Metabolite | CYP2C19 | CYP2C9 | CYP3A4 | CYP2A6 | CYP2D6 | |
---|---|---|---|---|---|---|
V max | Sulfone | — | — | 13.3 ± 0.53 | — | — |
5-O-desmethyl | 2.35 ± 0.15 | 0.77 ± 0.4 | 0.74 ± 0.24 | — | NE | |
Hydroxy | 0.99 ± 0.1 | 1.71 ± 0.69 | 2.13 ± 0.80 | 1.11 ± 1.16 | NE | |
K m | Sulfone | — | — | 83 ± 8.8 | — | – |
5-O-desmethyl | 1.59 ± 0.99 | 107 ± 121 | 262 ± 162 | — | NE | |
Hydroxy | 6.01 ± 2.8 | 209 ± 140 | 367 ± 235 | 1000 ± 1440 | NE | |
CLint | Sulfone | — | — | 160 ± 11.6 | — | — |
5-O-desmethyl | 1479 ± 853 | 7.2 ± 4.6 | 2.8 ± 0.9 | — | 3.1 ± 0.3 | |
Hydroxy | 165 ± 67 | 8.1 ± 2.3 | 5.8 ± 1.7 | 1.11 | 6.5 ± 0.3 |
Km expressed as micromoles per liter,Vmax as nanomoles per minute per nanomoles of P450, and CLint as microliters per minute per nanomoles of P450. Trivial names of the metabolites given in Fig. 2 are used.
NE, not estimated.
—, indicates that no metabolite was detected.