Study of the Absorption, Metabolism, and Excretion of [14C]-Ecopipam in Healthy Male Subjects

A Phase 1, Open-label Study of the Absorption, Metabolism, and Excretion of [14C]-Ecopipam Following a Single Oral Capsule Dose in Healthy Male Subjects

Phase 1, single-center (United Kingdom), open-label, nonrandomized, single-dose study in healthy adult male subjects to assess the absorption, metabolism, and excretion of [14C]-Ecopipam in Healthy Male Subjects.

Study Overview

• Status: Completed
• Conditions: Healthy Volunteer
• Intervention / Treatment: Drug: [14C]-Ecopipam

Detailed Description

This study will be a Phase 1, open-label, nonrandomized, single-dose study in healthy male subjects. Potential subjects will be screened to assess their eligibility to enter the study within 29 days prior to dose administration. Subjects will be admitted into the clinical research unit (CRU) on Day -1 and be confined to the CRU until at least Day 8 (Discharge). On Day 1, subjects will receive a single oral dose of 200 mg ecopipam HCl containing approximately 88.5 µCi of [14C]-ecopipam HCl. Subjects will be discharged when the following discharge criteria are met:

• plasma radioactivity levels below the limit of quantitation for 2 consecutive collections;
• ≥ 90% mass balance recovery; and
• ≤ 1% of the total radioactive dose is recovered in combined excreta (urine and feces) in 2 consecutive 24-hour periods in which collections occur. If discharge criteria are not met on Day 8, subjects will remain in the CRU and additional 24-hour collections (blood, urine, and feces) for total radioactivity will continue until these criteria are met, up to a maximum of Day 15.

• Study Type: Interventional
• Enrollment (Actual): 8
• Phase: Phase 1

Contacts and Locations

Study Locations

• United Kingdom
  • Leeds, United Kingdom, LS2 9LH
    • Covance Clinical Research Unit Ltd.

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 35 years to 55 years (Adult)
• Accepts Healthy Volunteers: Yes
• Genders Eligible for Study: Male

Description

Inclusion Criteria:

• Males of any race between 35 and 55 years of age
• Body mass index between 18.0 and 30.0 kg/m2
• In good health
• Males will agree to use contraception
• Able to comprehend and sign an informed consent form
• History of a minimum of 1 bowel movement per day

Exclusion Criteria:

• History of significant medical illness
• History of clinically significant drug allergy
• History of a seizure disorder, not including infantile seizures
• History of stomach or intestinal surgery that would potentially alter absorption and/or excretion of orally administered drugs
• Clinically significant medical treatment within 8 weeks or infection treatment within 4 weeks of dosing
• Clinically significant ECG abnormality
• History of alcoholism or drug/chemical abuse within the previous 2 years or positive screening test
• Significant alcohol consumption
• Positive hepatitis panel and/or positive human immunodeficiency virus test
• Use of prohibited prescription, over-the-counter medications or natural health products
• Use of tobacco or nicotine-containing products within 3 months prior to Check-in or positive screening test
• Receipt of blood products within 2 months prior to Check in
• Recent donation of blood, plasma, or platelets prior to Screening
• Exposure to significant diagnostic, therapeutic or employment in a job requiring radiation exposure monitoring within 12 months prior to Check-in
• Evidence or history of active suicidal thoughts in the previous 5 years or have any lifetime history of a suicide attempt
• Not suitable for study in the opinion of the Principal Investigator

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Basic Science
• 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: [14C]-Ecopipam; Single oral capsule dose of 200 mg ecopipam HCl containing approximately 88.5 µCi of [14C]-ecopipam HCl	Drug: [14C]-Ecopipam; [14C]-Ecopipam

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Amount of radioactivity excreted in urine (Aeu)	Up to 18 urine samples will be collected at the indicated time points	Up to Day 15
Cumulative radioactivity excreted in urine (Aeu)	Up to 18 urine samples will be collected at the indicated time points	Up to Day 15
Amount of radioactivity excreted in feces (Aef)	Up to 16 feces samples will be collected at the indicated time points	Up to Day 15
Cumulative radioactivity excreted in feces (Aef)	Up to 16 feces samples will be collected at the indicated time points	Up to Day 15
Percentage of dose excreted in urine (feu)	Up to 18 urine samples will be collected at the indicated time points	Up to Day 15
Percentage of dose excreted in feces (fef)	Up to 16 feces samples will be collected at the indicated time points	Up to Day 15
Cumulative dose excreted in urine (feu)	Up to 18 urine samples will be collected at the indicated time points	Up to Day 15
Cumulative dose excreted in feces (fef)	Up to 16 feces samples will be collected at the indicated time points	Up to Day 15
Percentage of total radioactivity in total excreta (feces + urine)	Up to 18 urine and feces samples will be collected at the indicated time points	Up to Day 15
Area under the plasma concentration versus time curve (AUC) from time zero extrapolated to infinity (AUC0-inf)	Up to 28 blood samples will be collected at the indicated time points	Up to Day 15
AUC from time zero to the last quantifiable concentration (AUC0 last)	Up to 28 blood samples will be collected at the indicated time points	Up to Day 15
Maximum observed concentration (Cmax) radioactivity feces + urine)	Up to 28 blood samples will be collected at the indicated time points	Up to Day 15
Time of Cmax (Tmax)	Up to 28 blood samples will be collected at the indicated time points	Up to Day 15
Apparent terminal elimination half-life (t1/2)	Up to 28 blood samples will be collected at the indicated time points	Up to Day 15
Apparent total clearance (CL/F; ecopipam only)	Up to 28 blood samples will be collected at the indicated time points	Up to Day 15
Apparent volume of distribution (Vz/F; ecopipam only)	Up to 28 blood samples will be collected at the indicated time points	Up to Day 15
AUC0-inf of plasma ecopipam concentration relative to AUC0-inf of plasma total radioactivity (AUC0-inf Plasma ecopipam/Total Radioactivity Ratio)	Up to 28 blood samples will be collected at the indicated time points	Up to Day 15
AUC0-inf of whole blood total radioactivity to AUC0-inf of plasma total radioactivity (AUC0 inf Blood/Plasma Ratio)	Up to 28 blood samples will be collected at the indicated time points	Up to Day 15

Secondary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Percentage of ecopipam and metabolites to total radioactivity in plasma	Up to 28 blood samples will be collected at the indicated time points	Up to Day 15
Percentage of ecopipam and metabolites to total radioactivity in urine and faeces	Up to 18 urine and faeces samples will be collected at the indicated time points	Up to Day 15

Collaborators and Investigators

• Sponsor: Emalex Biosciences Inc.
• Collaborators: Covance

Study record dates

Study Major Dates

• Study Start (Actual): May 12, 2021
• Primary Completion (Actual): September 7, 2021
• Study Completion (Actual): September 7, 2021

Study Registration Dates

• First Submitted: April 29, 2021
• First Submitted That Met QC Criteria: May 7, 2021
• First Posted (Actual): May 11, 2021

Study Record Updates

• Last Update Posted (Actual): December 3, 2021
• Last Update Submitted That Met QC Criteria: December 2, 2021
• Last Verified: December 1, 2021

More Information

Terms related to this study

• Additional Relevant MeSH Terms: Physiological Effects of Drugs; Neurotransmitter Agents; Molecular Mechanisms of Pharmacological Action; Central Nervous System Depressants; Antipsychotic Agents; Tranquilizing Agents; Psychotropic Drugs; Dopamine Agents; Dopamine Antagonists; Ecopipam
• Other Study ID Numbers: EBS-101-HV-103

Plan for Individual participant data (IPD)

• Plan to Share Individual Participant Data (IPD)?: NO

Drug and device information, study documents

• Studies a U.S. FDA-regulated drug product: Yes
• Studies a U.S. FDA-regulated device product: No