TABLE 2

Kinetic parameters of time-dependent inhibitors in different in vitro matrices


Compound

P450 Isoform

Enzyme Source

KI

kinact

Reference
μM min-1
Tienilic acid CYP2C9 rCYP2C9 2 0.19 This laboratory
rCYP2C9 (2C10) 4 0.20 Lopez-Garcia et al., 1994
Human hepatocytes 2 0.05 This laboratory
Erythromycin CYP3A4 rCYP3A4 9 0.12 This laboratory Atkinson et al., 2005
rCYP3A4 5 0.12 Chan and Delucchi, 2000
HLMs 16a 0.07 Kanamitsu et al., 2000
HLMs 82a 0.07 Yamano et al., 2001
HLMs 13a 0.02 Ito et al., 2003
HLMs 10a 0.08 Dai et al., 2003
HLMs 11a 0.05 McConn et al., 2004
HLMs 15a 0.07 Zhao et al., 2005
Human hepatocytes 11 0.07 This laboratory
Troleandomycin CYP3A4 rCYP3A4 0.3 0.12 This laboratory Atkinson et al., 2005
rCYP3A4 0.2 0.15 Chan and Delucchi, 2000
HLMs 2a 0.03 Zhao et al., 2005
Human hepatocytes 0.4 0.05 This laboratory
Fluoxetine CYP3A4 rCYP3A4 2 0.03 This laboratory
HLMs 5a (0.5) 0.01 This laboratory
HLMs 5a 0.02 Mayhew et al., 2000
Human hepatocytes 1 0.01 This laboratory
CYP2C19 rCYP2C19 0.4 0.5 This laboratory
HLMs 8a (0.8) 0.03 This laboratory
Human hepatocytes 0.2 0.04 This laboratory
AZ1 CYP2C9 rCYP2C9 30 0.02 This laboratory


Human hepatocytes
19
0.02
This laboratory
  • a Apparent KI values. All other values including those in parentheses are unbound KI estimates.