TABLE 1

Binding and clearance properties of four inhibitors selected for study

InhibitorKpCLint hepatocytesfu, microsomes (at 1 mg/ml)fu, hepatocytes (at 106 cells)a
μl/min/106 cells
Enoxacin20b9.6c0.99c0.99
Clarithromycin22b16.9c0.81c0.86
Saquinavir306d486d0.093d0.14
Nelfinavir3352d1290d0.022d0.035

  • CLint, intrinsic clearance; fu, fraction of unbound drug.

  • ↵a Calculated from Kilford et al. (2008).

  • ↵b Data from Yamano et al. (1999).

  • ↵c J. Alder and J. D. Davis, unpublished data.

  • ↵d Data from Parker and Houston (2008).