This is a single centre, open-label, single group, non-randomised, single oral dose study in healthy male subjects designed to assess the mass balance recovery, PK, metabolite profile and metabolite identification, and exploratory pharmacodynamics of acoziborole. It is planned to enrol 6 subjects. All subjects will receive an oral dose of 960 mg \[14C\] acoziborole on a single occasion as 4 capsules containing a small amount of radioactivity (not more than \[NMT\] 1000 nCi \[37 KBq\] 14C).
The present study aims to further understand and quantify the absorption, distribution, metabolism and elimination (ADME) of acoziborole in humans through the assessment of the mass balance recovery after a single oral dose of \[14C\]-acoziborole. The routes and rates of elimination of \[14C\]-acoziborole will be determined and plasma, urine and faecal samples will be used for metabolic profiling and structural identification. Subjects will be screened for inclusion in the study up to 28 days before dosing. Subjects will be admitted in the evening on the day before dosing (Day 1). Subjects will be dosed on the morning of Day 1 following an overnight fast of a minimum of 9 h, and will remain resident in the clinic until up to 240 h after dosing (up to Day 11). Subjects will return to the clinical unit for 5 additional 48 h collection periods, admitting to the clinical unit the evening before the collection period. The additional collection periods will be on Days 14 to 17, 28 to 31, 58 to 61, 88 to 91 and 118 to 121. A follow up call will take place 5 to 10 days post-final discharge to ensure the ongoing wellbeing of subjects.
Study Type
INTERVENTIONAL
Allocation
NA
Purpose
TREATMENT
Masking
NONE
Enrollment
6
960 mg (4 × 240 mg capsules)of acoziborole in oral and fasted condition
Quotient Sciences
Nottingham, United Kingdom
total radioactivity in urines and feces
Total radioactivity in urine and faeces at each time interval and cumulative radioactivity excretion (mass balance). For the sample collection periods following 240 h after the dose, excretion will be interpolated between collection periods
Time frame: 121 days
Plasma and urine concentrations of acoziborole and of its main metabolite, SCYX 3109
Plasma and urine concentrations of acoziborole and of its main metabolite, SCYX 3109, to determine relevant PK parameters
Time frame: 121 days
Total radioactivity in whole blood (optional), plasma, urine and faeces
Total radioactivity in whole blood (optional), plasma, urine and faeces at each time point, to determine relevant PK parameters
Time frame: 121 days
Quantitative metabolite profiling and identification of metabolites in pooled samples of plasma, urine and faeces
Quantitative metabolite profiling and identification of metabolites in pooled samples of plasma, urine and faeces, using liquid chromatography (LC)/accelerator mass spectrometry (AMS) in conjunction with LC/tandem mass spectrometry (MS-MS)
Time frame: 121 days
safety and tolerability of 14C acoziborole after single dose as measured by number of subjects with adverse events
Safety and tolerability of 14C acoziborole after single dose as measured by d number of subjects with adverse events
Time frame: 126 days
safety and tolerability of 14C acoziborole after single dose as measured by adverse events severity
Safety and tolerability of 14C acoziborole after single dose as measured by adverse events severity
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Time frame: 126 days
safety and tolerability of 14C acoziborole after single dose as measured by number of subjects with vital signs findings
Safety and tolerability of 14C acoziborole after single dose as measured by number of subjects with vital signs findings
Time frame: 121 days
safety and tolerability of 14C acoziborole after single dose as measured by number of subjects with 12 -lead ECG findings
Safety and tolerability of 14C acoziborole after single dose as measured by number of subjects with 12 -lead ECG findings
Time frame: 121 days
safety and tolerability of 14C acoziborole after single dose as measured by number of subjects with clinical laboratory tests findings (hematology)
Safety and tolerability of 14C acoziborole after single dose as measured by number of subjects with clinical laboratory tests findings (hematology)
Time frame: 121 days
safety and tolerability of 14C acoziborole after single dose as measured by number of subjects with clinical laboratory tests findings (biochemistry)
Safety and tolerability of 14C acoziborole after single dose as measured by number of subjects with clinical laboratory tests findings (biochemistry)
Time frame: 121 days
safety and tolerability of 14C acoziborole after single dose as measured by number of subjects with physical examination findings
Safety and tolerability of 14C acoziborole after single dose as measured by number of subjects with physical examination findings
Time frame: 121 days
Amount of radioactivity in plasma, faeces and urine over time
Amount of radioactivity in plasma, faeces and urine over time exploratory and optional
Time frame: 121 days