TABLE 1

Summary of kinetic parameters for carbamazepine 10,11-epoxidation in different in vitro systems


In Vitro System

Type of Kinetics

Vmax

Km or Ks

α

αKs

CLint or CLmax

CLint or CLmax
pmol/min/pmol CYP or mg protein or 106 cells μM μM μl/min/pmol CYP or mg protein or 106 cells μl/min/g liver
rCYP3A4 Michaelis-Menten 5.3 630 n/a n/a 0.0083a 36
rCYP3A5 Sigmoidalb 10 2300 0.092 210 0.0077 (rCYP3A4 + rCYP3A5)
HLMs Sigmoidalb 440 1900 0.012 23 1.1 34
Human hepatocytes
Sigmoidalb
27
840
0.045
38
0.076
7.5
  • a The value represents CLint

  • b The kinetic parameters were determined using the two-site kinetic model assuming the equivalence of two active sites (Houston and Kenworthy, 2000)