TABLE 2

Efflux ratio of [3H]prazosin, [14C]zidovudine, [3H]abacavir, and [14C]imitanib in MDCK wild-type, MDCK Bcrp1 cells, and MDCK Bcrp1 cells in the presence of the inhibitors Ko143, GF120918, nelfinavir, and Pluronic P85

Efflux ratio = Papp B-to-A transport/Papp A-to-B transport.




MDCK WT

MDCK Bcrp1

MDCK Bcrp1 + Ko143 (200 nM)

MDCK Bcrp1 + GF120918 (5 μM)

MDCK-Bcrp1 + Nelfinavir (25 μM)

MDCK-Bcrp1 +P85 (0.01% w/v)
Prazosin 1.3 10.5 1.4 (complete)a 5.0 (partial)b 9.8 (N.S.)c 12.5 (N.S.)
Zidovudine 0.9 10 0.8 (complete) 1.3 (complete) 1.6 (complete) 4.4 (partial)
Abacavir 1.3 27 1.1 (complete) 1.4 (complete) 1.5 (complete) 7.8 (partial)
Imatinib (STI-571)
1.8
62
2.2 (complete)
27.5 (partial)
24.7 (partial)
57 (N.S.)
  • WT, wild type; N.S., not significant.

  • a Efflux ratio in the Bcrp1-transfected cells reduced by at least 85%.

  • b Efflux ratio reduced by at least 50% but less than 85%.

  • c No significant reduction in efflux ratio.