TABLE 1.
Drug | fum | Cell | C0 | Cr,AB | Cr,BA | ER |
---|---|---|---|---|---|---|
μM | ||||||
Atorvastatin1 | 0.52 | MDCK-MDR1 | 5 | 0.004 | 0.47 | 38 |
MDCK-MDR1 + CsA | 5 | 0.01 | 0.02 | 0.4 | ||
Atorvastatin2 | 0.52 | MDCK-MDR1 | 0.5 | 0.001 | 0.05 | 12 |
MDCK-MDR1 + CsA | 0.5 | 0.005 | 0.01 | 0.9 | ||
Atorvastatin3 | 0.52 | MDCK-MDR1 | 5 | 0.01 | 0.75 | 17 |
MDCK-MDR1 + CsA | 5 | 0.07 | 0.16 | 0.7 |
Notations are defined as follows: fum: fraction of drug unbound in microsomes; C0: drug concentration at time zero; Cr,AB: concentration in the receiver compartment upon apical drug exposure; Cr,BA: concentration in the receiver compartment upon basolateral drug exposure; ER: efflux ratio