TABLE 4.
Kinetic parameters for 8-hydroxyefavirenz formation from S-efavirenz
Results (Vmax, K, n, Ki, and Vi) are the parameter estimates and S.E. of the estimate, determined by nonlinear regression analysis using a model of cooperative substrate binding with substrate inhibition and cooperative inhibitor binding over the substrate concentration range 0.25–100 μM.
| Vmax | K | n | Clmax | Ki | Vi | |
|---|---|---|---|---|---|---|
| pmol⋅min/pmol | µM | mM | pmol/min per picomoles | |||
| CYP2B6.1 | 7.4 ± 2.4 | 17 ± 8 | 1.4 ± 0.3 | 0.25 | 47 ± 10 | 0.0001 ± 0.42 |
| CYP2B6.4 | 6.2 ± 1.0 | 9 ± 2 | 1.7 ± 0.3 | 0.35 | 53 ± 8 | 0.0002 ± 0.44 |
| CYP2B6.5 | 4.1 ± 0.4 | 11 ± 2 | 1.2 ± 0.1 | 0.25 | 75 ± 10 | 5.8e−5 ± 0.42 |
| CYP2B6.6 | 3.6 ± 0.2 | 13 ± 1 | 1.7 ± 0.1 | 0.14 | 84 ± 16 | 1.46 ± 0.43 |
| CYP2B6.7 | 2.7 ± 1.0 | 16 ± 12 | 1.0 ± 0.2 | 0.17 | 46 ± 11 | 4.5e−5 ± 0.14 |
| CYP2B6.9 | 2.8 ± 0.7 | 21 ± 10 | 0.9 ± 0.1 | 0.13 | 57 ± 9 | 4.4e−5 ± 0.15 |
| CYP2B6.17 | 5.5 ± 0.5 | 13 ± 2 | 1.4 ± 0.1 | 0.23 | 71 ± 8 | 2.8e−5 ± 0.44 |
| CYP2B6.19 | 3.5 ± 0.2 | 14 ± 2 | 1.5 ± 0.1 | 0.13 | 173 ± 448 | 7.1e−5 ± 21 |
| CYP2B6.26 | 2.1 ± 0.4 | 9 ± 4 | 1.2 ± 0.3 | 0.15 | 56 ± 11 | 5.7e−5 ± 0.18 |