FIGURE 5.

Median GSK3206944 intracellular molar concentration over time (linear and semilog) in (A) part A^a and (B) part C^b, day 1 (pharmacokinetic population^c). The median intracellular molar concentration of the metabolite GSK3206944 in monocytes over 4 hours in participants in part A treated with a single dose of GSK3358699 (10, 20, 35, 30 and 40 mg) are shown on a linear (top left) and semilogarithmic scale (top right). Concentrations were not quantifiable for single doses of 1 and 3 mg in part A. There was no evidence for enhanced intracellular GSK3206944 concentrations on repeat dosing at the 10 mg dose investigated in part C (bottom). SD, single dose. ^aPart A was a single ascending‐dose crossover study in two interlocking cohorts. Each participant received a maximum of two single ascending oral doses of GSK3358699 (1, 3, 10, 20, 40 or 30 mg) and one dose of placebo. ^bIn part C, participants received 10 mg of GSK3358699 or placebo daily for up to 14 days. ^cThe pharmacokinetic population included all participants who received an active dose of the study drug and for whom pharmacokinetic samples were obtained and analysed