Summary of predicted hepatic clearance of aldehyde oxidase substrates in cryopreserved human hepatocytes compared with reported human pharmacokinetic properties

Hepatic clearance estimates (ml · min−1 · kg−1) were calculated as described under Materials and Methods. Data are presented as mean (S.D.) from n = 4 replicates.

SubstratePredicted Hepatic ClearanceaPredicted Hepatic ClearancebEhcPredicted Oral BioavailabilitydHuman Total ClearanceHuman Oral BioavailabilityReference
ml · min1 · kg1ml · min1 · kg1%F
BIBX138217.6 (0.2)18.2 (0.2)85–8812–1525–552–12Dittrich et al., 2002
Carbazeran17.8 (0.1)17.3 (0.6)84–8614–1638<5Kaye et al., 1984
O6-Benzylguanine11.2 (0.2)12.8 (0.2)54–6215.6Dolan et al., 1998
Zaleplon<4.3<4.3<21>7915.730Rosen et al., 1999
XK-469<4.3<4.3<21<1Alousi et al., 2007
  • a Celsis/In Vitro Technologies (lot OOO).

  • b Life Technologies, Inc. (lot HuE104).

  • c Calculated using eq. 3 using range of hepatic clearance values observed in cryopreserved hepatocytes.

  • d Calculated using eq. 5.