Trial Outcomes & Findings for Absorption, Metabolism and Excretion (AME) of Single Dose Radiolabeled Prucalopride Succinate in Volunteers (NCT NCT01807000)

NCT ID: NCT01807000

Last Updated: 2021-06-10

Results Overview

AUC can be used as a measure of drug exposure. It is derived from drug concentration and time so it gives a measure how much and how long a drug stays in a body.

Recruitment status

COMPLETED

Study phase

PHASE1

Target enrollment

6 participants

Primary outcome timeframe

Over 240 hours post-dose

Results posted on

2021-06-10

Participant Flow

Participant milestones

Participant milestones
Measure	[14C] PRUCALOPRIDE SUCCINATE A single oral dose of 2 mg radiolabeled prucalopride succinate administered on Day 1.
Overall Study STARTED	6
Overall Study COMPLETED	6
Overall Study NOT COMPLETED	0

Reasons for withdrawal

Withdrawal data not reported

Baseline Characteristics

Absorption, Metabolism and Excretion (AME) of Single Dose Radiolabeled Prucalopride Succinate in Volunteers

Baseline characteristics by cohort

Baseline characteristics by cohort
Measure	[14C] PRUCALOPRIDE SUCCINATE n=6 Participants
Age, Continuous	35.5 Years STANDARD_DEVIATION 10.45 • n=5 Participants
Age, Customized 18 - 64	6 Participants n=5 Participants
Sex: Female, Male Female	0 Participants n=5 Participants
Sex: Female, Male Male	6 Participants n=5 Participants
Region of Enrollment UNITED STATES	6 Participants n=5 Participants

PRIMARY outcome

Timeframe: Over 240 hours post-dose

Population: The Pharmacokinetic Analysis Set included all subjects with at least 1 pharmacokinetic parameter estimated adequately in the Pharmacokinetic Concentration Analysis Set which included all subjects who took 1 dose of investigational product, underwent plasma pharmacokinetic sampling, and had evaluable pharmacokinetic assay results.

AUC can be used as a measure of drug exposure. It is derived from drug concentration and time so it gives a measure how much and how long a drug stays in a body.

Outcome measures

Outcome measures
Measure	[14C] PRUCALOPRIDE SUCCINATE n=6 Participants A single oral dose of 2 mg radiolabeled prucalopride succinate administered on Day 1.
Area Under the Plasma Concentration Versus Time Curve From Time Zero to Infinity (AUC 0→∞) of Radiolabelled Prucalopride Succinate	96.5 ng*h/ml Standard Deviation 9.64

PRIMARY outcome

Timeframe: Over 240 hours post-dose

Population: Pharmacokinetic Analysis Set

Cmax is a term that refers to the maximum (or peak) concentration that a drug achieves in the body after the drug has been administered.

Outcome measures

Outcome measures
Measure	[14C] PRUCALOPRIDE SUCCINATE n=6 Participants A single oral dose of 2 mg radiolabeled prucalopride succinate administered on Day 1.
Maximum Plasma Concentration (Cmax) of Radiolabelled Prucalopride Succinate	3.79 ng/ml Standard Deviation 1.10

PRIMARY outcome

Timeframe: Over 240 hours post-dose

Population: Pharmacokinetic Analysis Set

Tmax is the time after administration of a drug when the maximum plasma concentration in the body is reached.

Outcome measures

Outcome measures
Measure	[14C] PRUCALOPRIDE SUCCINATE n=6 Participants A single oral dose of 2 mg radiolabeled prucalopride succinate administered on Day 1.
Time to Maximum Plasma Concentration (Tmax) of Radiolabelled Prucalopride Succinate	2.75 hours Interval 1.13 to 4.0

PRIMARY outcome

Timeframe: Over 240 hours post-dose

Population: Pharmacokinetic Analysis Set

The time it takes for the blood plasma concentration of a substance to halve.

Outcome measures

Outcome measures
Measure	[14C] PRUCALOPRIDE SUCCINATE n=6 Participants A single oral dose of 2 mg radiolabeled prucalopride succinate administered on Day 1.
Plasma Half-Life (T1/2) of Radiolabelled Prucalopride Succinate	20.6 hours Standard Deviation 5.35

PRIMARY outcome

Timeframe: Over 240 hours post-dose

Population: Pharmacokinetic Analysis Set

The rate at which a drug is removed from the body.

Outcome measures

Outcome measures
Measure	[14C] PRUCALOPRIDE SUCCINATE n=6 Participants A single oral dose of 2 mg radiolabeled prucalopride succinate administered on Day 1.
Total Body Clearance (CL/F) of Radiolabelled Prucalopride Succinate	20.9 L/h Standard Deviation 2.07

PRIMARY outcome

Timeframe: Over 240 hours post-dose

Population: Pharmacokinetic Analysis Set

The distribution of a medication between plasma and the rest of the body.

Outcome measures

Outcome measures
Measure	[14C] PRUCALOPRIDE SUCCINATE n=6 Participants A single oral dose of 2 mg radiolabeled prucalopride succinate administered on Day 1.
Volume of Distribution (Vz/F) of Radiolabelled Prucalopride Succinate	623 Liters Standard Deviation 185

PRIMARY outcome

Timeframe: Over 240 hours post-dose

Population: Pharmacokinetic Analysis Set

Outcome measures

Outcome measures
Measure	[14C] PRUCALOPRIDE SUCCINATE n=6 Participants A single oral dose of 2 mg radiolabeled prucalopride succinate administered on Day 1.
AUC 0→∞ Whole Blood Total Radioactivity of Radiolabelled Prucalopride Succinate	192 ng equivalents*h/ml Standard Deviation 31.9

PRIMARY outcome

Timeframe: Over 240 hours post-dose

Population: Pharmacokinetic Analysis Set

Outcome measures

Outcome measures
Measure	[14C] PRUCALOPRIDE SUCCINATE n=6 Participants A single oral dose of 2 mg radiolabeled prucalopride succinate administered on Day 1.
Cmax Whole Blood Total Radioactivity of Radiolabelled Prucalopride Succinate	7.74 ng equivalents/ml Standard Deviation 2.34

PRIMARY outcome

Timeframe: Over 240 hours post-dose

Population: Pharmacokinetic Analysis Set

Outcome measures

Outcome measures
Measure	[14C] PRUCALOPRIDE SUCCINATE n=6 Participants A single oral dose of 2 mg radiolabeled prucalopride succinate administered on Day 1.
Tmax Whole Blood Total Radioactivity of Radiolabelled Prucalopride Succinate	2.75 hours Interval 1.53 to 4.0

PRIMARY outcome

Timeframe: Over 240 hours post-dose

Population: Pharmacokinetic Analysis Set

Outcome measures

Outcome measures
Measure	[14C] PRUCALOPRIDE SUCCINATE n=6 Participants A single oral dose of 2 mg radiolabeled prucalopride succinate administered on Day 1.
Half-Life Whole Blood Total Radioactivity of Radiolabelled Prucalopride Succinate	18.0 hours Standard Deviation 5.18

PRIMARY outcome

Timeframe: Over 240 hours post-dose

Population: Pharmacokinetic Analysis Set

Outcome measures

Outcome measures
Measure	[14C] PRUCALOPRIDE SUCCINATE n=6 Participants A single oral dose of 2 mg radiolabeled prucalopride succinate administered on Day 1.
AUC 0→∞ Plasma Total Radioactivity of Radiolabelled Prucalopride Succinate	102 ng equivalents*h/ml Standard Deviation 11.2

PRIMARY outcome

Timeframe: Over 240 hours post-dose

Population: Pharmacokinetic Analysis Set

Outcome measures

Outcome measures
Measure	[14C] PRUCALOPRIDE SUCCINATE n=6 Participants A single oral dose of 2 mg radiolabeled prucalopride succinate administered on Day 1.
Cmax Plasma Total Radioactivity of Radiolabelled Prucalopride Succinate	4.14 ng equivalents/ml Standard Deviation 1.29

PRIMARY outcome

Timeframe: Over 240 hours post-dose

Population: Pharmacokinetic Analysis Set

Outcome measures

Outcome measures
Measure	[14C] PRUCALOPRIDE SUCCINATE n=6 Participants A single oral dose of 2 mg radiolabeled prucalopride succinate administered on Day 1.
Tmax Plasma Total Radioactivity of Radiolabelled Prucalopride Succinate	2.25 hours Interval 1.13 to 4.0

PRIMARY outcome

Timeframe: Over 240 hours post-dose

Population: Pharmacokinetic Analysis Set

Outcome measures

Outcome measures
Measure	[14C] PRUCALOPRIDE SUCCINATE n=6 Participants A single oral dose of 2 mg radiolabeled prucalopride succinate administered on Day 1.
Half-Life Plasma Total Radioactivity of Radiolabelled Prucalopride Succinate	19.7 hours Standard Deviation 5.64

PRIMARY outcome

Timeframe: 240 hours post-dose

Population: Pharmacokinetic Analysis Set

Outcome measures

Outcome measures
Measure	[14C] PRUCALOPRIDE SUCCINATE n=6 Participants A single oral dose of 2 mg radiolabeled prucalopride succinate administered on Day 1.
Percent Total Radioactivity Excreted in Urine of Radiolabelled Prucalopride Succinate	84.2 percentage of radioactvity Standard Deviation 8.88

PRIMARY outcome

Timeframe: Over 240 hours post-dose

Population: Pharmacokinetic Analysis Set

Outcome measures

Outcome measures
Measure	[14C] PRUCALOPRIDE SUCCINATE n=6 Participants A single oral dose of 2 mg radiolabeled prucalopride succinate administered on Day 1.
Percent Total Radioactivity Excreted in Stool of Radiolabelled Prucalopride Succinate	13.3 percentage of radioactivity Standard Deviation 1.73

Adverse Events

[14C] PRUCALOPRIDE SUCCINATE

Serious events: 0 serious events

Other events: 4 other events

Deaths: 0 deaths

Serious adverse events

Adverse event data not reported

Other adverse events

Other adverse events
Measure	[14C] PRUCALOPRIDE SUCCINATE n=6 participants at risk A single oral dose of 2 mg radiolabeled prucalopride succinate administered on Day 1.
Gastrointestinal disorders Abdominal discomfort	16.7% 1/6 • Number of events 2
Gastrointestinal disorders Diarrhoea	50.0% 3/6 • Number of events 6
Nervous system disorders Presyncope	16.7% 1/6 • Number of events 1
Skin and subcutaneous tissue disorders Dermatitis allergic	16.7% 1/6 • Number of events 1
Skin and subcutaneous tissue disorders Dry skin	16.7% 1/6 • Number of events 1
Skin and subcutaneous tissue disorders Photosensitivity reaction	16.7% 1/6 • Number of events 1

Additional Information

Study Director

Shire

Phone: +1 866 842 5335

Email: [email protected]

Results disclosure agreements

Principal investigator is a sponsor employee If a multicenter publication is not submitted within twelve (12) months after conclusion, abandonment or termination of the Study at all sites, or after Sponsor confirms there shall be no multicenter Study publication, the Institution and/or such Principal Investigator may publish the results from the Institution site individually.
Publication restrictions are in place

Restriction type: OTHER