Table 2.
KI values (in μM) calculated for 21 inhibitors and 5 probe substrates of CYP2C9. Taken with permission from Table 1 of Kumar et al. (2006).
CYP2C9.1 | CYP2C9.3 | |||||||||
---|---|---|---|---|---|---|---|---|---|---|
Flurbiprofen | Warfarin | Phenytoin | Tolbutamide | Diclofenac | Flurbiprofen | Warfarin | Phenytoin | Tolbutamide | Diclofenac | |
Amiodarone | 2.1 | 2.99 | 4.03 | 0.69 | 1.89 | 3.64 | 1.66 | 1.87 | 0.81 | 2.1 |
Benzbromarone | 0.004 | 0.001 | 0.04 | 0.02 | 0.01 | 1.54 | 0.01 | 0.71 | 0.03 | 0.04 |
Clozapine | 4.13 | 3.46 | 12.88 | 11 | 11.43 | 10.49 | 2.8 | 5.07 | 5.92 | 8.04 |
Fluvoxamine | 0.63 | 0.58 | 2.46 | 2.74 | 4.12 | 4.19 | 0.67 | 2.37 | 1.57 | 2.53 |
Gemfibrozil | 12.43 | 0.79 | 2.38 | 2.83 | 3.64 | 14.33 | 1.65 | 4.95 | 7.21 | 14.41 |
(S)-Ibuprofen | 4.27 | 3.06 | 4.02 | 3.95 | 4.46 | 9.78 | 3.15 | 5.5 | 14.03 | 14.68 |
Indomethacin | 53.41 | 0.66 | 15.76 | 14.24 | 14.47 | 38.74 | 5.04 | 12.66 | 16.87 | 25.62 |
Ketoconazole | 0.38 | 0.08 | 1.81 | 1.79 | 1.52 | 1.51 | 0.08 | 0.69 | 0.7 | 0.79 |
Mibefradil | 11.1 | 1.04 | 6.75 | 6.63 | 13.79 | 13.08 | 1.8 | 6.9 | 6.9 | 14.3 |
Miconazole | 0.03 | 0.01 | 0.11 | 0.05 | 0.04 | 0.1 | 0.02 | 0.12 | 0.06 | 0.07 |
α-Naphthoflavone | 0.78 | 0.29 | 0.75 | 0.34 | 0.41 | 1.13 | 0.18 | 0.39 | 0.24 | 0.44 |
Nicardipine | 0.07 | 0.01 | 0.33 | 0.03 | 0.03 | 0.29 | 0.01 | 0.02 | 0.02 | 0.02 |
Nifedipine | 1.14 | 0.34 | 1.35 | 0.84 | 0.57 | 1.53 | 0.28 | 0.61 | 0.28 | 1.18 |
Omeprazole | 5.33 | 0.64 | 2.16 | 0.92 | 0.41 | 16.24 | 0.9 | 1.6 | 1.46 | 0.3 |
Progesterone | 1.72 | 1.41 | 4.3 | 4.01 | 5.2 | 11.03 | 1.97 | 3.27 | 2.58 | 7.91 |
Quercetin | 1.18 | 0.25 | 0.27 | 0.14 | 0.13 | 0.25 | 0.11 | 0.29 | 0.08 | 0.13 |
Quinine | 3.45 | 19.8 | 85.53 | 76.35 | 100 | 21.2 | 18.89 | 39.68 | 86.52 | 96.7 |
Sulfamethizole | 17.9 | 2.22 | 13.08 | 7.17 | 14.69 | 35.04 | 3.87 | 24.74 | 25.93 | 31.86 |
Sulfaphenazole | 0.06 | 0.12 | 0.23 | 0.22 | 0.15 | 0.72 | 0.15 | 0.39 | 0.33 | 0.36 |
Tamoxifen | 3.44 | 0.66 | 3.77 | 3.32 | 4.67 | 9.77 | 0.58 | 6.69 | 2.72 | 8.36 |
Thiobendazole | >100 | 17.22 | 36.21 | 33.09 | 41.08 | 100 | 11.02 | 26.92 | 24.54 | 69.85 |