TABLE 3

IC₅₀ values of edoxaban for OAT1, OAT3, OCT1, OCT2, OATP1B1, OATP1B3, and P-gp using their expressing cells

Inhibitory effects of edoxaban (1–100 μM) on OAT1-mediated [³H]PAH (1 μM) uptake, OAT3-mediated [³H]ES (50 nM) uptake, OCT1-mediated [¹⁴C]TEA (5 μM) uptake, OCT2-mediated [¹⁴C]metformin (10 μM) uptake, OATP1B1-mediated [³H]EG (50 nM) uptake, OATP1B3-mediated [³H]EG (50 nM) uptake, and P-gp–mediated vectorial transport of [³H]digoxin (1 μM) were evaluated using OAT1- and OAT3-expressing S2 cells, OCT1-, OCT2-, OATP1B1-, and OATP1B3-expressing HEK293 cells, and Caco-2 cells expressing P-gp.