IC502-a of efflux protein inhibitors for CPT-11 transport across MDCK II/Pgp and MDCK II/cMOAT cells
| Inhibitors | MDCK II/Pgp (Mean ± S.D.) | MDCK II/cMOAT (Mean ± S.D.) | ||
|---|---|---|---|---|
| Absorption | Efflux | Absorption | Efflux | |
| μM | ||||
| GF120918 | 0.21 ± 0.05 | 0.38 ± 0.06 | N.E. | N.E. |
| Verapamil | 29 ± 6 | 234 ± 48 | N.D. | N.D. |
| Etoposide | 468 ± 56 | 1185 ± 190 | N.D. | N.D. |
| MK-571 | N.E. | N.E. | 50 ± 14 | 470 ± 60 |
↵2-a IC50 is defined as the concentration of inhibitor corresponding to 50% of change in permeability.
N.E., No effect.
N.D., Not determinable.