Healthy
Conditions
Brief summary
Phase I study to evaluate the excretion of radioactivity, the metabolic profile, pharmacokinetics, safety and tolerability following a single oral administration of \[14C\] Prucalopride Succinate in healthy male volunteers aged 18 to 50 years (inclusive).The purpose of this study is to investigate how and how quickly Prucalopride Succinate or its break down products are excreted by analysing blood, faeces and urine samples collected during the study.
Interventions
DRUGRadiolabeled Prucalopride Succinate
A single oral dose of 2 mg radiolabeled prucalopride succinate administered on Day 1.
Sponsors
Shire
Study design
Allocation
NA
Intervention model
SINGLE_GROUP
Primary purpose
OTHER
Masking
NONE
Eligibility
Sex/Gender
MALE
Age
18 Years to 50 Years
Healthy volunteers
Yes
Inclusion criteria
* Males aged between 18 and 50 years, inclusive * Body mass index (BMI) of ≥18 and ≤30 kg/m2 * No more than 2 bowel movements per day or fewer than 3 bowel movement per week * Provision of signed and dated, written informed consent prior to any study specific procedures
Exclusion criteria
* Have participated in a \[14C\]-study within the last 6 months. * Exposure to clinically significant radiation within 12 months prior to dose (for example, serial X-ray or computed tomography scans, barium meal, current employment in a job requiring radiation exposure monitoring). * Male subjects who consume more than 21 units of alcohol per week or 3 units per day.
Design outcomes
Primary
| Measure | Time frame | Description |
|---|---|---|
| Area Under the Plasma Concentration Versus Time Curve From Time Zero to Infinity (AUC 0→∞) of Radiolabelled Prucalopride Succinate | Over 240 hours post-dose | 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. |
| Maximum Plasma Concentration (Cmax) of Radiolabelled Prucalopride Succinate | Over 240 hours post-dose | 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. |
| Time to Maximum Plasma Concentration (Tmax) of Radiolabelled Prucalopride Succinate | Over 240 hours post-dose | Tmax is the time after administration of a drug when the maximum plasma concentration in the body is reached. |
| Plasma Half-Life (T1/2) of Radiolabelled Prucalopride Succinate | Over 240 hours post-dose | The time it takes for the blood plasma concentration of a substance to halve. |
| Total Body Clearance (CL/F) of Radiolabelled Prucalopride Succinate | Over 240 hours post-dose | The rate at which a drug is removed from the body. |
| Volume of Distribution (Vz/F) of Radiolabelled Prucalopride Succinate | Over 240 hours post-dose | The distribution of a medication between plasma and the rest of the body. |
| AUC 0→∞ Whole Blood Total Radioactivity of Radiolabelled Prucalopride Succinate | Over 240 hours post-dose | — |
| Cmax Whole Blood Total Radioactivity of Radiolabelled Prucalopride Succinate | Over 240 hours post-dose | — |
| Tmax Whole Blood Total Radioactivity of Radiolabelled Prucalopride Succinate | Over 240 hours post-dose | — |
| Half-Life Whole Blood Total Radioactivity of Radiolabelled Prucalopride Succinate | Over 240 hours post-dose | — |
| AUC 0→∞ Plasma Total Radioactivity of Radiolabelled Prucalopride Succinate | Over 240 hours post-dose | — |
| Cmax Plasma Total Radioactivity of Radiolabelled Prucalopride Succinate | Over 240 hours post-dose | — |
| Tmax Plasma Total Radioactivity of Radiolabelled Prucalopride Succinate | Over 240 hours post-dose | — |
| Half-Life Plasma Total Radioactivity of Radiolabelled Prucalopride Succinate | Over 240 hours post-dose | — |
| Percent Total Radioactivity Excreted in Urine of Radiolabelled Prucalopride Succinate | 240 hours post-dose | — |
| Percent Total Radioactivity Excreted in Stool of Radiolabelled Prucalopride Succinate | Over 240 hours post-dose | — |
Countries
United States
Participant flow
Participants by arm
| Arm | Count |
|---|---|
| [14C] PRUCALOPRIDE SUCCINATE | 6 |
| Total | 6 |
Baseline characteristics
| Characteristic | [14C] PRUCALOPRIDE SUCCINATE |
|---|---|
| Age, Continuous | 35.5 Years STANDARD_DEVIATION 10.45 |
| Age, Customized 18 - 64 | 6 Participants |
| Region of Enrollment UNITED STATES | 6 Participants |
| Sex: Female, Male Female | 0 Participants |
| Sex: Female, Male Male | 6 Participants |
Adverse events
| Event type | EG000 affected / at risk |
|---|---|
| deaths Total, all-cause mortality | — / — |
| other Total, other adverse events | 4 / 6 |
| serious Total, serious adverse events | 0 / 6 |
Outcome results
Primary
Area Under the Plasma Concentration Versus Time Curve From Time Zero to Infinity (AUC 0→∞) of Radiolabelled Prucalopride Succinate
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.
Time frame: 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.
| Arm | Measure | Value (MEAN) | Dispersion |
|---|---|---|---|
| [14C] PRUCALOPRIDE SUCCINATE | 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
AUC 0→∞ Plasma Total Radioactivity of Radiolabelled Prucalopride Succinate
Time frame: Over 240 hours post-dose
Population: Pharmacokinetic Analysis Set
| Arm | Measure | Value (MEAN) | Dispersion |
|---|---|---|---|
| [14C] PRUCALOPRIDE SUCCINATE | AUC 0→∞ Plasma Total Radioactivity of Radiolabelled Prucalopride Succinate | 102 ng equivalents*h/ml | Standard Deviation 11.2 |
Primary
AUC 0→∞ Whole Blood Total Radioactivity of Radiolabelled Prucalopride Succinate
Time frame: Over 240 hours post-dose
Population: Pharmacokinetic Analysis Set
| Arm | Measure | Value (MEAN) | Dispersion |
|---|---|---|---|
| [14C] PRUCALOPRIDE SUCCINATE | AUC 0→∞ Whole Blood Total Radioactivity of Radiolabelled Prucalopride Succinate | 192 ng equivalents*h/ml | Standard Deviation 31.9 |
Primary
Cmax Plasma Total Radioactivity of Radiolabelled Prucalopride Succinate
Time frame: Over 240 hours post-dose
Population: Pharmacokinetic Analysis Set
| Arm | Measure | Value (MEAN) | Dispersion |
|---|---|---|---|
| [14C] PRUCALOPRIDE SUCCINATE | Cmax Plasma Total Radioactivity of Radiolabelled Prucalopride Succinate | 4.14 ng equivalents/ml | Standard Deviation 1.29 |
Primary
Cmax Whole Blood Total Radioactivity of Radiolabelled Prucalopride Succinate
Time frame: Over 240 hours post-dose
Population: Pharmacokinetic Analysis Set
| Arm | Measure | Value (MEAN) | Dispersion |
|---|---|---|---|
| [14C] PRUCALOPRIDE SUCCINATE | Cmax Whole Blood Total Radioactivity of Radiolabelled Prucalopride Succinate | 7.74 ng equivalents/ml | Standard Deviation 2.34 |
Primary
Half-Life Plasma Total Radioactivity of Radiolabelled Prucalopride Succinate
Time frame: Over 240 hours post-dose
Population: Pharmacokinetic Analysis Set
| Arm | Measure | Value (MEAN) | Dispersion |
|---|---|---|---|
| [14C] PRUCALOPRIDE SUCCINATE | Half-Life Plasma Total Radioactivity of Radiolabelled Prucalopride Succinate | 19.7 hours | Standard Deviation 5.64 |
Primary
Half-Life Whole Blood Total Radioactivity of Radiolabelled Prucalopride Succinate
Time frame: Over 240 hours post-dose
Population: Pharmacokinetic Analysis Set
| Arm | Measure | Value (MEAN) | Dispersion |
|---|---|---|---|
| [14C] PRUCALOPRIDE SUCCINATE | Half-Life Whole Blood Total Radioactivity of Radiolabelled Prucalopride Succinate | 18.0 hours | Standard Deviation 5.18 |
Primary
Maximum Plasma Concentration (Cmax) of Radiolabelled Prucalopride Succinate
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.
Time frame: Over 240 hours post-dose
Population: Pharmacokinetic Analysis Set
| Arm | Measure | Value (MEAN) | Dispersion |
|---|---|---|---|
| [14C] PRUCALOPRIDE SUCCINATE | Maximum Plasma Concentration (Cmax) of Radiolabelled Prucalopride Succinate | 3.79 ng/ml | Standard Deviation 1.1 |
Primary
Percent Total Radioactivity Excreted in Stool of Radiolabelled Prucalopride Succinate
Time frame: Over 240 hours post-dose
Population: Pharmacokinetic Analysis Set
| Arm | Measure | Value (MEAN) | Dispersion |
|---|---|---|---|
| [14C] PRUCALOPRIDE SUCCINATE | Percent Total Radioactivity Excreted in Stool of Radiolabelled Prucalopride Succinate | 13.3 percentage of radioactivity | Standard Deviation 1.73 |
Primary
Percent Total Radioactivity Excreted in Urine of Radiolabelled Prucalopride Succinate
Time frame: 240 hours post-dose
Population: Pharmacokinetic Analysis Set
| Arm | Measure | Value (MEAN) | Dispersion |
|---|---|---|---|
| [14C] PRUCALOPRIDE SUCCINATE | Percent Total Radioactivity Excreted in Urine of Radiolabelled Prucalopride Succinate | 84.2 percentage of radioactvity | Standard Deviation 8.88 |
Primary
Plasma Half-Life (T1/2) of Radiolabelled Prucalopride Succinate
The time it takes for the blood plasma concentration of a substance to halve.
Time frame: Over 240 hours post-dose
Population: Pharmacokinetic Analysis Set
| Arm | Measure | Value (MEAN) | Dispersion |
|---|---|---|---|
| [14C] PRUCALOPRIDE SUCCINATE | Plasma Half-Life (T1/2) of Radiolabelled Prucalopride Succinate | 20.6 hours | Standard Deviation 5.35 |
Primary
Time to Maximum Plasma Concentration (Tmax) of Radiolabelled Prucalopride Succinate
Tmax is the time after administration of a drug when the maximum plasma concentration in the body is reached.
Time frame: Over 240 hours post-dose
Population: Pharmacokinetic Analysis Set
| Arm | Measure | Value (MEDIAN) |
|---|---|---|
| [14C] PRUCALOPRIDE SUCCINATE | Time to Maximum Plasma Concentration (Tmax) of Radiolabelled Prucalopride Succinate | 2.75 hours |
Primary
Tmax Plasma Total Radioactivity of Radiolabelled Prucalopride Succinate
Time frame: Over 240 hours post-dose
Population: Pharmacokinetic Analysis Set
| Arm | Measure | Value (MEDIAN) |
|---|---|---|
| [14C] PRUCALOPRIDE SUCCINATE | Tmax Plasma Total Radioactivity of Radiolabelled Prucalopride Succinate | 2.25 hours |
Primary
Tmax Whole Blood Total Radioactivity of Radiolabelled Prucalopride Succinate
Time frame: Over 240 hours post-dose
Population: Pharmacokinetic Analysis Set
| Arm | Measure | Value (MEDIAN) |
|---|---|---|
| [14C] PRUCALOPRIDE SUCCINATE | Tmax Whole Blood Total Radioactivity of Radiolabelled Prucalopride Succinate | 2.75 hours |
Primary
Total Body Clearance (CL/F) of Radiolabelled Prucalopride Succinate
The rate at which a drug is removed from the body.
Time frame: Over 240 hours post-dose
Population: Pharmacokinetic Analysis Set
| Arm | Measure | Value (MEAN) | Dispersion |
|---|---|---|---|
| [14C] PRUCALOPRIDE SUCCINATE | Total Body Clearance (CL/F) of Radiolabelled Prucalopride Succinate | 20.9 L/h | Standard Deviation 2.07 |
Primary
Volume of Distribution (Vz/F) of Radiolabelled Prucalopride Succinate
The distribution of a medication between plasma and the rest of the body.
Time frame: Over 240 hours post-dose
Population: Pharmacokinetic Analysis Set
| Arm | Measure | Value (MEAN) | Dispersion |
|---|---|---|---|
| [14C] PRUCALOPRIDE SUCCINATE | Volume of Distribution (Vz/F) of Radiolabelled Prucalopride Succinate | 623 Liters | Standard Deviation 185 |