This study will investigate the safety and pharmacokinetics (PK) of a single dose of GSK2256294 in healthy young and elderly subjects to explore the effects of food, gender and age on drug exposure. The biliary metabolites in healthy young males will be investigated using the Entero-test after a single oral dose of GSK2256294. This study will be conducted in two cohorts (Cohort 1 and Cohort 2). Cohort 1 is open label in order to characterise the PK profile of GSK2256294 in healthy young males and also to investigate the biliary metabolites of GSK2256294. Cohort 2 uses a crossover design to allow comparison of the PK parameters of GSK2256294 between in the fed and fasted state within subject and also to compare the PK parameters of GSK2256294 between male and female subjects. A washout period of a minimum of 2 weeks has been chosen to allow and adequate washout of GSK2256294.
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
TREATMENT
Masking
NONE
Enrollment
28
GSK2256294 is a 5 mg capsule administered orally as a 10 mg dose in the fasted or fed state
GSK Investigational Site
Baltimore, Maryland, United States
Cohort 2: PK profiles of a single oral dose of GSK2256294
PK parameters including area under the concentration-time curve (AUC) and maximum blood concentrations (Cmax), half life (T1/2), time to Cmax (Tmax) following a single oral dose of GSK2256294 administered under fed and fasted conditions in healthy elderly male and female subjects will be estimated
Time frame: Pre-dose, 15 minutes (min), 30 min, 1 hour (h), 1.5 h, 2 h, 3 h, 4 h, 6 h, 8 h, 12 h (Day 1) and 24 h (Day 2), 48 h (Day 3) and 72 h (Day 4)
Cohort 2: Electrocardiogram (ECG) as a measure of safety and tolerability
Twelve-lead ECGs will be obtained as a measure of safety and tolerability
Time frame: Screening, Pre-dose, 30 min, 2 h, 4 h, 6 h and at follow-up
Cohort 2: Adverse events (AEs ) as a measure of safety and tolerability
Time frame: From the start of study treatment and until approximately 2 weeks after the final dose
Cohort 2: Vital signs as a measure of safety and tolerability
Vital sign measurements will include systolic and diastolic blood pressure (BP) and pulse rate
Time frame: Screening, Pre-dose, 30 min, 2 h, 4 h, 6 h and at follow-up
Cohort 2: Laboratory assessments as a measure of safety and tolerability
Clinical laboratory assessments will include haematology, clinical chemistry, urinalysis and other screening tests
Time frame: Screening and follow-up. In addition, clinical chemistry will also be done at 12 h (Day 1) and 24 h (Day 2)
Cohort 1: Biliary metabolite profile of GSK2256294
Bile will be collected for metabolic analysis of GSK2256294 + metabolites via the use of the Entero-Test capsule in healthy male younger subjects
Time frame: Until 7 hours post-dose on Day 1
Cohort 1: AEs as a measure of safety and tolerability
Time frame: From the start of study treatment and until approximately 2 weeks after the final dose
Cohort 1: ECG as a measure of safety and tolerability
Twelve-lead ECGs will be obtained to assess safety and tolerability
Time frame: Screening, Pre-dose, 30 min, 2 h, 4 h, 6 h and at follow-up
Cohort 1: Vital signs as a measure of safety and tolerability
Vital sign measurements will include systolic and diastolic BP and pulse rate
Time frame: Screening, Pre-dose, 30 min, 2 h, 4 h, 6 h and at follow-up
Cohort 1: Laboratory assessments as a measure of safety and tolerability
Clinical laboratory assessments will include haematology, clinical chemistry, urinalysis and other screening tests
Time frame: Screening and follow-up
Cohort 1 and Cohort 2: AUC, Cmax, t1/2,and Tmax of GSK2256294
To compare the pharmacokinetic profiles of single oral doses of GSK2256294 in healthy elderly and healthy younger subjects, and between healthy elderly male and female subjects
Time frame: Cohort 1: Pre-dose, 15 min, 30 min, 1 h, 1.5 h, 2 h, 3 h, 4 h, 6 h, 7 h, 12 h and 24 h, 48 h, and 72 h; Cohort 2: Pre-dose, 15 min, 30 min, 1 h, 1.5 h, 2 h, 3 h, 4 h, 6 h, 8 h, 12 h and 24 h, 48 h and 72 h
This platform is for informational purposes only and does not constitute medical advice. Always consult a qualified healthcare professional.