TABLE 2.
BEI, in vitro intrinsic Clbiliary, and predicted Clbiliary compared with estimated in vivo hepatic clearance for selected ARBs and HMG-CoA reductase inhibitors in humans
Data represent mean ± S.E.M. of three individual experiments in triplicate.
| Compound | BEI | In Vitro Intrinsic Clbiliary | Plasma Unbound Fraction | Predicted Clbiliary | Estimated In Vivo Hepatic Clearance |
|---|---|---|---|---|---|
| % | ml/min/kga | fu,p | ml/min/kgb | ml/min/kgc | |
| Olmesartan | 34.6 ± 3.0 | 0.943 ± 0.330 | 0.01d | 0.00942 ± 0.00329 | 0.205 |
| Valsartan | 23.0 ± 3.4 | 1.20 ± 0.33 | 0.059e | 0.0702 ± 0.0193 | 0.370 |
| Pravastatin | 30.9 ± 3.1 | 0.484 ± 0.061 | 0.5f | 0.237 ± 0.029 | 7.20 |
| Rosuvastatin | 24.6 ± 4.7 | 3.39 ± 0.89 | 0.12g | 0.390 ± 0.098 | 8.38 |
| Pitavastatin | 15.6 ± 2.7 | 5.48 ± 1.21 | 0.004h | 0.0219 ± 0.0048 | No data |
In vitro intrinsic Clbiliary values were calculated according to eq. 2.
Predicted Clbiliary values were calculated according to eq. 3.
Estimated in vivo hepatic clearance values were calculated based on the difference between total clearance and renal clearance (see Materials and Methods).
Rosuvastatin regulatory documentation.
Pitavastatin regulatory documentation.