Figure 9.

Transport of 1 µM ensartinib across MDCKII-parent (A), MDCKII-ABCB1 (B), MDCKII-ABCG2 (C), and MDCKII-ABCC1 (D) cell monolayers. LY335979 (1 µM) was used as a control ABCB1 inhibitor. Cell monolayers were exposed to ensartinib or a combination of ensartinib with a model inhibitor in the donor compartment, and sampling was performed in the acceptor chambers at selected time points. Ensartinib levels were assessed by HPLC-MS/MS. Transport ratios (r) were calculated by dividing the percentage of ensartinib transported in the BA direction by that in the AB direction 4 h after drug addition. The statistical significance of changes in r ratios in the absence/presence of the model inhibitor was analyzed using the two-tailed unpaired t-test (** p < 0.01).