Analysis of major metabolites M1 and M2 in human and rat plasma samples collected after multiple oral doses
All doses indicate free base equivalents.
| Species | Original Study | Dose Level in Original Study | Once-Daily Dose Level | Collection Day | No. of Time Points for AUC Proportional Sample Pooling | No. of Samples Pooled | Measured Concentration in Pooled Plasma Sample | |
|---|---|---|---|---|---|---|---|---|
| M1 | M2 | |||||||
| μM | ||||||||
| Human | MAD | Intermediate | 40 mg | 15 | 12 | 7 | 4.58 | 7.93 |
| Placebo | 15 | 12 | 3 | N.A. | N.A. | |||
| Rat | TK | Middle | 15 mg/kg | 92 | 6 | 3 M/3 F | 1.24 | 19.2 |
| Rat, M | TK | High | 75 mg/kg | 92 | 6 | 3 | 9.05 | 57.9 |
| Rat, F | TK | High | 50 mg/kg | 92 | 6 | 3 | 3.32 | 32.8 |
N.A., not applicable; M, male; F, female.