TABLE 2

In vitro interaction of statins with MDR1 P-glycoprotein in the MDR1-MDCK transport and ATPase assays (n = 2)

Compound
MDR1-MDCK Efflux Ratio (2 μM)
MDCK B-A/A-B (2 μM)
Km in ATPase Assay
μM
Pravastatin acid 1.87 1.51 N.A.
Atorvastatin acid 4.46 2.26 N.A.
Atorvastatin lactone 2.32 4.31 3.61
Lovastatin acid 3.17 1.58 N.A.
Lovastatin lactone 2.17 1.16 11.5
Simvastatin acid 2.00 1.31 N.A.
Simvastatin lactone 0.93 0.46 12.3
Prazosina 3.50 1.80 not applicable
Quinidinea 15.0 4.1 not applicable
Verapamilb
not applicable
not applicable
7.55

  • N.A., not available because the compound did not show stimulation of ATP hydrolysis.

  • ↵ a Positive controls as P-glycoprotein substrates used for the MDR1-MDCK transport assay

  • ↵ b Positive control used for the ATPase assay