Clearance obtained for 10 drugs in the presence of individual P450 and UGT cofactors
Data are mean ± S.D. References for major UGT enzymes are available at http://www.pharmacy.manchester.ac.uk/capkr/.
Compound | Major P450 | Major UGT | CLint, u | In Vitroa | ||||
|---|---|---|---|---|---|---|---|---|
| P450 | UGT | fmUGT | fmCYP | |||||
| μl/min/mg | ||||||||
| Buprenorphine | CYP3A4 | UGT1A1 | 472 ± 40 | 279 ± 28 | 0.37 | 0.63 | ||
| Carvedilol | CYP2D6 | UGT1A1 | 252 ± 17.6 | 36.0 ± 9.8 | 0.13 | 0.87 | ||
| Codeine | CYP3A4 | UGT2B7 | 2.44 ± 0.06 | 2.53 ± 0.01 | 0.51 | 0.49 | ||
| Diclofenac | CYP2C9 | UGT2B7 | 129 ± 32.2 | 214 ± 46.1 | 0.62 | 0.38 | ||
| Gemfibrozil | CYP3A4 | UGT2B7 | 18.4 ± 9.3 | 70 ± 9.3 | 0.79 | 0.21 | ||
| Ketoprofen | CYP2C9 | UGT2B7 | 9.35 ± 3.6 | 9.35 ± 4.3 | 0.50 | 0.50 | ||
| Midazolam | CYP3A4 | UGT1A4 | 144 ± 41.8 | 8.83 ± 1.9 | 0.06 | 0.94 | ||
| Naloxone | UGT2B7 | 5.52 ± 3.2 | 10.2 ± 2.9 | 0.65 | 0.35 | |||
| Raloxifene | UGT1A9/1A1 | 197 ± 25.8 | 444 ± 86.4 | 0.69 | 0.31 | |||
| Zidovudine |
| UGT2B7 | 3.84 ± 0.7 | 2.21 ± 1.4 | 0.37 | 0.63 | ||
↵ a In vitro fmUGT and fmCYP were calculated using eqs. 5 and 6, respectively.