This study is being conducted to measure the relative bioavailability of the original gelatin capsule formulation and a new formulation, immediate release (IR) tablet of Afuresertib (GSK2110183). The study will be composed of Screening, Treatment, and Follow-up Periods. A subject's total time involved in the study will be approximately 9 weeks. The study will enroll approximately 18 healthy volunteers.
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
TREATMENT
Masking
NONE
Enrollment
18
White opaque hard gelatin capsule with a unit dose strength of 25 milligrams (mg) for oral administration
White round biconvex film coated IR tablet with a unit dose strength of 25 mg for oral administration
GSK Investigational Site
Randwick, New South Wales, Australia
Composite of pharmacokinetic (PK) parameters to determine relative bioavailability of afuresertib after administering it as a single dose in an original gelatin capsule in the fasted state and in a newly formulated IR tablet in the fed and fasted state.
PK parameters include: area under the plasma concentration-time curve from time zero to infinity (AUC \[0-infinity\]), area under the plasma concentration time curve from time zero to last time of quantifiable concentration (AUC \[0-t\]), maximum observed plasma concentration (Cmax), and time to Cmax (tmax).
Time frame: PK Samples will be collected Pre-dose and 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 24, 36, 48, 72, 120, and 168 hours post-dose
Number of subjects with adverse events (AEs).
AEs will be collected from the start of Study Treatment and until the Follow-up contact.
Time frame: Up to 9 weeks
Clinical laboratory parameter assessment as a measure of safety and tolerability
Laboratory parameters include: hematology, clinical chemistry and urinalysis.
Time frame: Up to 9 weeks
Concomitant medications review as a measure of safety and tolerability
Time frame: Up to 9 weeks
Electrocardiogram (ECGs) measurement as a measure of safety and tolerability
Triplicate 12-lead ECGs will be collected at Screening; in each Dosing Period on Day 1 and Day 3 of Dosing Period; and at Follow-up.
Time frame: Up to 9 weeks
Vital sign measurement as a measure of safety and tolerability
Vital sign measurements will include systolic and diastolic blood pressure and pulse rate.
Time frame: Up to 9 weeks
This platform is for informational purposes only and does not constitute medical advice. Always consult a qualified healthcare professional.
Composite of PK parameter following single dose administration of IR tablet in fasted state
PK parameters include: AUC (0 - infinity), AUC (0 - t), Cmax, and tmax.
Time frame: PK Samples will be collected Pre-dose and 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 24, 36, 48, 72, 120, and 168 hours post-dose