TABLE 2

Inactivation kinetic constants for PPP, thioTEPA, clopidogrel, and ticlopidine for CYP2B6 catalyzed bupropion hydroxylase in pooled human liver microsomes a

Parameter
PPP
ThioTEPA
Clopidogrelb
Ticlopidine
K1 (μM) 5.6 ± 1.2 4.8 ± 1.0 1.4 ± 0.1 0.32 ± 0.04
kinact (1/min) 0.13 ± 0.01 0.20 ± 0.01 1.9 ± 0.1 0.43 ± 0.02
kinact/K1 (ml/min/μmol)
23
42
1400
1300

  • ↵ a Values represent the mean ± S.E.

  • ↵ b Kinetic parameters for clopidogrel were estimated using data obtained at [clopidogrel] < 2 μM, excluding the decrease in kinact,app observed at high concentrations, and should be considered as estimates.