TABLE 3

Permeability and ERs of drugs across MDCKII monolayers transduced with BacMam2-BCRP viruses

Permeability across MDCKII-BCRP was determined with 1 µM of donor concentration and 90 minutes of transport time. One micromolar of LY335979 was included in the transport medium. Data are presented as the mean ± S.D. from three individual transwell assays.

DrugTransport Medium without Ko143 and with 1 µM of LY335979Transport Medium with 0.2 µM of Ko143 and 1 µM of LY335979Corrected ER
PA→BMB (A→B)PB→AMB (B→A)ERPA→BMB (A→B)PB→AMB (B→A)ER
nm/s%nm/s%nm/s%nm/s%
Dantrolene54.0 ± 4.992.6484 ± 17995.78.98 ± 3.42453 ± 2495.0228 ± 491.50.503 ± 0.02817.8 ± 6.9
Coumestrol29.3 ± 1.085.9287 ± 3697.69.80 ± 1.29143 ± 2547.749.4 ± 2.588.70.345 ± 0.06328.4 ± 6.4
Daidzein26.9 ± 6.895.9745 ± 15596.427.7 ± 9.0224 ± 1978.9147 ± 2596.60.657 ± 0.12542.1 ± 15.9
Axitinib114 ± 492.6353 ± 991.33.10 ± 0.14324 ± 2687.3224 ± 251030.691 ± 0.0954.49 ± 0.65
Dasatinib8.94 ± 0.51110268 ± 1698.829.9 ± 2.5110 ± 1092.371.2 ± 5.11130.646 ± 0.07746.4 ± 6.7
Erlotinib53.3 ± 8.5117423 ± 891177.93 ± 2.08304 ± 2297.6228 ± 391000.749 ± 0.13910.6 ± 3.4
Flavopiridol20.3 ± 1.8103610 ± 4310730.1 ± 3.4274 ± 694.2176 ± 241300.642 ± 0.09046.9 ± 8.4
Gefitinib19.4 ± 1.290.9471 ± 3687.724.3 ± 2.4177 ± 1871.8106 ± 699.10.596 ± 0.06740.8 ± 6.1
Imatinib22.8 ± 2.373.6301 ± 3074.813.2 ± 1.9201 ± 4272.0113 ± 1079.40.565 ± 0.13023.4 ± 6.3
Prazosin28.6 ± 3.5106395 ± 1394.413.8 ± 1.8310 ± 9104212 ± 6298.30.684 ± 0.20020.2 ± 6.4
Sorafenib17.7 ± 5.643.853.8 ± 4.381.33.05 ± 1.0020.3 ± 3.542.63.66 ± 0.2379.20.180 ± 0.03316.9 ± 6.3
Sunitinib34.8 ± 7.188.0418 ± 1882.112.0 ± 2.5158 ± 1063.884.9 ± 11.776.30.536 ± 0.08222.4 ± 5.8
  • MB, mass balance; MB (A→B), apical-to-basolateral mass balance in percentage; MB (B→A), basolateral-to-apical mass balance in percentage; PA→B, apical-to-basolateral permeability; PB→A, basolateral-to-apical permeability.