Table 2.
IC50 values for tazarotenic acid sulfoxide formation in recombinant CYP26 enzyme preparations by inhibitors of CYP2C8. Previously reported CYP2C8 IC50 data with the relevant probe substrate is also shown. IC50 values are shown ± standard error (N.R.: not reported).
| Inhibitor | CYP26A1 IC50 (μM) | CYP26B1 IC50 (μM) | CYP2C8 IC50 (μM) | Substrate | Reference |
|---|---|---|---|---|---|
| Benzbromarone | 0.63 ± 0.06 | 7.57 ± 4.93 | 0.38 (N.R.) | Montelukast (HLM) | (44) |
| Candesartan | 25.6 ± 25.8 | 58.3 ± 180 | 36.2 ± 1.7 | Amodiaquine | (51) |
| Candesartan Cilexetil | 0.41 ± 0.32 | 0.27 ± 0.06 | 0.496 ± 0.190 | Amodiaquine | (51) |
| Clotrimazole | 0.02 ± 0.01 | 0.05 ± 0.01 | 0.725 ± 0.116 | Amodiaquine | (51) |
| 17α-Ethynylestradiol | 2.24 ± 1.33 | 6.73 ± 3.77 | 6.54 ± 1.22 | Amodiaquine | (51) |
| Fluconazole | 0.70 ± 0.19 | 19.8 ± 3.21 | 48.9 (N.R.) | Amodiaquine | (50) |
| Itraconazole | 0.55 ± 0.09 | 0.16 ± 0.02 | 2.16 ± 0.41 | Paclitaxel | Unpublished Data |
| Mometasone | 0.90 ± 0.08 | 6.81 ± 1.19 | 0.813 ± 0.112 | Amodiaquine | (51) |
| Montelukast | 0.12 ± 0.02 | 0.61 ± 0.09 | 0.009 ± 0.001 | Amodiaquine | (51) |
| Pioglitazone | 0.93 ± 0.26 | 8.48 ± 1.19 | 11.7 ± 4.0 | Amodiaquine | (51) |
| Quercetin | 1.92 ± 0.39 | 76.2 ± 148 | 3.94 ± 0.64 | Amodiaquine | (51) |
| Raloxifene | 1.78 ± 0.77 | 3.28 ± 1.15 | 2.15 ± 0.90 | Amodiaquine | (51) |
| Repaglinide | 7.73 ± 2.69 | 0.61 ± 0.25 | 11.1 (N.R.) | Montelukast (HLM) | (44) |
| Ritonavir | 3.84 ± 2.82 | 2.56 ± 0.25 | 3.03 ± 1.14 | Amodiaquine | (51) |
| Rosiglitazone | 11.9 ± 1.02 | 8.47 ± 6.64 | 10.8 ± 3.1 | Amodiaquine | (51) |
| Tamoxifen | 21.4 ± 20.3 | 14.0 ± 1.11 | 3.34 ± 1.55 | Amodiaquine | (51) |
| Zafirlukast | 0.06 ± 0.02 | 0.71 ± 0.23 | 0.644 ± 0.273 | Amodiaquine | (51) |