Table III.
Published AUC Ratios in Drug-Drug Interaction Studies Involving CYP3A4, Used for External Validation
| Victim drug | Inhibitor | Inhibitor dosage (mg/day) | Observed AUC ratio | Reference |
|---|---|---|---|---|
| Alprazolam | Ritonavir | 200 × 2 | 2.50 | (42) |
| Alprazolam | Telaprevir | 750 × 3a | 1.35 | (31) |
| Atorvastatin | Boceprevir | 800 × 3 | 2.30 | (43) |
| Atorvastatin | Ticagrelor | 90 × 2a | 1.36 | (39) |
| Boceprevir | Cyclosporin | 100 | 1.16 | (40) |
| Boceprevir | Ketoconazole | 200a | 2.31 | (44,45) |
| Boceprevir | Ritonavir | 100 | 0.81 | (40) |
| Cyclosporin | Boceprevir | 800 × 3 | 2.68 | (40) |
| Cyclosporin | Telaprevir | 750 × 3a | 4.64 | (31) |
| Clarithromycin | Fluconazole | 200 | 1.18 | (26) |
| Clarithromycin | Ritonavir | 200 × 3 | 1.77 | (26) |
| Colchicine | Azithromycin | 500 | 1.40 | (28) |
| Colchicine | Clarithromycin | 250 × 2 | 3.40 | (28) |
| Colchicine | Diltiazem | 240 | 1.30 | (28) |
| Colchicine | Ketoconazole | 200 × 2 | 2.90 | (28) |
| Dronedarone | Diltiazem | 240 × 2 | 1.70 | (29) |
| Dronedarone | Ketoconazole | 200 | 17.00 | (29) |
| Dronedarone | Verapamil | 240 | 1.40 | (24) |
| Ketoconazole | Ritonavir | 500 × 2 | 3.40 | (42) |
| Methylprednisolone | Itraconazole | 200 | 3.14 | (46) |
| Methylprednisolone | Ketoconazole | 200 | 2.40 | (47) |
| Prednisolone | Ritonavir | 200 × 2 | 1.30 | (42) |
| Quinidine | Erythromycin | 250 × 4 | 1.30 | (48) |
| Quinidine | Verapamil | 240a | 1.50 | (49) |
| Rivaroxaban | Clarithromycin | 500 × 2 | 1.50 | (35) |
| Rivaroxaban | Ketoconazole | 400 | 2.60 | (35) |
| Saquinavir | Erythromycin | 250 × 4 | 1.99 | (27) |
| Saquinavir | Fluconazole | 400a | 1.50 | (27) |
| Saquinavir | Ranitidine | 300a | 1.67 | (27) |
| Sildenafil | Azithromycin | 500 | 1.02 | (36) |
| Sildenafil | Saquinavir | 3,600a | 3.10 | (36) |
| Simvastatine | Posaconazole | 100 | 7.42 | (41) |
| Sirolimus | Diltiazem | 120 | 1.60 | (37) |
| Sirolimus | Erythromycin | 250 × 4a | 4.20 | (37) |
| Tacrolimus | Posaconazole | 400 × 2 | 4.58 | (50) |
| Tadalafil | Ritonavir | 200 × 2 | 2.24 | (38) |
| Ticagrelor | Ketoconazole | 200a | 7.30 | (39) |
| Triazolam | Ritonavir | 200 × 4 | 20.00 | (42) |
| Zolpidem | Ritonavir | 200 × 4 | 1.28 | (42) |
AUC area under the plasma concentration-time curve
aStandard dose due to the uncertainty of the AUC reports