This study is an open-label, randomized, single dose, four period, balanced crossover study to assess in eligible healthy male or female subjects.
This study is an open-label, randomized, single dose, four period, balanced crossover study to assess in eligible healthy male or female subjects: * The relative bioavailability of the wet milled GSK1322322 tablet formulation with and without food compared to an oral mesylate salt solution. * The effect of body weight on the pharmacokinetics of GSK1322322 when given either orally or IV. * The absolute bioavailability of the wet milled tablet and the oral mesylate salt solution compared to the IV formulation.
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
TREATMENT
Masking
NONE
Enrollment
24
1500 mg (mesylate salt) as free base, dissolved in sterile water for injection to a concentration of 100 mg/mL free base equivalent and sterilized via filtration. 15 mL of solution, equivalent to 1500 mg GSK 1322322, is the diluted into 0.9% Sodium Chloride Injection prior to infusion
500 mg tablets for a 1500 mg total single dose (3 tablets). Taken with 240 mL of water
1500 mg as a free base, dissolved in purified water to a concentration of 100 mg/mL free base equivalent. 15 mL of solution, equivalent to1500 mg GSK1322322 is administered orally with 225 mL of water
GSK Investigational Site
Minneapolis, Minnesota, United States
To estimate the relative bioavailability of wet milled tablet formulations of GSK1322322 with and without food as compared to an oral mesylate salt solution following single doses in healthy subjects.
GSK1322322 AUC(0-∞) and Cmax following wet milled tablet formulation administered with and without moderate fat/calorie meal. GSK1322322 AUC(0-∞) and Cmax following oral mesylate salt solution administration.
Time frame: 72 Hours
To estimate the effect of body weight on the pharmacokinetics of GSK1322322 formulations (IV and oral) following single dose administration to healthy subjects.
GSK1322322 AUC(0-∞) and Cmax in each body weight group following IV or oral formulation administration to assess effect of body weight.
Time frame: 72 Hours
To evaluate the safety and tolerability of GSK1322322 after single doses of each formulation in healthy subjects.
Safety parameters including adverse events, clinical laboratory tests, concomitant medications, electrocardiograms, and vital signs.
Time frame: 14 Days
To estimate the absolute bioavailability of the different oral formulations of GSK1322322 as compared to IV mesylate salt formulation following single doses in healthy subjects.
GSK1322322 AUC(0-∞) following different oral formulations (oral mesylate salt solution and wet milled tablet) versus IV formulation to assess absolute bioavailability. GSK1322322 pharmacokinetic parameters will be computed with noncompartmental analysis
Time frame: 72 Hours
This platform is for informational purposes only and does not constitute medical advice. Always consult a qualified healthcare professional.
Drug 500 mg tablets for a 1500 mg total single dose (3 tablets) (FED moderate fat meal) Taken with 240 mL of water