TABLE 2

Peff and ER values of [14C]dasatinib across wild-type and Bcrp1-transfected MDCKII cell monolayers in the presence and absence of BCRP inhibitor Ko143



MDCK Wild Type (Control)

MDCK Bcrp1-Transfected

A-to-B Peff
B-to-A Peff
ER
A-to-B Peff
B-to-A Peff
ER
mean ± S.D. × 10–6 cm/s
Treatment control 3.09 ± 0.61 12.73 ± 0.60* 4.1 0.31 ± 0.25 16.20 ± 0.66* 51.6
200 nM Ko143
2.60 ± 0.10
10.68 ± 0.63*
4.1
1.66 ± 0.10
15.19 ± 0.56*
9.2
  • * p < 0.001 compared with A-to-B transport

  • p < 0.001 compared with treatment control