TABLE 5

Predictions of FG and QGut using the QGut model from in vitro clearance and permeability data for 25 drugs

Data are predicted values ± S.D.

SubstrateFGQGut Estimated
PredictedaObserved
l/h
Alfentanil0.82 ± 0.060.6016.6
Alprazolam0.99 ± 0.010.9416.4
Atorvastatin0.90 ± 0.040.2412.7
Buspirone0.68 ± 0.040.2116.4
Cisapride0.65 ± 0.060.5516.6
Cyclosporine0.82 ± 0.07b0.448.6b
Felodipine0.20 ± 0.070.4514.5
Indinavir0.25 ± 0.070.935.7c
Lovastatin0.10 ± 0.040.0715.4
Methadone0.97 ± 0.010.7816.2
Midazolam0.54 ± 0.140.5116.6
Nifedipine0.66 ± 0.030.7416.3
Nisoldipine0.08 ± 0.030.1116.3
Quinidine0.99 ± 0.0010.9013.9c
Repaglinide0.84 ± 0.050.8916.3
Rifabutin0.87 ± 0.030.2114.3c
Saquinavir0.01 ± 0.0030.18d2.4c
Sildenafil0.78 ± 0.020.5416.4
Simvastatin0.06 ± 0.020.1413.2
Tacrolimus0.34 ± 0.160.1415.1
Terfenadine0.11 ± 0.020.4011.9
Trazodone0.91 ± 0.030.8316.3
Triazolam0.95 ± 0.040.7516.5
Verapamil0.67 ± 0.07b0.6515.2b
Zolpidem0.98 ± 0.010.7916.6
  • 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).