TABLE 1

Physicochemical and in vitro properties for the compounds studied

CompoundLog D7.4ChargeapKaB/Pfu, pHLM CLint, u, met
μl · min1 · mg1
Pravastatin−0.84A4.60.550.430
Cerivastatin1.8Z5.3 (B); 5.0 (A)0.760.004829
Bosentan1.3A5.20.480.005322b
Fluvastatin1.6A4.60.570.004176
Rosuvastatin−0.33A4.20.560.0940
Valsartan−0.88A3.8; 4.60.550.00100
Repaglinide2.1Z6.1 (B); 4.4 (A)0.480.0074128c
  • a A, acidic; B, basic; Z, zwitterionic.

  • b Data from Lave et al. (1996), corrected for microsomal binding (fu = 0.87).

  • c Data from Gertz et al. (2010).