Table 2

IC502-a of efflux protein inhibitors for CPT-11 transport across MDCK II/Pgp and MDCK II/cMOAT cells

InhibitorsMDCK II/Pgp (Mean ± S.D.)MDCK II/cMOAT (Mean ± S.D.)
AbsorptionEffluxAbsorptionEfflux
μM
GF1209180.21  ± 0.050.38  ± 0.06N.E.N.E.
Verapamil29  ± 6234  ± 48N.D.N.D.
Etoposide468  ± 561185  ± 190N.D.N.D.
MK-571N.E.N.E.50  ± 14470  ± 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.