TABLE 3.
Active efflux of GS-441524 (5 µM) in Caco-2, MDCK-MDR1 and MDCK-BCRP cell monolayers with the present and absence of Valspodar (MDR1 inhibitor) and Ko143 (BCRP inhibitor) (Data presented are the average of duplicate samples).
| Cell Line | Inhibitor | Papp A to B (10–6 cm/s) | Papp B to A (10–6 cm/s) | Efflux Ratio |
|---|---|---|---|---|
| Caco-2 | None | 0.099 | 0.971 | 9.78 |
| 1 µM Valspodar | 0.16 | 0.79 | 4.93 | |
| 0.5 µM Ko143 | 0.229 | 0.267 | 1.16 | |
| MDCK-MDR1 | None | 0.158 | 0.521 | 3.29 |
| 1 µM Valspodar | 0.484 | 0.468 | 0.967 | |
| MDCK-BCRP | None | <0.197 | 0.385 | >1.96 |
| 0.5 µM Ko143 | <0.198 | <0.281 | ND |