TABLE 1

Experiment 1: A-B and B-A receiver concentrations at 90 min and apparent permeabilities for 10 compounds in MDCK cells and MDR1-MDCK cells

DrugCell TypeCr,ABCr,BAPapp,ABPapp,BAER
μM106 cm/s
AmprenavirMDCK0.0541.52.7258.9
AmprenavirMDR10.00574.20.2970240
AtorvastatinMDCK0.00890.0370.450.621.4
AtorvastatinMDR10.00341.70.1729170
DigoxinMDCK0.00390.270.194.624
DigoxinMDR10.00160.590.0789.9130
LabetalolMDCK0.00510.0360.260.62.3
LabetalolMDR10.00361.60.1826150
LoperamideMDCK0.0260.91.31511
LoperamideMDR10.0053.10.2552210
MinoxidilMDCK0.0150.0470.740.791.1
MinoxidilMDR10.0210.171.12.82.6
PitavastatinMDCK0.0120.0240.620.40.65
PitavastatinMDR10.0142.30.73956
RepaglinideMDCK0.261.213211.6
RepaglinideMDR10.0124.10.669120
SimvastatinMDCK0.0610.443.17.42.4
SimvastatinMDR10.040.622.0105.2
VerapamilMDCK0.361.918331.8
VerapamilMDR10.034.91.58355
  • Cr,AB, concentration in receiver (basolateral side) upon apical dosing; Cr,BA, concentration in receiver (apical side) upon basolateral dosing; Papp,BA, apparent permeability calculated from B-A experiments; Papp,AB, apparent permeability calculated from A-B experiments; ER, efflux ratio.