TABLE 1

Kinetic parameter estimates for the formation of carbamazepine-10,11-epoxide in HLM and rCYP3A4 according to the two-site equation (Korzekwa et al., 1998)

Vmax1 was set to 0 when relative parameter errors supported the removal of Vmax1 from the two-site equation. Estimates are given as ± S.D. of the fit.


Data Fitted

Equation

Vmax a

n

S50 b

Km1 b

Vmax1 a

Km2 b

Vmax2 a
HLM Hill 0.67 ± 0.02 1.67 ± 0.07 415 ± 19
No felbamate Two-site 617 ± 133 0.10 ± 0.07 214 ± 34 0.71 ± 0.02
Two-site, Vmax1 = 0 516 ± 109 204 ± 31 0.71 ± 0.02
HLM Hill 0.77 ± 0.03 1.40 ± 0.05 471 ± 31
1 mM felbamate Two-site 273 ± 175 0.12 ± 0.12 418 ± 97 0.83 ± 0.06
Two-site, Vmax1 = 0 97 ± 26 517 ± 74 0.89 ± 0.04
rCYP3A4 Hill 1.05 ± 0.02 1.47 ± 0.06 129 ± 5.3
No felbamate Two-site 612 ± 96 2.47 ± 0.34 118 ± 31 0.89 ± 0.04
rCYP3A4 Hill 1.12 ± 0.01 1.53 ± 0.06 101 ± 3.4
500 μM felbamate
Two-site



345 ± 99
1.52 ± 0.52
60.0 ± 15.3
1.07 ± 0.03
  • a Units are in nanomoles per minute per milligram HLM and nanomoles per minute per picomole rCYP

  • b Units are in micromolar