TABLE 1

Peff and ER values of [14C]dasatinib across wild-type and MDR1-transfected MDCKII cell monolayers, in the presence and absence of P-gp inhibitor LY335979



MDCK Wild Type (Control)

MDCK MDR1-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 2.02 ± 0.33 9.64 ± 0.98* 4.8 0.45 ± 0.05 11.58 ± 0.65* 25.6
1 μM LY335979
5.16 ± 0.15
4.83 ± 0.19
0.9
3.79 ± 0.37
4.53 ± 0.10
1.2
  • * p < 0.001 compared with A-to-B transport

  • p < 0.001 compared with treatment control