval 46.2 to 66.5
AUClast: Area Under the Plasma Concentration-time Curve From Time 0 to the Time of the Last Quantifiable Concentration for TAK-954 and TAK-954 Metabolites
THRX-513466
0.0371 hour*nanogram per milliliter (h*ng/mL)
Interval 0.00739 to 0.156

PRIMARY outcome

Timeframe: Day 1 pre-dose and at multiple time points (up to 336 hours) post-dose

Population: The PK analysis set included all the participants of safety analysis set with sufficient concentration data to facilitate the derivation of at least 1 PK parameter from the concentration time data.

Outcome measures

Outcome measures
Measure
[14C]-TAK-954 0.5 mg
n=6 Participants
\[14C\]-TAK-954 0.5 mg (containing approximately 1.5 µCi) of radioactive tracer administered as a 60-minute infusion, intravenously, once on Day 1.
AUC∞: Area Under the Plasma and Whole Blood Radioactivity-time Curve From Time 0 to Infinity for [14C]-TAK-954
Plasma
87.2 h*ng eq/mL
Interval 76.9 to 94.0
AUC∞: Area Under the Plasma and Whole Blood Radioactivity-time Curve From Time 0 to Infinity for [14C]-TAK-954
Whole Blood
79.0 h*ng eq/mL
Interval 67.6 to 92.1

PRIMARY outcome

Timeframe: Day 1 pre-dose and at multiple time points (up to 336 hours) post-dose

Population: The PK analysis set. PK data for metabolites could not be evaluated since metabolites were \< lower limit of quantification and apparent terminal elimination portion of the concentration-time curve could not be characterized.

Outcome measures

Outcome measures
Measure
[14C]-TAK-954 0.5 mg
n=6 Participants
\[14C\]-TAK-954 0.5 mg (containing approximately 1.5 µCi) of radioactive tracer administered as a 60-minute infusion, intravenously, once on Day 1.
AUC∞: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for TAK-954 and TAK-954 Metabolites
55.7 h*ng/mL
Interval 46.4 to 66.8

PRIMARY outcome

Timeframe: Day 1 pre-dose and at multiple time points (up to 336 hours) post-dose

Population: The PK analysis set included all the participants of safety analysis set with sufficient concentration data to facilitate the derivation of at least 1 PK parameter from the concentration time data.

Outcome measures

Outcome measures
Measure
[14C]-TAK-954 0.5 mg
n=6 Participants
\[14C\]-TAK-954 0.5 mg (containing approximately 1.5 µCi) of radioactive tracer administered as a 60-minute infusion, intravenously, once on Day 1.
Tmax: Time to Reach the Maximum Plasma and Whole Blood Radioactivity for [14C]-TAK-954
Plasma
1.00 hour
Interval 0.5 to 1.02
Tmax: Time to Reach the Maximum Plasma and Whole Blood Radioactivity for [14C]-TAK-954
Whole Blood
1.00 hour
Interval 0.55 to 1.02

PRIMARY outcome

Timeframe: Day 1 pre-dose and at multiple time points (up to 336 hours) post-dose

Population: The PK analysis set included all the participants of safety analysis set with sufficient concentration data to facilitate the derivation of at least 1 PK parameter from the concentration time data. PK data for TAK-954 metabolite (THRX913682) could not be evaluated since metabolites were \< lower limit of quantification.

Outcome measures

Outcome measures
Measure
[14C]-TAK-954 0.5 mg
n=6 Participants
\[14C\]-TAK-954 0.5 mg (containing approximately 1.5 µCi) of radioactive tracer administered as a 60-minute infusion, intravenously, once on Day 1.
Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for TAK-954 and TAK-954 Metabolites
TAK-954
1.00 hour
Interval 1.0 to 1.02
Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for TAK-954 and TAK-954 Metabolites
THRX-513466
1.00 hour
Interval 0.55 to 1.02

PRIMARY outcome

Timeframe: Day 1 pre-dose and at multiple time points (up to 336 hours) post-dose

Population: The PK analysis set included all the participants of safety analysis set with sufficient concentration data to facilitate the derivation of at least 1 PK parameter from the concentration time data.

Outcome measures

Outcome measures
Measure
[14C]-TAK-954 0.5 mg
n=6 Participants
\[14C\]-TAK-954 0.5 mg (containing approximately 1.5 µCi) of radioactive tracer administered as a 60-minute infusion, intravenously, once on Day 1.
t1/2z: Terminal Disposition Phase Half-life of Radioactivity in Plasma and Whole Blood for [14C]-TAK-954
Plasma
70.0 hour
Interval 57.9 to 89.9
t1/2z: Terminal Disposition Phase Half-life of Radioactivity in Plasma and Whole Blood for [14C]-TAK-954
Whole Blood
46.4 hour
Interval 30.2 to 73.6

PRIMARY outcome

Timeframe: Day 1 pre-dose and at multiple time points (up to 336 hours) post-dose

Population: The PK analysis set. PK data for metabolites could not be evaluated since metabolites were \< lower limit of quantification and apparent terminal elimination portion of the concentration-time curve could not be characterized.

Outcome measures

Outcome measures
Measure
[14C]-TAK-954 0.5 mg
n=6 Participants
\[14C\]-TAK-954 0.5 mg (containing approximately 1.5 µCi) of radioactive tracer administered as a 60-minute infusion, intravenously, once on Day 1.
t1/2z: Terminal Disposition Phase Half-life in Plasma for TAK-954 and TAK-954 Metabolites
34.3 hour
Interval 23.1 to 47.0

PRIMARY outcome

Timeframe: Day 1 pre-dose and at multiple time points (up to 336 hours) post-dose

Population: No participant was analyzed since this outcome measure was not planned to be assessed but added in the protocol summary by error.

Outcome measures

Outcome data not reported

PRIMARY outcome

Timeframe: Day 1 pre-dose and at multiple time points (up to 336 hours) post-dose

Population: The PK analysis set included all the participants of safety analysis set with sufficient concentration data to facilitate the derivation of at least 1 PK parameter from the concentration time data.

Outcome measures

Outcome measures
Measure
[14C]-TAK-954 0.5 mg
n=6 Participants
\[14C\]-TAK-954 0.5 mg (containing approximately 1.5 µCi) of radioactive tracer administered as a 60-minute infusion, intravenously, once on Day 1.
CL: Total Clearance of TAK-954 After Intravenous Administration of [14C]-TAK-954
8.97 L/h
Interval 7.49 to 10.8

PRIMARY outcome

Timeframe: Day 1 pre-dose and at multiple time points (up to 336 hours) post-dose

Population: No participant was analyzed since this outcome measure was not planned to be assessed but added in the protocol summary by error.

Outcome measures

Outcome data not reported

PRIMARY outcome

Timeframe: Day 1 pre-dose and at multiple time points (up to 336 hours) post-dose

Population: The PK analysis set included all the participants of safety analysis set with sufficient concentration data to facilitate the derivation of at least 1 PK parameter from the concentration time data.

Outcome measures

Outcome measures
Measure
[14C]-TAK-954 0.5 mg
n=6 Participants
\[14C\]-TAK-954 0.5 mg (containing approximately 1.5 µCi) of radioactive tracer administered as a 60-minute infusion, intravenously, once on Day 1.
Vz: Volume of Distribution During the Terminal Disposition Phase After Intravenous Administration for TAK-954
444 liter
Interval 337.0 to 668.0

PRIMARY outcome

Timeframe: Day 1 pre-dose and at multiple time points (up to 336 hours) post-dose

Population: The PK analysis set included all the participants of safety analysis set with sufficient concentration data to facilitate the derivation of at least 1 PK parameter from the concentration time data.

Outcome measures

Outcome measures
Measure
[14C]-TAK-954 0.5 mg
n=6 Participants
\[14C\]-TAK-954 0.5 mg (containing approximately 1.5 µCi) of radioactive tracer administered as a 60-minute infusion, intravenously, once on Day 1.
Aet Urine: Amount of Total Radioactivity Excreted in Urine From Time 0 to Time t for [14C]-TAK-954
278 microgram equivalent (mcg eq)
Standard Deviation 16.2

PRIMARY outcome

Timeframe: Day 1 pre-dose and at multiple time points (up to 336 hours) post-dose

Population: The PK analysis set included all the participants of safety analysis set with sufficient concentration data to facilitate the derivation of at least 1 PK parameter from the concentration time data.

Outcome measures

Outcome measures
Measure
[14C]-TAK-954 0.5 mg
n=6 Participants
\[14C\]-TAK-954 0.5 mg (containing approximately 1.5 µCi) of radioactive tracer administered as a 60-minute infusion, intravenously, once on Day 1.
Aet Urine: Amount of Drug Excreted in Urine From Time 0 to Time t for TAK-954
157 microgram (mcg)
Standard Deviation 16.4

PRIMARY outcome

Timeframe: Day 1 pre-dose and at multiple time points (up to 336 hours) post-dose

Population: The PK analysis set included all the participants of safety analysis set with sufficient concentration data to facilitate the derivation of at least 1 PK parameter from the concentration time data.

Outcome measures

Outcome measures
Measure
[14C]-TAK-954 0.5 mg
n=6 Participants
\[14C\]-TAK-954 0.5 mg (containing approximately 1.5 µCi) of radioactive tracer administered as a 60-minute infusion, intravenously, once on Day 1.
Aet Feces: Amount of Total Radioactivity Excreted in Feces From Time 0 to Time t for [14C]-TAK-954
144 mcg eq
Standard Deviation 12.9

PRIMARY outcome

Timeframe: Day 1 pre-dose and at multiple time points (up to 336 hours) post-dose

Population: The PK analysis set included all the participants of safety analysis set with sufficient concentration data to facilitate the derivation of at least 1 PK parameter from the concentration time data.

Outcome measures

Outcome measures
Measure
[14C]-TAK-954 0.5 mg
n=6 Participants
\[14C\]-TAK-954 0.5 mg (containing approximately 1.5 µCi) of radioactive tracer administered as a 60-minute infusion, intravenously, once on Day 1.
Fet Urine: Fraction of Drug Excreted in Urine From Time 0 to Time t for TAK-954
31.3 percentage of dose
Standard Deviation 3.3

PRIMARY outcome

Timeframe: Day 1 pre-dose and at multiple time points (up to 336 hours) post-dose

Population: The PK analysis set included all the participants of safety analysis set with sufficient concentration data to facilitate the derivation of at least 1 PK parameter from the concentration time data.

Outcome measures

Outcome measures
Measure
[14C]-TAK-954 0.5 mg
n=6 Participants
\[14C\]-TAK-954 0.5 mg (containing approximately 1.5 µCi) of radioactive tracer administered as a 60-minute infusion, intravenously, once on Day 1.
Fet Urine: Fraction of Total Radioactivity Excreted in Urine From Time 0 to Time t for [14C]-TAK-954
55.6 percentage of dose
Standard Deviation 3.2

PRIMARY outcome

Timeframe: Day 1 pre-dose and at multiple time points (up to 336 hours) post-dose

Population: The PK analysis set included all the participants of safety analysis set with sufficient concentration data to facilitate the derivation of at least 1 PK parameter from the concentration time data.

Outcome measures

Outcome measures
Measure
[14C]-TAK-954 0.5 mg
n=6 Participants
\[14C\]-TAK-954 0.5 mg (containing approximately 1.5 µCi) of radioactive tracer administered as a 60-minute infusion, intravenously, once on Day 1.
Fet Feces: Fraction of Radioactivity Excreted in Feces From Time 0 to Time t for [14C]-TAK-954
28.8 percentage of dose
Standard Deviation 2.6

SECONDARY outcome

Timeframe: Day 1 pre-dose and at multiple time points (up to 264 hours) post-dose

Population: The PK analysis set included all the participants of safety analysis set with sufficient concentration data to facilitate the derivation of at least 1 PK parameter from the concentration time data. The PK analysis set where data at specified time points was available.

Outcome measures

Outcome measures
Measure
[14C]-TAK-954 0.5 mg
n=6 Participants
\[14C\]-TAK-954 0.5 mg (containing approximately 1.5 µCi) of radioactive tracer administered as a 60-minute infusion, intravenously, once on Day 1.
Ratio of Total Radioactivity in Whole Blood to Plasma
0.50 minute
0.92 ratio
Standard Deviation 0.13
Ratio of Total Radioactivity in Whole Blood to Plasma
1 hour
0.93 ratio
Standard Deviation 0.06
Ratio of Total Radioactivity in Whole Blood to Plasma
1.5 hour
0.94 ratio
Standard Deviation 0.09
Ratio of Total Radioactivity in Whole Blood to Plasma
2 hour
0.94 ratio
Standard Deviation 0.15
Ratio of Total Radioactivity in Whole Blood to Plasma
3 hour
0.92 ratio
Standard Deviation 0.17
Ratio of Total Radioactivity in Whole Blood to Plasma
4 hour
0.96 ratio
Standard Deviation 0.06
Ratio of Total Radioactivity in Whole Blood to Plasma
6 hour
1.02 ratio
Standard Deviation 0.14
Ratio of Total Radioactivity in Whole Blood to Plasma
12 hour
1.04 ratio
Standard Deviation 0.04
Ratio of Total Radioactivity in Whole Blood to Plasma
24 hour
0.94 ratio
Standard Deviation 0.07
Ratio of Total Radioactivity in Whole Blood to Plasma
36 hour
0.97 ratio
Standard Deviation 0.11
Ratio of Total Radioactivity in Whole Blood to Plasma
72 hour
0.86 ratio
Standard Deviation 0.08
Ratio of Total Radioactivity in Whole Blood to Plasma
96 hour
0.82 ratio
Standard Deviation 0.13
Ratio of Total Radioactivity in Whole Blood to Plasma
120 hour
0.78 ratio
Standard Deviation 0.12
Ratio of Total Radioactivity in Whole Blood to Plasma
144 hour
0.79 ratio
Standard Deviation 0.21
Ratio of Total Radioactivity in Whole Blood to Plasma
168 hour
0.85 ratio
Standard Deviation 0.16
Ratio of Total Radioactivity in Whole Blood to Plasma
192 hour
1.17 ratio
Standard Deviation 0.65
Ratio of Total Radioactivity in Whole Blood to Plasma
216 hour
1.06 ratio
Standard Deviation 0.37
Ratio of Total Radioactivity in Whole Blood to Plasma
240 hour
1.04 ratio
Standard Deviation 0.35
Ratio of Total Radioactivity in Whole Blood to Plasma
264 hour
0.97 ratio
Standard Deviation NA
Standard deviation could not be calculated since only one participant was analyzed.

SECONDARY outcome

Timeframe: Day 1 pre-dose and at multiple time points (up to 336 hours) post-dose

Population: The PK analysis set included all the participants of safety analysis set with sufficient concentration data to facilitate the derivation of at least 1 PK parameter from the concentration time data.

Outcome measures

Outcome measures
Measure
[14C]-TAK-954 0.5 mg
n=6 Participants
\[14C\]-TAK-954 0.5 mg (containing approximately 1.5 µCi) of radioactive tracer administered as a 60-minute infusion, intravenously, once on Day 1.
Ratio of AUC∞: Ratio of Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for TAK-954 to Total Radioactivity in Plasma TAK-954
0.642 ratio
Standard Deviation 0.0741

SECONDARY outcome

Timeframe: Baseline up to Day 31

Population: The safety analysis set included all participants who were enrolled in the study and received at least 1 dose of study drug.

Outcome measures

Outcome measures
Measure
[14C]-TAK-954 0.5 mg
n=6 Participants
\[14C\]-TAK-954 0.5 mg (containing approximately 1.5 µCi) of radioactive tracer administered as a 60-minute infusion, intravenously, once on Day 1.
Percentage of Participants Who Experience at Least One Treatment-emergent Adverse Event (TEAE)
50.0 percentage of participants

SECONDARY outcome

Timeframe: Baseline up to Day 15

Population: The safety analysis set included all participants who were enrolled in the study and received at least 1 dose of study drug.

Outcome measures

Outcome measures
Measure
[14C]-TAK-954 0.5 mg
n=6 Participants
\[14C\]-TAK-954 0.5 mg (containing approximately 1.5 µCi) of radioactive tracer administered as a 60-minute infusion, intravenously, once on Day 1.
Percentage of Participants With Adverse Events (AEs) Leading to Discontinuation of [14C]-TAK-954
0.0 percentage of participants

Adverse Events

[14C]-TAK-954 0.5 mg

Serious events: 0 serious events
Other events: 3 other events
Deaths: 0 deaths

Serious adverse events

Adverse event data not reported

Other adverse events

Other adverse events
Measure
[14C]-TAK-954 0.5 mg
n=6 participants at risk
\[14C\]-TAK-954 0.5 mg (containing approximately 1.5 µCi) of radioactive tracer administered as a 60-minute infusion, intravenously, once on Day 1.
Gastrointestinal disorders
Abdominal pain
16.7%
1/6 • Number of events 1 • A treatment-emergent adverse event (TEAE) are adverse events that started after the first dose of study drug and no more than 30 days (Day 31) after receiving the study drug
At each visit the investigator had to document any occurrence of adverse events and abnormal laboratory findings. Any event spontaneously reported by the participant or observed by the investigator was recorded, irrespective of the relation to study treatment.
Musculoskeletal and connective tissue disorders
Back pain
16.7%
1/6 • Number of events 1 • A treatment-emergent adverse event (TEAE) are adverse events that started after the first dose of study drug and no more than 30 days (Day 31) after receiving the study drug
At each visit the investigator had to document any occurrence of adverse events and abnormal laboratory findings. Any event spontaneously reported by the participant or observed by the investigator was recorded, irrespective of the relation to study treatment.
Musculoskeletal and connective tissue disorders
Myalgia
16.7%
1/6 • Number of events 1 • A treatment-emergent adverse event (TEAE) are adverse events that started after the first dose of study drug and no more than 30 days (Day 31) after receiving the study drug
At each visit the investigator had to document any occurrence of adverse events and abnormal laboratory findings. Any event spontaneously reported by the participant or observed by the investigator was recorded, irrespective of the relation to study treatment.
Nervous system disorders
Headache
33.3%
2/6 • Number of events 2 • A treatment-emergent adverse event (TEAE) are adverse events that started after the first dose of study drug and no more than 30 days (Day 31) after receiving the study drug
At each visit the investigator had to document any occurrence of adverse events and abnormal laboratory findings. Any event spontaneously reported by the participant or observed by the investigator was recorded, irrespective of the relation to study treatment.
Nervous system disorders
Head Discomfort
16.7%
1/6 • Number of events 1 • A treatment-emergent adverse event (TEAE) are adverse events that started after the first dose of study drug and no more than 30 days (Day 31) after receiving the study drug
At each visit the investigator had to document any occurrence of adverse events and abnormal laboratory findings. Any event spontaneously reported by the participant or observed by the investigator was recorded, irrespective of the relation to study treatment.

Additional Information

Medical Director

Takeda

Phone: +1-877-825-3327

Results disclosure agreements

  • Principal investigator is a sponsor employee Research Organization shall not publish any articles or papers nor make any presentations, nor assist any other person in publishing any articles or papers or in making any presentations relating or referring to the Study or any results, data or insights from or any data, information or materials obtained or generated in the performance of its obligations without the prior written consent of Takeda, which consent may be granted or withheld in Takeda's sole discretion.
  • Publication restrictions are in place

Restriction type: OTHER