Effect of various drugs on expression of P-glycoprotein and CYP3A in LS180 cells (Schuetz et al., 1996)
| Treatment | Fold-increase in Pgp | Rank order (Pgp) | Fold-increase in CYP3A4/5 | Rank order (CYP3A) |
|---|---|---|---|---|
| Reserpine | 29 ± 3.315-a | 1 | 7.6 ± 0.6 | 1 |
| Rifampicin | 16.2 ± 10.8 | 2 | 3.2 ± 1.4 | 3 |
| (range, 6.2–29.9) | ||||
| Phenobarbital | 14.4 ± 3.6 | 3 | 6.1 ± 3.3 | 2 |
| (range, 6.0–22) | ||||
| Verapamil | 10.8 ± 8.3 | 4 | 1.7 ± 0.4 | 7 |
| Midazolam | 5.9 ± 1.7 | 5 | 1.0 | |
| Rapamycin | 4.9 ± 2.1 | 6 | 1.0 | |
| Clotrimazole | 4.1 ± 1.3 | 7 | 4.5 ± 1.1 | 5 |
| FK506 | 3.2 ± 0.7 | 8 | 1.3 ± 0.2 | 9 |
| Isosafrole | 2.7 ± 0.3 | 9 | 2.6 ± 0.1 | 6 |
| Amiodarone | 2.4 ± 0.7 | 10 | 1.0 | |
| Triacetyloleandomycin | 2.3 ± 0.8 | 11 | 1.5 ± 0.2 | 8 |
| Erythromycin | 2.0 ± 0.6 | 12 | 5.3 ± 1.2 | 4 |
| Dexamethasone | 1.5 ± 0.3 | 13 | 1.0 | |
| Nifedipine | 1.3 ± 0.1 | 14 | 1.0 | |
| Phenytoin | 1.3 ± 0.1 | 15 | 1.0 |
↵15-a The values are the mean of up to five separate determinations ± standard deviations; values of 1.0 = no change from untreated control. All cultures were treated for 48–72 hr with 10 μM drug, except for phenobarbital (1 mM).