Substrate | FG | QGut Estimated | |
---|---|---|---|
Predicteda | Observed | ||
l/h | |||
Alfentanil | 0.82 ± 0.06 | 0.60 | 16.6 |
Alprazolam | 0.99 ± 0.01 | 0.94 | 16.4 |
Atorvastatin | 0.90 ± 0.04 | 0.24 | 12.7 |
Buspirone | 0.68 ± 0.04 | 0.21 | 16.4 |
Cisapride | 0.65 ± 0.06 | 0.55 | 16.6 |
Cyclosporine | 0.82 ± 0.07b | 0.44 | 8.6b |
Felodipine | 0.20 ± 0.07 | 0.45 | 14.5 |
Indinavir | 0.25 ± 0.07 | 0.93 | 5.7c |
Lovastatin | 0.10 ± 0.04 | 0.07 | 15.4 |
Methadone | 0.97 ± 0.01 | 0.78 | 16.2 |
Midazolam | 0.54 ± 0.14 | 0.51 | 16.6 |
Nifedipine | 0.66 ± 0.03 | 0.74 | 16.3 |
Nisoldipine | 0.08 ± 0.03 | 0.11 | 16.3 |
Quinidine | 0.99 ± 0.001 | 0.90 | 13.9c |
Repaglinide | 0.84 ± 0.05 | 0.89 | 16.3 |
Rifabutin | 0.87 ± 0.03 | 0.21 | 14.3c |
Saquinavir | 0.01 ± 0.003 | 0.18d | 2.4c |
Sildenafil | 0.78 ± 0.02 | 0.54 | 16.4 |
Simvastatin | 0.06 ± 0.02 | 0.14 | 13.2 |
Tacrolimus | 0.34 ± 0.16 | 0.14 | 15.1 |
Terfenadine | 0.11 ± 0.02 | 0.40 | 11.9 |
Trazodone | 0.91 ± 0.03 | 0.83 | 16.3 |
Triazolam | 0.95 ± 0.04 | 0.75 | 16.5 |
Verapamil | 0.67 ± 0.07b | 0.65 | 15.2b |
Zolpidem | 0.98 ± 0.01 | 0.79 | 16.6 |
↵a FG predictions based on the QGut model (eq. 2) using Caco-2 Papp (A-B) data.
↵b Estimates based on available human Peff data: cyclosporine 1.65 ± 0.53 μm/s and verapamil 6.8 ± 2.9 μm/s (Lennernäs, 2007).
↵c Indinavir, quinidine, rifabutin, and saquinavir QGut values were 13.8, 16.4, 15.9, and 13.5 l/h, respectively, if no additional contribution of P-gp was assumed (passive permeability only).
↵d FG data were determined from saquinavir (Invirase); no data were available for saquinavir (Fortovase).