TABLE 2.
The AUC (0–24 hours) for exposure to clemizole and the major in vivo metabolites were calculated for C57BL/6 mice and for human subjects using the data presented in Fig. 1.
For comparison with the in vitro results, the percentage of the total identified metabolites present after clemizole was incubated with human, rat, or mouse microsomes for 1 hour or after incubation with rat or human hepatocytes for 30 minutes are shown.
| Metabolite | % Total AUC |
Microsomes |
Hepatocytes |
||||
|---|---|---|---|---|---|---|---|
| Human | Mouse | Human | Mouse | Rat | Human | Rat | |
| Clemizole | 8.8 | 1.3 | 40 | 24 | 3 | 15 | 0 |
| M1 | 54.9 | 4.7 | 35 | 2 | 4 | 39 | 0 |
| M2 | 1.1 | 5.6 | 2 | 5 | 4 | 0.1 | 0 |
| M4 | 1.1 | 2.9 | 5 | 3 | 5 | 4 | 0 |
| M6 | 22.0 | 2.4 | 2 | 2 | 3 | 18 | 0 |
| M9 | 8.8 | 0.3 | 3 | 19 | 37 | 4 | 1 |
| M12 | 1.1 | 21.2 | 0.6 | 0 | 0 | 1 | 1 |
| M14 | 1.1 | 55.8 | 0 | 0 | 0 | 10 | 5 |
| M15 | 1.1 | 5.9 | 0 | 0 | 0 | 0 | 44 |