TABLE 5

Summary of in vitro pharmacokinetic parameters of all tested drugs in humans and cynomolgus monkeys

Lithium was excluded from all in vitro studies.

DrugsSpeciesRbPappProtein BindingfpfbCLintliverCLintintestinefb*CLintliver/QhATPase
×10−6cm/s%ml/min/kgμ l/min/mg proteinratio vs VER
HydrochlorothiazideHuman2.700.140.00.6000.222aaa0
Monkey1.8439.00.6100.331aaaNT
DexamethasoneHuman0.9516.452.00.4800.50766a1.620.01
Monkey1.3477.50.2250.16724a0.09NT
NifedipineHuman0.7413.493.40.0660.0894381381.890.03
Monkey0.6594.30.0570.08825976124.96NT
MidazolamHuman0.6930.897.00.0300.0448773851.850.28
Monkey0.7795.70.0430.056142216351.72NT
QuinidineHuman0.7217.991.40.0860.11952a0.304.57
Monkey0.7892.10.0790.1028722121.91NT
TacrolimusHuman20.0034.298.90.0110.00115386250.047.89
Monkey20.0099.00.0100.001579346630.06NT
VerapamilHuman0.9235.895.20.0480.052656691.651.00
Monkey0.9388.20.1180.12724916966.83NT
DigoxinHuman1.000.160.30.3970.398aaa56.1
Monkey0.8252.90.4710.574aaaNT
PropranololHuman0.89b37.4860.1400.157165a1.251.70
Monkey0.85c78.80.2120.249974a5.25NT
AmitriptylineHuman0.86d53.385.40.1460.17080a0.661.20
Monkey1.4087.20.1280.0912559a5.06NT
TimololHuman0.84b27.350.90.4910.58532a0.891.66
Monkey1.0295.50.0450.044391a0.37NT
IbuprofenHuman0.55d29.498.80.0120.02238a0.041.14
Monkey0.6198.50.0150.02425a0.01NT
  • Papp, apparent permeability; NT, not tested.

  • a The CLint could not be calculated because the tested drug was not depleted.

  • b Data were taken from Shibata et al., 2002.

  • c Data were taken from Evans et al., 1973.

  • d Data were taken from Obach, 1999.