TABLE 3

Kinetic parameters (mean ± S.D.) for the formation of 4-hydroxybupropion from bupropion in 15 human liver microsomal samples with CYP2B6*1/*1, CYP2B6*1/*6, and CYP2B6*6/*6 genotypes (n = 5 HLMs for each genotype)

Bupropion (10–1000 μM) were incubated with HLM samples (0.25 mg/ml) with CYP2B6*1/*1, CYP2B6*1/*6, and CYP2B6*6/*6 genotypes (n = 5 HLMs for each genotype) and a NADPH-generating system at 37°C for 15 min in duplicate. Kinetic parameters (V_max and K_m) for the formation of 4-hydroxybupropion were estimated by fitting the velocity versus bupropion concentrations to the simple single-site Michaelis-Menten. In vitro Cl_int was calculated as V_max/K_m. The kinetic parameters (V_max, K_m, and Cl_int) for each genotype group are listed in Supplemental Table 2. The data presented here are mean ± S.D. calculated from five individual HLM values for each genotype.