TABLE 4

Effect of incubation with 8-hydroxyefavirenz on the bupropion and cyclophosphamide hydroxylation activities of P450 2B6 and P450 2B6.4 Assay conditions were described under Materials and Methods. Data are representative of the means and S.D. of three separate experiments done in duplicate. Primary reaction mixtures contained 8-hydroxyefavirenz at a concentration of 20 μM.


Primary Reaction Conditions

% Control Activity Remaining
Bupropion
Cyclophosphamide
2B6 – NADPH + 8-hydroxyefavirenz 100 100
2B6 + NADPH + 8-hydroxyefavirenz 32 ± 1 39 ± 2
2B6.4 – NADPH + 8-hydroxyefavirenz 100 100
2B6.4 + NADPH + 8-hydroxyefavirenz
81 ± 5
84 ± 2