Percentage of dose excreted over 48 h in urine, bile, and feces identified as ruboxistaurin and its metabolites following a single oral dose of 5 mg/kg [14C]ruboxistaurin in Fischer 344 rats
Metabolite | Percentage of Dose | ||||||
|---|---|---|---|---|---|---|---|
| Urine | Bile | Fecesa | Total | ||||
| Ruboxistaurin | <0.1 | 0.1 | 9.1 | 9.2 | |||
| 1 | 1.4 | 1.5 | 8.6 | 11.5 | |||
| 2 | 0.2 | 2.1 | 0.4 | 2.7 | |||
| 3 | 0.2 | 0.9 | 0.7 | 1.8 | |||
| 5 | 0.9 | 31.9 | N.D. | 32.8 | |||
| 7 | N.D. | N.D. | 0.4 | 0.4 | |||
| 8 | N.D. | N.D. | <0.1 | <0.1 | |||
| 10 | 0.1 | 5.5 | 1.0 | 6.6 | |||
| 12 | N.D. | N.D. | b | b | |||
| 13 | N.D. | N.Q. | N.D. | N.Q. | |||
| 14 | N.D. | N.D. | <0.1 | <0.1 | |||
| 15 | N.D. | N.D. | N.Q. | N.Q. | |||
| 17 | N.D. | 5.0 | 0.6 | 5.6 | |||
| 18c + 22 | N.D. | 3.4 | N.D. | 3.4 | |||
| 19 d | N.D. | 3.3 | N.D. | 3.3 | |||
| 21 | N.D. | 2.2 | N.D. | 2.2 | |||
| 23 | N.D. | 0.9 | N.D. | 0.9 | |||
| 25 | N.D. | e | N.D. | e | |||
| Total percentage of dose excreted | 2.8 | 56.8 | 20.8 | 80.4 | |||
| Total percentage of dose recovered over 48 h in excretion portion of study | 2.9 | 59.1 | 34.5 | 96.5 | |||
N.D., not detected; N.Q., not quantifiable, observed with LC/MS detection.
↵ a Dose corrected for extraction recovery of 78% in feces.
↵ b In feces, 10 and 12 were not resolved.
↵ c In bile, 18 and 22 were not resolved.
↵ d A second hydroxylated N-desmethyl glucuronide metabolite was detected in bile and accounted for 2.2% of the dose.
↵ e In bile, 23 and 25 were not resolved.