This is a single-centre, open-label, non-randomized, single dose study in healthy male subjects designed to assess mass balance recovery, metabolite profile and metabolite identification of radio-labeled BC-3781 administered via the intravenous or oral routes.
This is a single-centre, open-label, non-randomised, single dose study to assess the pharmacokinetics, mass balance recovery, and metabolite profiling and identification following administration of iv or oral 14C-BC-3781 to healthy male subjects It is planned to enrol 2 cohorts of 5 subjects or 10 subjects in total. The active substance being investigated in this study is radiolabeled lefamulin (\[14C\] BC 3781), present in the investigational medicinal products (IMPs) as the acetate salt (\[14C\]-BC-3781.Ac). Subjects assigned to Cohort A will receive a single IV administration of 14C-BC-3781 containing 150 mg BC-3781 and not more than (NMT) 4.3 MBq (117 µCi) 14C, administered as an infusion over 60 min after a light breakfast. Subjects assigned to Cohort B will receive a single oral administration of 14C-BC-3781 containing 600 mg BC-3781 and NMT 4.1 MBq (112 µCi) 14C, in the fasted state
Study Type
INTERVENTIONAL
Allocation
NON_RANDOMIZED
Purpose
BASIC_SCIENCE
Masking
NONE
Enrollment
10
Lefamulin (BC-3781) is a potent, semi-synthetic antibacterial belonging to a novel class for systemic human use known as the pleuromutilins
Quotient Clinical
Nottingham, United Kingdom
Amount of radioactivity eliminated in urine
Amount excreted (Ae) and AE as a percentage of administered dose (%Ae)
Time frame: Day 1 pre-dose to Day 8 post-dose
Amount of radioactivity eliminated in feces
Amount excreted (Ae) and AE as a percentage of administered dose (%Ae)
Time frame: Day 1 pre-dose to Day 8 post-dose
Amount of radioactivity eliminated in urine and feces
Amount excreted (Ae) and AE as a percentage of administered dose (%Ae)
Time frame: Day 1 pre-dose to Day 8 post-dose
Cumulative amount of radioactivity eliminated in urine
Cumulative recovery (CumAe)and CumAe as a percentage of the dose (Cum%Ae)
Time frame: Day 1 pre-dose to Day 8 post-dose
Cumulative amount of radioactivity eliminated in feces
Cumulative recovery (CumAe)and CumAe as a percentage of the dose (Cum%Ae)
Time frame: Day 1 pre-dose to Day 8 post-dose
Cumulative amount of radioactivity eliminated in urine and feces
Cumulative recovery (CumAe)and CumAe as a percentage of the dose (Cum%Ae)
Time frame: Day 1 pre-dose to Day 8 post-dose
Safety - hematology
Safety as assessed by review of changes in hematology
Time frame: Day 1 pre-dose to Day 8 post-dose
Safety - clinical chemistry
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Safety as assessed by review of changes in clinical chemistry
Time frame: Day 1 pre-dose to Day 8 post-dose
Safety - urinalysis
Safety as assessed by review of changes in urinalysis
Time frame: Day 1 pre-dose to Day 8 post-dose
Safety - electrocardiograms
Safety as assessed by review of changes in electrocardiograms
Time frame: Day 1 pre-dose to Day 8 post-dose
Safety - vital signs
Safety as assessed by review of changes in vital signs
Time frame: Day 1 pre-dose to Day 8 post-dose
Safety - adverse events
Safety as assessed by review of adverse events
Time frame: Day 1 pre-dose to Day 8 post-dose
Metabolic profiling and structural identification in plasma
Number of metabolites \>10% of circulating radioactivity in plasma
Time frame: Day 1 pre-dose to Day 8 post-dose
Metabolic profiling and structural identification in urine
Number of metabolites \>10% of the dose in urine
Time frame: Day 1 pre-dose to Day 8 post-dose
Metabolic profiling and structural identification in feces
Number of metabolites \>10% of the dose in feces
Time frame: Day 1 pre-dose to Day 8 post-dose
PK of total radioactivity: lag time (tlag), BC-3781 and major metabolites
Assessment of pharmacokinetics of lefamulin as assessed by radioactivity lag time
Time frame: Day 1 pre-dose to Day 8 post-dose
PK of total radioactivity: Cmax
Peak plasma concentration (Cmax), BC-3781 and major metabolites
Time frame: Day 1 pre-dose to Day 8 post-dose
PK of total radioactivity: AUC
area under the plasma concentration-time curve from time zero to time of last measurable concentration (AUC last) of BC-3781 and major metabolites
Time frame: Day 1 pre-dose to Day 8 post-dose
PK of total radioactivity: AUC (0-infinity)
area under the plasma concentration-time curve from time zero to infinity (AUCinf), BC-3781 and major metabolites
Time frame: Day 1 pre-dose to Day 8 post-dose
PK of total radioactivity: Time to Cmax
Time to reach total maximum observed concentration (tmax), BC-3781 and major metabolites
Time frame: Day 1 pre-dose to Day 8 post-dose
PK of total radioactivity: elimination half-life
elimination half-life (t1/2), BC-3781 and major metabolites
Time frame: Day 1 pre-dose to Day 8 post-dose