TABLE 4

Permeability and ERs of drugs across MDCKII monolayers transduced with BacMam2-Bcrp1 viruses

Permeability across MDCKII-Bcrp1 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%
Dantrolene32.9 ± 5.4103822 ± 8511225.0 ± 4.9387 ± 12102361 ± 5294.90.931 ± 0.13726.9 ± 6.5
Coumestrol24.2 ± 1.995.8407 ± 8911716.8 ± 3.9156 ± 847.545.9 ± 6.61080.295 ± 0.04557.0 ± 15.8
Daidzein20.4 ± 2.5100673 ± 8697.433.0 ± 5.8246 ± 1968.6151 ± 1892.50.614 ± 0.08853.8 ± 12.2
Axitinib100 ± 8103294 ± 431042.94 ± 0.49336 ± 2180.7227 ± 2987.30.678 ± 0.0964.34 ± 0.95
Dasatinib10.0 ± 0.499.3218 ± 3495.021.8 ± 3.5157 ± 1180.198.9 ± 2.691.80.631 ± 0.04934.5 ± 6.1
Erlotinib65.4 ± 3.992.7842 ± 12593.212.9 ± 2.1368 ± 18106332 ± 1393.30.902 ± 0.05614.3 ± 2.4
Flavopiridol23.0 ± 0.595.9388 ± 3496.616.9 ± 1.6319 ± 1096.5252 ± 2397.70.789 ± 0.07621.4 ± 2.9
Gefitinib18.4 ± 2.595.4309 ± 5793.916.8 ± 3.9206 ± 480.292.0 ± 13.81020.448 ± 0.06837.5 ± 10.3
Imatinib31.9 ± 3.797.5644 ± 4296.620.2 ± 2.7277 ± 15101187 ± 1799.20.674 ± 0.07129.9 ± 5.1
Prazosin27.5 ± 3.599.0596 ± 5396.721.6 ± 3.4414 ± 11110508 ± 271001.23 ± 0.0717.6 ± 2.9
Sorafenib14.2 ± 4.146.365.3 ± 8.265.34.60 ± 1.4547.2 ± 3.329.924.9 ± 2.977.30.528 ± 0.0718.70 ± 2.98
Sunitinib30.7 ± 4.087.3418 ± 9787.313.6 ± 3.6156 ± 666.4106 ± 34.777.20.678 ± 0.22420.0 ± 8.5
  • 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.