TABLE 1

Directional flux of dabrafenib in MDCKII-WT– and MDCKII-Bcrp1–transfected cell lines

Data represent the mean ± S.D. (n = 3).

Cell LinePappERCFR
A-to-BB-to-A
cm/s ×10−6cm/s ×10−6
MDCKII-WT11.5 ± 1.414.1 ± 1.41.2
MDCKII-WT + 0.2 μM Ko14316.4 ± 0.915.3 ± 2.60.9
MDCKII-Bcrp11.3 ± 0.3a27.3 ± 4.1a21.017.5
MDCKII-Bcrp1 + 0.2 μM Ko14313.2 ± 2.1b9.6 ± 0.33b0.7
  • A, apical; B, basolateral; Bcrp1, breast cancer resistance protein 1; CFR, corrected efflux ratio; ER, efflux ratio; MDCKII, Madin-Darby canine kidney II; Papp, apparent permeability of dabrafenib; WT, wild type.

  • a Significantly different compared with respective wild-type control cells.

  • b Significantly different compared with untreated Bcrp1 control cells.