This study is a Phase I, open-label, single dose, mass balance study in a cohort of 6 healthy adult male subjects. The study will consist of: Screening evaluations, a treatment phase, and follow-up evaluations. In the treatment phase, after an overnight fast of at least 10 hours, each subject will receive a single oral suspension dose of GSK2248761 200mg containing \[14C\] - GSK2248761. Following dosing, serial whole blood, plasma, urine, and fecal samples will be collected. Subjects will be required to remain in the unit until the radiocarbon excreted falls to less than or equal to 1% of the administered dose for two consecutive 24-hour collections in both urine and feces, whichever occurs first. Safety will be assessed by vital signs, 12-lead electrocardiogram (ECG), clinical laboratory tests, AE monitoring, and physical examinations as indicated.
ViiV Healthcare is the new sponsor of this study, and GlaxoSmithKline is in the process of updating systems to reflect the change in sponsorship
Study Type
INTERVENTIONAL
Allocation
NA
Masking
NONE
single oral suspension dose of \[14C\]- GSK2248761 200 mg
GSK Investigational Site
Madison, Wisconsin, United States
Percent recovery of total radiocarbon in urine and feces
Time frame: up to 10 days
Area under the concentration-time curve from time zero to last time of quantifiable concentration within a subject (AUC (0-t)) of total drug-related material (radiocarbon) in blood and plasma
Time frame: up to 10 days
Area under the concentration-time curve from time zero extrapolated to infinite time (AUC (0-infinity)) of total drug-related material (radiocarbon) in blood and plasma
Time frame: up to 10 days
Percentage of AUC(0-infinity) obtained by extrapolation (%AUCex) of total drug-related material (radiocarbon) in blood and plasma.
Time frame: up to 10 days
Minimum observed concentration (Cmax) of total drug-related material (radiocarbon) in blood and plasma
Time frame: up to 10 days
Time occurence of Cmax (tmax) of total drug-related material (radiocarbon) in blood and plasma
Time frame: up to 10 days
Terminal phase rate constant (lambda z) of total drug-related material (radiocarbon) in blood and plasma
Time frame: up to 10 days
Lag time before observation of drug concentrations in sampled matrix (tlag) of total drug-related material (radiocarbon) in blood and plasma
Time frame: up to 10 days
Terminal phase half life (t1/2) of total drug-related material (radiocarbon) in blood and plasma
Time frame: up to 10 days
AUC (0-t) of GSK2248761 in plasma
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Time frame: up to 10 days
AUC (0-infinity) of GSK2248761 in plasma
Time frame: up to 10 days
%AUCex of GSK2248761 in plasma
Time frame: up to 10 days
Cmax of GSK2248761 in plasma
Time frame: up to 10 days
tmax of GSK2248761 in plasma
Time frame: up to 10 days
Lambda z of GSK2248761 in plasma
Time frame: up to 10 days
tlag of GSK2248761 in plasma
Time frame: up to 10 days
Apparent clearance following oral dosing (CL/F) of GSK2248761 in plasma
Time frame: up to 10 days
Apparent volume of distribution after oral administration (Vz/F) of GSK2248761 in plasma
Time frame: up to 10 days
t1/2 of GSK2248761 in plasma
Time frame: up to 10 days
Safety and tolerability parameters including number of adverse events (AEs)
Time frame: up to 25 days
Safety and tolerability parameters including change from baseline for vital signs (blood pressure and heart rate)
Time frame: up to 25 days
Safety and tolerability parameters including change from baseline for electrocardiogram assessments (ECGs)
Time frame: up to 25 days
Safety and tolerability parameters including change from baseline for clinical laboratory assessments
Time frame: up to 25 days
Blood:plasma ratio of total drug-related material (radioactivity)
Time frame: up to 10 days
Percent of total radiocarbon associated with red blood cells
Time frame: up to 10 days