In vitro parameters estimated from sandwich culture human hepatocyte parameters at a single substrate concentration
Data represent mean from multiple replicates in one to two donors (S.D., where replicates are >2).
| Compounda | CLint, u, active | CLint, u, passive | CLint, u, bile | Predicted fu, cell |
|---|---|---|---|---|
| μl · min−1 · Mcells−1 | ||||
| Pravastatin | 1.8 | 0.1 | 1.2 | 0.60 |
| Cerivastatin | 9.6 (2.7) | 25 (3.5) | 6.2 (1.8) | 0.0096 |
| Bosentan | 9.1 | 4.8 | 7.4 | 0.011 |
| Fluvastatin | 45 (21) | 20 (9.6) | 17 | 0.0082 |
| Rosuvastatin | 9.3 (2.6) | 1.7 (0.73) | 1.5 (0.088) | 0.17 |
| Valsartan | 2.1 (0.48) | 0.60 (0.18) | 96 | 0.0020 |
| Repaglinide | 30 (16) | 89 (75) | 0 | 0.015 |
↵a Lots: pravastatin: BD109 (n = 1), HU4168 (n = 1); cerivastatin: BD109 (n = 2), HU4168 (n = 2); bosentan: HU4168 (n = 1); fluvastatin: BD109 (n = 2), HU4168 (n = 1); rosuvastatin: BD109 (n = 6), HU4166 (n = 2); valsartan: BD109 (n = 2), HU4168 (n = 1); repaglinide: HU4168 (n = 3), RTM (n = 2).