TABLE 1

Drug doses, pharmacokinetic results, and hERG inhibition


Drug

Cumulative Dose

Free Drug

Free/Ceff Ratio

Free/hERG IC20 Ratio
mg / kg μM
Moxifloxacin (mol. wt. = 401, fu=0.54, Ceff = 5.0 μM) 0.5 0.8 ± 0.1 0.16 0.03
2.5 3.1 ± 0.4 0.62 0.10
9.5 10.0 ± 1.3 2.00 0.32
33.5 41.0 ± 8.1 8.20 1.32
Erythromycin (mol. wt. = 733, fu=0.60, Ceff = 8.5 μM) 1.5 0.8 ± 0.1 0.09 0.04
6.0 3.0 ± 0.2 0.35 0.14
24.0 13.9 ± 1.0 1.64 0.66
96.0 58.3 ± 4.9 6.86 2.78
Telithromycin (mol. wt. = 812, fu=0.23, Ceff = 1.0 μM) 1.5 0.1 ± 0.01 0.1 0.01
6.0 0.4 ± 0.03 0.4 0.04
24.0 2.3 ± 0.4 2.3 0.21

96.0
7.9 ± 0.6
7.9
0.72
  • fu, fraction unbound in plasma