Table 5.
Relative Exposure to the Major Metabolites of S807 as a Function of Administered Dose in Male and Female Rats.
| Metabolite | Dose (mg/kg bw) | Males |
Females |
||||||
|---|---|---|---|---|---|---|---|---|---|
| Tmax (hr) | Cmax Ratioa |
AUClast Ratiob | % Total Metabolite AUClastc | Tmax (hr) | Cmax Ratioa |
AUClast Ratiob |
% Total Metabolite AUClastc | ||
| M265(A-B)-1 | 20 | 0.31 | 1.0 | 1.0 | 44.17 | 0.25 | 1.0 | 1.0 | 41.70 |
| 50 | 0.75 | 1.94 | 3.37 | 45.94 | 0.38 | 1.48 | 2.60 | 46.58 | |
| 200 | 3.0 | 4.32 | 17.7 | 50.06 | 0.50 | 2.66 | 11.6 | 48.54 | |
| M441B-1 | 20 | 4.5 | 1.0 | 1.0 | 29.26 | 2.2 | 1.0 | 1.0 | 35.74 |
| 50 | 6.0 | 2.10 | 2.17 | 19.55 | 2.8 | 1.83 | 2.14 | 32.82 | |
| 200 | 8.0 | 3.80 | 3.97 | 7.42 | 8.0 | 4.24 | 5.49 | 19.64 | |
| M427B-1 | 20 | 7.0 | 1.0 | 1.0 | 5.40 | 5.0 | 1.0 | 1.0 | 10.43 |
| 50 | 15 | 1.55 | 1.86 | 3.10 | 4.3 | 1.33 | 1.27 | 5.68 | |
| 200 | 24 | 3.98 | 3.20 | 1.10 | 8.3 | 3.05 | 3.33 | 3.47 | |
| M293A-1 | 20 | 0.50 | 1.0 | 1.0 | 7.34 | 0.44 | 1.0 | 1.0 | 7.25 |
| 50 | 1.75 | 2.34 | 3.26 | 7.37 | 1.0 | 1.28 | 2.59 | 8.06 | |
| 200 | 1.5 | 4.63 | 8.95 | 4.20 | 1.4 | 3.48 | 11.8 | 8.55 | |
| M279B-1 | 20 | 0.56 | 1.0 | 1.0 | 1.83 | 0.38 | 1.0 | 1.0 | 2.00 |
| 50 | 2.5 | 5.59 | 13.6 | 7.65 | 0.75 | 2.30 | 4.94 | 4.24 | |
| 200 | 6.0 | 51.1 | 156 | 18.19 | 8.0 | 17.7 | 87.1 | 17.43 | |
| M345B-1 | 20 | 1.0 | 1.0 | 1.0 | 6.65 | 0.50 | 1.0 | 1.0 | 0.80 |
| 50 | 2.0 | 2.19 | 4.37 | 8.96 | 0.88 | 1.49 | 2.43 | 0.84 | |
| 200 | 5.0 | 3.96 | 12.8 | 5.44 | 0.88 | 2.84 | 6.10 | 0.49 | |
| M281A-1 | 20 | 0.38 | 1.0 | 1.0 | 5.25 | 0.25 | 1.0 | 1.0 | 1.89 |
| 50 | 0.75 | 1.73 | 4.33 | 7.02 | 0.38 | 1.23 | 1.84 | 1.49 | |
| 200 | 3.0 | 6.48 | 39.2 | 13.16 | 0.50 | 1.73 | 5.61 | 1.06 | |
| M251A-1 | 20 | 0.31 | 1.0 | 1.0 | 0.09 | 0.25 | 1.0 | 1.0 | 0.19 |
| 50 | 0.44 | 2.63 | 13.8 | 0.39 | 0.31 | 1.63 | 3.47 | 0.28 | |
| 200 | 0.50 | 14.3 | 73.7 | 0.44 | 0.31 | 12.1 | 43.7 | 0.82 | |
Cmax Ratio = Cmax/Cmax at 20 mg/kg bw dose.
AUC Ratio = AUClast/AUClast at the 20 mg/kg bw dose.
% Total Metabolite AUClast =% peak area for a given metabolite as a% of the total peak area of the eight designated metabolites at that dose.