Table 4.
List of clinical AUC fold increases (with ± two-fold boundary values) for 20 test compounds compared with the in vitro predicted interactions, determined from chemical inhibitor and recombinant cytochrome P450 experiments (see Methods). Values in bold represent predictions falling outside of the two-fold boundaries
| Predicted AUC fold increase | ||||||||
|---|---|---|---|---|---|---|---|---|
| Clinical AUC fold increase | Two-fold boundaries | Chemical inhibitors | PanVera CLint ISEF | PanVera Vmax ISEF | Gentest Vmax ISEF | |||
| 1 | Eletriptan | 4.8 | 2.40 | 9.60 | 2.40 | 4.92 | 6.15 | 3.54 |
| 2 | Tolteradine | 2.1 | 1.00 | 4.20 | 1.30 | 2.16 | 2.25 | 1.34 |
| 3 | Celecoxib | 1.1 | 0.55 | 2.20 | 2.51 | 1.46 | 1.63 | 1.09 |
| 4 | Alprazolam | 3.00 | 1.50 | 6.00 | ND | 3.79 | 4.77 | 3.03 |
| 5 | Triazolam | 12.7 | 6.40 | 25.40 | 1.96 | 4.51 | 3.59 | 6.40 |
| 6 | Conivaptin | 10.9 | 5.45 | 21.80 | 3.85 | 8.09 | 7.29 | 7.26 |
| 7 | Eplerenone | 4.90 | 2.45 | 9.80 | 1.56 | 7.24 | 6.86 | 6.8 |
| 8 | Lasofoxefene | 1.2 | 0.60 | 2.40 | ND | 8.53 | 8.02 | 4.75 |
| 9 | Tirilazed | 4.1 | 2.05 | 8.20 | 30 | 36.13 | 20.03 | 7.65 |
| 10 | Ziprasidone | 1.35 | 0.68 | 2.70 | 5.87 | 6.18 | 4.49 | 6.26 |
| 11 | Dofetilide | 1.55 | 0.78 | 3.10 | ND | 1.28 | 1.16 | 1.15 |
| 12 | PF-A | 3.2 | 1.60 | 6.40 | 7.94 | 7.14 | 6.73 | 3.04 |
| 13 | PF-B | 10.5 | 5.25 | 21.00 | 4.05 | 12.16 | 17.85 | 8.55 |
| 14 | PF-C | 5.16 | 2.58 | 10.32 | 2.69 | 6.48 | 5.54 | 6 |
| 15 | PF-D | 7.6 | 3.80 | 15.20 | 8.48 | 9.57 | 7.69 | 8.44 |
| 16 | PF-E | 8.3 | 4.15 | 16.60 | 3.59 | 9.08 | 7.21 | 5.99 |
| 17 | PF-F | 2 | 1.00 | 4.00 | 1.30 | 1.36 | 1.27 | 1.36 |
| 18 | PF-G | 6 | 3.00 | 12.00 | 9.97 | 8.7 | 7.57 | 7.37 |
| 19 | PF-H | 1.25 | 0.63 | 2.50 | 6.76 | 5.86 | 6.2 | 4.64 |
| 20 | PF-I | 1.34 | 0.67 | 2.68 | ND | 1.25 | 1.14 | 1.57 |