TABLE 2

Correlation of formation rates of 8-hydroxyefavirenz (MI), 7-hydroxyefavirenz (MII), and 8,14-dihydroxyefavirenz (MIII) from efavirenz (10 μM) with the activities of different P450 isoforms and total P450 contents in 11 HLMs

Data were analyzed using the nonparametric correlation test (Spearman r). The activity of each isoform was determined using the respective specific substrate probe reaction as indicated by the supplier (see Materials and Methods). p = 0.05 is considered statistically significant.



Metabolites of Efavirenz
P450s MI
MII
MIII
MI + MIII

r
p
r
p
r
p
r
p
Total P450 0.65 0.049 -0.1 0.79 0.66 0.044 0.65 0.049
Oxidoreductase 0.43 0.22 0.42 0.23 0.47 0.18 0.43 0.22
Cytocrhome b5 -0.44 0.2 0.47 0.18 -0.45 0.19 -0.44 0.2
1A2 -0.16 0.66 0.02 0.97 -0.25 0.49 -0.17 0.66
2A6 0.20 0.58 0.45 0.19 0.42 0.23 0.20 0.58
2B6 0.77 0.013 -0.31 0.39 0.72 0.02 0.77 0.013
2C8 0.66 0.044 0.26 0.47 0.61 0.067 0.66 0.044
2C9 0.15 0.68 0.20 0.58 0.26 0.47 0.15 0.68
2C19 0.16 0.66 0.08 0.84 0.07 0.87 0.16 0.66
2D6 -0.16 0.66 -0.01 1.0 -0.07 0.87 -0.16 0.66
2E1 0.49 0.15 0.04 0.91 0.58 0.088 0.49 0.15
3A 0.85 0.003 0.09 0.8 0.95 0.0001 0.85 0.003
4A
0.05
0.89
0.6
0.07
-0.06
1.0
0.05
0.89