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

A Phase 1 Study to Investigate the Absorption, Metabolism, and Excretion of [14C] Prucalopride Succinate Following a Single Oral Dose in Healthy Male Subjects

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.

Study Overview

• Status: Completed
• Conditions: Healthy
• Intervention / Treatment: Drug: Radiolabeled Prucalopride Succinate

• Study Type: Interventional
• Enrollment (Actual): 6
• Phase: Phase 1

Contacts and Locations

Study Locations

• United States
  • Wisconsin
    • Madison, Wisconsin, United States, 53704
      • Covance Global Clinical Research Unit Inc.

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 14 years to 46 years (Adult)
• Accepts Healthy Volunteers: No
• Genders Eligible for Study: Male

Description

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.

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Other
• Allocation: N/A
• Interventional Model: Single Group Assignment
• Masking: None (Open Label)

Number of Arms

1

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: Radiolabeled Prucalopride Succinate	Drug: Radiolabeled Prucalopride Succinate; A single oral dose of 2 mg radiolabeled prucalopride succinate administered on Day 1.

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
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.	Over 240 hours post-dose
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.	Over 240 hours post-dose
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.	Over 240 hours post-dose
Plasma Half-Life (T1/2) of Radiolabelled Prucalopride Succinate	The time it takes for the blood plasma concentration of a substance to halve.	Over 240 hours post-dose
Total Body Clearance (CL/F) of Radiolabelled Prucalopride Succinate	The rate at which a drug is removed from the body.	Over 240 hours post-dose
Volume of Distribution (Vz/F) of Radiolabelled Prucalopride Succinate	The distribution of a medication between plasma and the rest of the body.	Over 240 hours post-dose
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

Collaborators and Investigators

• Sponsor: Shire

Publications and helpful links

General Publications

• Flach S, Scarfe G, Dragone J, Ding J, Seymour M, Pennick M, Pankratz T, Troy S, Getsy J. A Phase I Study to Investigate the Absorption, Pharmacokinetics, and Excretion of [(14)C]Prucalopride After a Single Oral Dose in Healthy Volunteers. Clin Ther. 2016 Sep;38(9):2106-15. doi: 10.1016/j.clinthera.2016.08.003. Epub 2016 Sep 7.

Study record dates

Study Major Dates

• Study Start (Actual): March 18, 2013
• Primary Completion (Actual): April 28, 2013
• Study Completion (Actual): April 28, 2013

Study Registration Dates

• First Submitted: March 6, 2013
• First Submitted That Met QC Criteria: March 6, 2013
• First Posted (Estimate): March 8, 2013

Study Record Updates

• Last Update Posted (Actual): June 10, 2021
• Last Update Submitted That Met QC Criteria: May 26, 2021
• Last Verified: May 1, 2021

More Information

Terms related to this study

• Additional Relevant MeSH Terms: Physiological Effects of Drugs; Neurotransmitter Agents; Molecular Mechanisms of Pharmacological Action; Gastrointestinal Agents; Serotonin Agents; Serotonin Receptor Agonists; Laxatives; Serotonin 5-HT4 Receptor Agonists; Prucalopride
• Other Study ID Numbers: SPD555-104