Relative Bioavailability Study of a Pediatric Granule Formulation of Dolutegravir
Status:
Completed
Trial end date:
2011-08-01
Target enrollment:
Participant gender:
Summary
Dolutegravir (DTG, GSK1349572) is an integrase inhibitor currently in Phase 3 clinical trials
for the treatment of human immunodeficiency virus (HIV) infection. A granule formulation has
been developed as an alternative to the current tablet formulation for administration in
pediatric populations.
This is a single-center, randomized, open-label, 5-way crossover study in healthy adult
subjects. The study will evaluate the relative bioavailability of a 50 mg granule formulation
of dolutegravir when administered 1) directly to mouth; 2) with purified water; 3) with
Contrex brand water; and 4) with milk-based infant formula compared to the current 50 mg
tablet formulation administered with tap water. Safety evaluations and serial PK samples will
be collected during each treatment period. A taste assessment of the granule will also be
performed. A follow-up visit will occur 5-7 days after the last dose of study drug.
Pharmacokinetic assessments during the study will include area under the concentration-time
curve from time zero (pre-dose) extrapolated to infinite time (AUC(0-infinity)), area under
the concentration-time curve from time zero (pre-dose) to last time of quantifiable
concentration within a subject across all treatments (AUC(0-t)), maximum observed
concentration (Cmax), terminal phase half-life (t½), lag time before observation of drug
concentrations in sampled matrix (tlag), time of occurrence of Cmax (tmax), concentration at
24 hours post-dose (C24), and apparent clearance following oral dosing (CL/F).