A Single Dose Study to Assess the Regional Absorption and Bioavailability of 100mg GSK2190915A
Status:
Completed
Trial end date:
2011-03-11
Target enrollment:
Participant gender:
Summary
GSK2190915 is a high affinity 5-lipoxygenase-activating protein (FLAP) inhibitor that
attenuates the production of leukotrienes through the blockage of the first step in the
leukotriene pathway, 5-lipoxygenase (5-LO) activation. GSK2190915 inhibits the production of
leukotriene B4 (LTB4) and cysteinyl leukotrienes (cysLTs).
This is an open label, 4-way, 4-treatment period, non-randomised, crossover study with an
interim analysis. The GSK2190915 formulations used in this study will be: a 100mg and 200mg
milled tablet, a 100mg enteric-coated tablet, and a [14C] radiolabelled GSK2190915
intravenous solution.
This study aims to determine the pharmacokinetics and absolute bioavailability of GSK2190915
to enable optimisation of suitable formulations to be used in clinical development Fourteen
subjects will be dosed to ensure data in 10 at the end of the clinical study. Seven of the
subjects will receive an IV microtracer in addition to the other treatments.