Mean (n = 6) percentage of dose excreted in urine and feces identified as ruboxistaurin and metabolites from healthy male subjects after a single oral administration of 64 mg of [14C]ruboxistaurin
Metabolite I.D. | Percentage of Dose Represented by Metabolitea | ||||
|---|---|---|---|---|---|
| Urine (0-48 h) | Fecesb (0-120 h) | Total | |||
| Ruboxistaurin | <1.0 | 1.2 | 1.3 | ||
| 1 (LY338522) | 1.1 | 28.0 | 29.2 | ||
| 5 | <1.0 | 9.2 | 9.4 | ||
| 3 | <1.0 | 4.1 | 4.2 | ||
| 28 c | <1.0 | 3.9 | 3.9 | ||
| 17 | <0.1 | 3.0 | 3.1 | ||
| 14 | c | 2.5 | 2.5 | ||
| 2 c | <0.1 | 1.8 | 1.8 | ||
| 10 + 12 | <0.1 | 1.1 | 1.1 | ||
| Total radioactivity identifiedd | 2.3 | 57.2 | 59.5 | ||
| Total radioactivity excreted | 3.0 | 78.2 | 81.2 | ||
1 = N-desmethyl ruboxistaurin; 2 = N,N-didesmethyl ruboxistaurin; 17, 10, 5, 15, 8, 11, 9 = N-desmethyl ruboxistaurin + O; 3, 14, 12, 16, 28 = ruboxistaurin + O; 29 = dealkylated ruboxistaurin (alcohol); 6 = N-oxide of ruboxistaurin; 27 = ruboxistaurin + O2; 18 = ruboxistaurin + O + glucuronide.
↵ a Metabolite percentages have been adjusted for the extraction recovery results of approximately 91% for feces and approximately 100% for urine.
↵ b For subject 4027, 0- to 144-h fecal samples were examined.
↵ c In urine, 2 elutes with 14, and 15 elutes with 28.
↵ d Metabolites 11, 8, 15, 27, 16, 29, 9, 18, and 6 each represented <1.0% of the total dose and are not included in the totals.