TABLE 3

Kinetic parameters of nor-VER, D617, M1, M2, M3, and M4 metabolites in human CYP3A7 The values are expressed as mean of three and S.D.


Parameters

R-(+)- or S-(-)-VER

Metabolite
nor-VER
D617
M1
M2
M3
M4
Km (μM) R 68.1 ± 7.7 53.2 ± 5.7 30.3 ± 1.5 58.6 ± 7.1 85.9 ± 11.0 60.0 ± 8.8
S 55.6 ± 4.4 38.2 ± 3.9 22.0 ± 1.0 50.2 ± 4.0 51.8 ± 5.8 61.8 ± 7.0
Vmax (pmol/min/mg) R 306 ± 19 112 ± 4 2.43 ± 0.03 1.42 ± 0.05 1.15 ± 0.05 2.21 ± 0.10
S 605 ± 26 173 ± 5 3.14 ± 0.04 2.13 ± 0.05 0.94 ± 0.03 1.63 ± 0.06
Ki (μM) R 482 ± 69 NA NA NA NA NA

S
365 ± 34
NA
NA
NA
NA
NA
  • NA, not applicable.