TABLE 1

Uptake kinetic parameters of seven OATP substrates estimated in human hepatocyte using a mechanistic two-compartment model

Uptake kinetics was measured in cryopreserved human hepatocytes (donor HU4122) plated for 6 h over 2 min at seven concentrations (0.1–300 μM).

DrugKm, uVmaxPdiff,ufucellafumedCLactive, u
μMpmol · min1 · 106 cells1μl · min1 · 106 cells1μl · min1 · 106 cells1
Bosentan22.54029.740.0960.8517.9
Pitavastatin1.596513.20.0530.6340.7
Pravastatin2.256.240.2080.9630.912.77
Repaglinide15.6123610.00.0740.9579.0
Rosuvastatin11.21040.3910.4770.939.21
Telmisartanb2.0319314.10.0240.7195.2
Valsartan10.4300.064112.88
  • a Data from uptake experiments performed in rat hepatocytes (Ménochet et al., 2012).

  • b Kinetics parameters obtained when telmisartan metabolism was incorporated in the modeling (CLmet = 4.3 μl · min−1 · 106 cells−1).