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Figure 1 | BMC Pharmacology and Toxicology

Figure 1

From: Safety, tolerability, pharmacokinetics and pharmacodynamics of GSK2239633, a CC-chemokine receptor 4 antagonist, in healthy male subjects: results from an open-label and from a randomised study

Figure 1

Population fits per dose level for pre-dose (Panel A) and 1 hour post-dose (Panel B) in the Single Oral Dose Study. Following single oral dosing of GSK2239633, blood samples were collected from subjects and stimulated with TARC as described. Formation of F-actin was determined following staining with Alexa fluor 647 phalloidin and analysis with a FACSCantoII flow cytometer by measuring the mean Alexa fluor 647 fluorescence intensity of 1,000 cells. The ratio of F-actin formation in CD4+ CCR4+ and CD4+ CCR4- T-cells was calculated, and the fractional receptor occupancy of CCR4 (Ro) was then determined by estimating a dose-ratio (DR) from the change in effective concentration giving 50% of the maximal response (EC50) of the TARC concentration-response curve before and after dosing with GSK2239633 and using the formula Ro = (DR – 1)/DR.

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BMC Pharmacology and Toxicology

ISSN: 2050-6511

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