TABLE 2

Kinetic parameters of CYP3A time-dependent inhibitors

CompoundFreshCryopreservedHepaRGHLM
KI (μM)kinact (min−1)KI (μM)kinact (min−1)KI (μM)kinact (min−1)KI (μM)kinact (min−1)
Clarithromycin12.60.068.10.095.40.0817.70.05
Mibefradil0.60.100.20.281.10.911.10.70
Troleandomycin0.90.100.60.082.20.171.80.31
Verapamil12.60.141.90.145.50.128.90.10
Fluoxetine7.30.0317.10.0335.70.018.60.005
  • Fresh, freshly plated human hepatocytes; Cryopreserved, cryopreserved plated human hepatocytes; HepaRG, cryopreserved plated HepaRG.