This is a single-center, randomized, two part, open-label, crossover study in healthy adult subjects to assess the effect of up to three formulations on the relative bioavailability of GSK2248761 100mg administered with and without food. Part A will evaluate two new formulations compared to the current formulation. Part B will evaluate one additional formulation if the bioavailability of the two formulations in Part A do not meet pre-specified criteria. Safety evaluations and serial PK samples will be collected during each treatment period. A follow-up visit will occur 7-10 days after the last dose of study drug.
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
TREATMENT
Masking
NONE
Enrollment
24
100mg GSK2248761 formulation 1- fasted 100mg GSK2248761 formulation 1 - with food (moderate fat meal)
GSK2248761 100mg Gelucire reference capsule with food
100mg GSK2248761 formulation 3 fasted 100mg GSK2248761 formulation 3 with food (moderate fat meal)
100mg GSK2248761 formulation 2 or 4 - fasted 100mg GSK2248761 formulation 2 or 4 - with food (moderate fat meal)
GSK Investigational Site
Buffalo, New York, United States
Area under the concentration-time curve zero to infinity of plasma GSK2248761
Plasma samples will be collected for the analysis of AUC (0-inf) of GSK2248761.
Time frame: Up to 5 weeks
AUC from time zero to end of dosing interval AUC (0-tau)
Plasma samples will be collected for the analysis AUC (0-tau) of GSK2248761.
Time frame: Up to 5 weeks
Maximum concentration (Cmax) of GSK2248761
Plasma samples will be collected for the analysis of Cmax of GSK2248761.
Time frame: Up to 5 weeks
Terminal half life (t1/2) of GSK2248761
Plasma samples will be collected for the analysis of t1/2 of GSK2248761.
Time frame: Up to 5 weeks
Lag time before observation of drug concentration (tlag) of GSK2248761
Plasma samples will be collected for the analysis of tlag of GSK2248761.
Time frame: Up to 5 weeks
Time to Cmax of GSK2248761
Plasma samples will be collected for the analysis of Tmax of GSK2248761.
Time frame: Up to 5 weeks
Percentage of AUC obtained by extrapolation (%AUCex) for GSK2248761
Plasma samples will be collected for the analysis of %AUCex for GSK2248761.
Time frame: Up to 5 weeks
Apparent clearance following oral dosing (CL/F) for GSK2248761
Plasma samples will be collected for the analysis of CL/F for GSK2248761.
Time frame: Up to 5 weeks
Number of participants with seious adverse events (SAEs) and non-serious adverse events (non-SAEs)
An AE is any untoward medical occurrence in a clinical study participant, temporally associated with the use of a study treatment, whether or not considered related to the study treatment. A SAE is defined as any untoward medical occurrence that, at any dose results in death, is life-threatening, requires inpatient hospitalization or prolongation of existing hospitalization, results in persistent disability/incapacity, is a congenital anomaly/birth defect, associated with liver injury and impaired liver function or any other situations as per medical or scientific judgement.
Time frame: Up to 5 weeks
Number of participants with concurrent medication
Number of participants with concurrent medication will be summarized.
Time frame: Up to 5 weeks
Number of participants with abnormal clinical laboratory parameters
Blood samples will be collected for the analysis of clinical laboratory parameters.
Time frame: Up to 5 weeks
Number of participants with abnormal electrocardiogram (ECG) values
12-lead ECG will be obtained using an ECG machine. Participants will be in supine or a semi-recumbent position (about 30 degrees of elevation) and rested for approximately 2 minutes before ECGs are recorded.
Time frame: Up to 5 weeks
Number of participants with abnormal vital signs
Vital signs will be measured at indicated time points in semi-supine position after 5 minutes rest.
Time frame: Up to 5 weeks
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