TABLE 6

The effects of P-gp inhibitors on transcellular transport of P-gp substrates in Caco-2 cell monolayers

Substrate (μM) Inhibitor (μM) −InhibitoraRcaco(−I) B-A/A-B +InhibitoraRcaco (+I) B-A/A-B Ratio(+I/cont) Typeb Reference
A-B B-A A-B B-A A-B B-A
Grepafloxacin (5) Grepafloxacin 1000 0.6 2.1 3.4 1.7 1.6 0.9 2.77 0.76 A Yamaguchi et al., 2000
Saquinavir (5) PSC-833 1 2.3 22.8 9.8 8.8 12.9 1.5 3.78 0.57 B Kim et al., 1998
Indinavir (5) PSC-833 1 1.7 18.4 11 7.0 10.6 1.5 4.20 0.58 B Kim et al., 1998
Rhodamine-123 (5) Verapamil 100 0.1 3.7 34 0.3 0.3 1.3 2.46 0.09 C Takano et al., 1998
Cyclosporine (1) Verapamil 100 3.5 25.4 7.2 6.4 7.5 1.2 1.80 0.30 C Alsenz et al., 1998
Vinblastine (0) GF120918 10 3.8 12.9 3.4 6.2 5.9 1.0 1.61 0.46 C Lentz et al., 2000
Digoxin (5) CP114416 1 1.6 12.5 7.7 4.2 3.5 0.8 2.57 0.28 C Wandel et al., 1999

  • ↵ a Papp (×10−6 cm/s).

  • ↵ b Classification types for the effect of P-gp inhibitors on the transcellular transport of P-gp substrates shown in Fig. 1.