Inhibitor | Caco-2 | LLC-MDR1 | CYP3A4-Expression System |
---|---|---|---|
Ketoconazole | 1.50 | —1-b | 0.0340 |
Verapamil | 16.8 | 224 | 10.3 |
L754.394 | >31-c | >31-d | 0.0182 |
Valspodar | 0.114 | 0.0222 | 7.06 |
↵1-a Data represent IC50 values defined as the concentration of inhibitors (μM) necessary to induce a 50% inhibition of digoxin transport (Fig.3) and midazolam hydroxylation activity (Fig. 1).
↵1-b No inhibitory effect was observed up to 3 μM ketoconazole.
↵1-c 89.2 ± 7.7% of control at 3 μM L754.394.
↵1-d 72.0 ± 9.5% of control at 3 μM L754.394.