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.
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
Allocation
NA
Purpose
BASIC_SCIENCE
Masking
NONE
Enrollment
8
\[14C\]-Ecopipam
Covance Clinical Research Unit Ltd.
Leeds, United Kingdom
Amount of radioactivity excreted in urine (Aeu)
Up to 18 urine samples will be collected at the indicated time points
Time frame: Up to Day 15
Cumulative radioactivity excreted in urine (Aeu)
Up to 18 urine samples will be collected at the indicated time points
Time frame: Up to Day 15
Amount of radioactivity excreted in feces (Aef)
Up to 16 feces samples will be collected at the indicated time points
Time frame: Up to Day 15
Cumulative radioactivity excreted in feces (Aef)
Up to 16 feces samples will be collected at the indicated time points
Time frame: Up to Day 15
Percentage of dose excreted in urine (feu)
Up to 18 urine samples will be collected at the indicated time points
Time frame: Up to Day 15
Percentage of dose excreted in feces (fef)
Up to 16 feces samples will be collected at the indicated time points
Time frame: Up to Day 15
Cumulative dose excreted in urine (feu)
Up to 18 urine samples will be collected at the indicated time points
Time frame: Up to Day 15
Cumulative dose excreted in feces (fef)
Up to 16 feces samples will be collected at the indicated time points
Time frame: Up to Day 15
Percentage of total radioactivity in total excreta (feces + urine)
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Up to 18 urine and feces samples will be collected at the indicated time points
Time frame: 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
Time frame: 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
Time frame: Up to Day 15
Maximum observed concentration (Cmax) radioactivity feces + urine)
Up to 28 blood samples will be collected at the indicated time points
Time frame: Up to Day 15
Time of Cmax (Tmax)
Up to 28 blood samples will be collected at the indicated time points
Time frame: Up to Day 15
Apparent terminal elimination half-life (t1/2)
Up to 28 blood samples will be collected at the indicated time points
Time frame: Up to Day 15
Apparent total clearance (CL/F; ecopipam only)
Up to 28 blood samples will be collected at the indicated time points
Time frame: 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
Time frame: 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
Time frame: 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
Time frame: Up to Day 15
Percentage of ecopipam and metabolites to total radioactivity in plasma
Up to 28 blood samples will be collected at the indicated time points
Time frame: 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
Time frame: Up to Day 15