Table 2

Inhibition of OATP-mediated fexofenadine uptake by drugs, an organic anion, and bile acids

Inhibitor	Percent Inhibition (Mean ± S.E.) of OATP-Mediated [¹⁴C]Fexofenadine (2 μM) Uptake
Inhibitor	1 μM	10 μM	100 μM
P-gp substrates/ inhibitors
Ritonavir	13 ± 6.9	76 ± 3.5^**	94 ± 2.9^**
Saquinavir	32 ± 3.2^*	75 ± 9.4^***	105 ± 5.6^***
Lovastatin	26 ± 6.8^*	67 ± 5.6^***	95 ± 11^**
Nelfinavir	12 ± 19	62 ± 6.3^*	81 ± 14^*
Quinidine	16 ± 15	57 ± 8.2^**	91 ± 9.6^***
Ketoconazole	−2.8 ± 5.8	55 ± 5.4^**	107 ± 1.2^***
Verapamil	15 ± 0.7	50 ± 6.1^**	100 ± 3.8^***
PSC-833	16 ± 10	46 ± 13^*	85 ± 5.4^***
Indinavir	16 ± 3	37 ± 5.8^**	70 ± 5.2^***
Erythromycin	6 ± 16	14 ± 9.7	66 ± 8.0^**
Cortisol	5 ± 30	10 ± 25	35 ± 23
Organic anion
BSP	24 ± 13	49 ± 5.6^**	78 ± 13^**
Bile acids
Cholate	6 ± 10	2 ± 14	10 ± 7.4
Taurocholate	2 ± 8	−1 ± 15	4 ± 10

Data are shown as mean ± S.E. Statistical difference compared to uptake rate in the absence of inhibitor was assessed by a two-sided Student’s t test and Mann–Whitney U test, withp < .05 as the limit of significance (^* p < .05, ^** p < .01,^*** p < .001).