TABLE 3

Predicted mean in vivo LTG AUC ratios calculated from Ki values generated in the absence and presence of BSA



In vitro Ki

Predicted AUC Ratio Based on

[I]max
[I]max.unbound
[I]ave
[I]ave.unbound
[I]inlet.max
[I]inlet.max.unbound
[I]inlet.ave
[I]inlet.ave.unbound
μM
Without BSA
   Mean 2465 1.22 1.02 1.17 1.00 1.28 1.03 1.23 1.02
   S.D. 370 0.03 0.01 0.03 0.00 0.04 0.00 0.03 0.00
   Range 1988–2987 1.18–1.26 1.01–1.02 1.14–1.20 1.00–1.00 1.23–1.34 1.02–1.04 1.19–1.28 1.02–1.03
With BSA
   Mean 387 2.08 1.10 1.86 1.01 2.31 1.18 2.12 1.15
   S.D. 12 0.05 0.01 0.04 0.00 0.05 0.01 0.05 0.01
   Range
361–430
1.99–2.13
1.09–1.11
1.79–1.91
1.01–1.01
2.21–2.37
1.16–1.19
2.04–2.18
1.13–1.16