TABLE 2

Inhibitory effects of the statins on the ATP-dependent uptake of TCA by hBSEP- and rBsep-expressing membrane vesicles The values are expressed as mean ± computer-calculated S.D. The log P values were estimated by Ishigami et al. (2001).


Statin

Log P

Ki Value for hBSEP

Ki Value for rBSEP
μM
Atorvastatin 1.5 9.12 ± 0.82 7.57 ± 1.17
Cerivastatin 2.3 11.4 ± 1.3 30.3 ± 4.1
Fluvastatin 1.8 30.2 ± 4.5 30.7 ± 3.1
Pitavastatin 1.5 25.6 ± 3.6 40.8 ± 4.8
Pravastatin -0.47 163 ± 20 805 ± 97
Rosuvastatin -0.30 120 ± 15 385 ± 59
Simvastatin acid 1.9 12.7 ± 1.4 30.0 ± 4.0
Atorvastatin lactone 4.2 13.7 ± 4.4 12.0 ± 5.3
Pitavastatin lactone 4.6a 59.9 ± 12.8 228 ± 48
Pravastatin lactone 2.4 37.6 ± 4.5 260 ± 35
Simvastatin (lactone)
4.4
23.1 ± 5.8
48.2 ± 10.4
  • a Calculated by ChemDraw version 7.0 (Chemical Drawing software; CambridgeSoft Corporation, Cambridge, MA)