Summary of in vitro inhibition data for CYP3A for 42 drugs Values represent the mean ± S.E. When IC50 was greater than 300 μM, the percent inhibition value at 300 μM was included (in parentheses).
IC50 | |||||
|---|---|---|---|---|---|
| Testosterone | Midazolam | Felodipine | |||
| μM | |||||
| Alprazolam | >300 (34%) | >300 (45%) | >300 (17%) | ||
| Atenolol | >300 (–3%) | >300 (6%) | >300 (–20%) | ||
| Atorvastatin | 300 (48%) | 16 ± 1 | 36 ± 7 | ||
| Azithromycin | >300 (–4%) | >300 (9%) | >300 (–10%) | ||
| Buspirone | 70 ± 14 | 59 ± 8 | >300 (36%) | ||
| Caffeine | >300 (6%) | >300 (5%) | >300 (3%) | ||
| Cimetidine | 230 ± 30 | >300 (47%) | >300 (46%) | ||
| Citalopram | >300 (48%) | >300 (29%) | >300 (29%) | ||
| Clarithromycin | >300 (46%) | 99 ± 7 | >300 (22%) | ||
| Cyclosporin | 4.5 ± 1.0 | 1.4 ± 0.1 | 300 ± 50 | ||
| Digoxin | >300 (8%) | >300 (–5%) | >300 (–17%) | ||
| Diltiazem | 60 ± 4 | 83 ± 17 | >300 (49%) | ||
| Disulfiram | 6.9 ± 1.0 | 3.6 ± 0.9 | 7.9 ± 1.6 | ||
| Erythromycin | 220 ± 20 | 18 ± 2 | 16 ± 7 | ||
| Fluconazole | 17 ± 1 | 6.8 ± 0.2 | 23±5 | ||
| Fluoxetine | 16 ± 2 | 36 ± 4 | 88 ± 15 | ||
| Fluvoxamine | 28 ± 2 | 43 ± 6 | 62 ± 18 | ||
| Gatifloxacin | >300 (5%) | >300 (6%) | >300 (7%) | ||
| Gemfibrozil | >300 (13%) | >300 (–1%) | >300 (7%) | ||
| Itraconazole | 0.010 ± 0.001 | 0.045 ± 0.007 | 0.021 ± 0.003 | ||
| Ketoconazole | 0.012 ± 0.001 | 0.011 ± 0.001 | 0.019 ± 0.003 | ||
| Metoprolol | >300 (11%) | >300 (5%) | >300 (–5%) | ||
| Metronidazole | >300 (0%) | >300 (25%) | >300(0%) | ||
| Mibefradil | 0.33 ± 0.04 | 0.19 ± 0.03 | 0.68 ± 0.14 | ||
| Nefazodone | 1.4 ± 0.1 | 0.90 ± 0.21 | 8.6 ± 1.1 | ||
| Nelfinavir | 0.65 ± 0.07 | 0.17 ± 0.02 | 0.18 ± 0.03 | ||
| Omeprazole | 110 ± 29 | 68 ± 8 | >300 (24%) | ||
| Paroxetine | 23 ± 4 | 23 ± 2 | 17 ± 4 | ||
| Propoxyphene | 72 ± 7 | 84 ± 17 | 140 ± 20 | ||
| Propranolol | 140 ± 30 | >300 (47%) | >300 (45%) | ||
| Quinidine | 140 ± 40 | 58 ± 17 | >300 (43%) | ||
| Ranitidine | >300 (0%) | >300 (29%) | >300 (0%) | ||
| Repaglinide | 180 ± 30 | >300 (45%) | 120 ± 20 | ||
| Ritonavir | 0.0088 ± 0.0014 | 0.0042 ± 0.0008 | 0.0037 ± 0.0015 | ||
| Roxithromycin | >300 (40%) | 68 ± 11 | >300 (41%) | ||
| Saquinavir | 2.0 ± 0.2 | 0.82 ± 0.15 | 0.51 ± 0.02 | ||
| Sertraline | 8.6 ± 1.0 | 16 ± 4 | 18 ± 6 | ||
| Simvastatin | 2.0 ± 0.4 | 0.77 ± 0.07 | 2.6 ± 0.7 | ||
| Terbinafine | >300 (42%) | >300 (–41%) | >300 (38%) | ||
| Troleandomycin | 9.3 ± 0.4 | 2.6 ± 0.0 | 12 ± 3 | ||
| Venlafaxine | >300 (23%) | >300 (30%) | >300 (3%) | ||
| Verapamil | 23 ± 2 | 23 ± 1 | 50 ± 10 | ||