Transepithelial transport of selpercatinib (5 µM) assessed in MDCK-II cells either nontransduced (A,B), transduced with hABCB1 (C,D), hABCG2 (E,F) or mAbcg2 (G,H) cDNA. At t = 0 h, drug was applied in the donor compartment and the concentrations in the acceptor compartment at t = 1, 2, 4 and 8 h were measured and plotted as cumulative amount of selpercatinib transported per well (pmol) in the graphs (n = 3). (B,D–H): Zosuquidar (Zos, 5 μM) was applied to inhibit human and/or endogenous canine ABCB1. (F,H): the ABCG2 inhibitor Ko143 (5 μM) was applied to inhibit ABCG2/Abcg2-mediated transport. r, relative transport ratio. AB (●), translocation from the apical to the basolateral compartment; BA (■), translocation from the basolateral to the apical compartment. Points, mean; bars, S.D.