TABLE 1

Inactivation of P450 2B6 and P450 2B6.4 using tert-butylhydroperoxide to support the reaction.

P450s were incubated with tBHP and the inactivators indicated as described under Materials and Methods. Activity remaining was determined using the 7EFC O-deethylation assay. The data are presented as percent activity remaining as compared to a control sample incubated with tBHP in the absence of efavirenz or 17EE.


P450

Inactivator

Activity Remaining
50 μM Inactivator
80 μM Inactivator
% %
2B6 Efavirenz 52 ± 2 32 ± 1
2B6.4 Efavirenz 66 ± 3 48 ± 1
2B6 17EE 33 ± 1 21 ± 2
2B6.4
17EE
81 ± 4
70 ± 2