The study is designed to determine the absorption, distribution, metabolism and elimination (ADME) of BIA 28-6156 in humans, further explore the PK of BIA 28-6156, evaluate the extent of distribution of total radioactivity into blood cells, provide additional safety and tolerability information and collect samples for metabolite profiling and structural identification.
This is an open-label, single-dose, single period study in healthy male subjects. It is planned to enroll 6 subjects. All subjects will receive a single oral dose Carbon-14 BIA 28-6156. Blood samples will be collected at regular intervals for PK analysis, mass balance and metabolite profiling and identification from pre-dose up to 240 h post-dose. Urine and faecal samples will be collected at regular intervals for mass balance and metabolite profiling and identification from pre-dose until the mass balance criteria have been met.
Study Type
INTERVENTIONAL
Allocation
NA
Purpose
TREATMENT
Masking
NONE
Enrollment
6
Carbon-14 BIA 28-6156 60 mg, containing NMT 3.7 MBq Carbon-14
Quotient Sciences
Ruddington, Nottingham, United Kingdom
Mass balance recovery of total radioactivity in all excreta (urine and faeces)
CumAe and Cum%Ae
Time frame: Urine: Day 1 through Day 11, Faeces: Day -1 through Day 11
Collection of urine and faecal samples for total radioactivity
Total radioactivity for total recovery of Carbon-14 BIA28-6156
Time frame: Urine and Faeces: Pre-dose until 288 hours post-dose
Collection of plasma samples for metabolite profiling
Collection of major metabolites for metabolite profiling of BIA28-6156
Time frame: Pre-dose until 240 hours post-dose
Collection of plasma samples for structural identification
Identification of chemical structure of major metabolites of BIA28-6156
Time frame: Pre-dose until 240 hours post-dose
Collection of whole blood samples for total radioactivity
Total radioactivity for total recovery of Carbon-14 BIA28-6156
Time frame: Pre-dose until 240 hours post-dose
Determination of routes and rates of elimination of Carbon-14 BIA 28-6156
Time frame: Day 1 through Day 11
Identification of the chemical structure of each metabolite accounting for more than 10% by AUC of circulating plasma total radioactivity and more than 10% of total radioactive dose
Time frame: Urine and Faeces: Day 1 through Day 11, Plasma: Day 1 through Day 7
Measurement of BIA 28-6156 PK parameters
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Time frame: Day 1 through Day 11
Evaluation of whole blood: plasma concentration ratios for total radioactivity
Time frame: Day 1 through Day 7
Adverse events (AEs)
Time frame: Screening through Day 11