Relative abundance of unchanged [14C]R115777 and some of its metabolites in an overall pool of the 0- to 24-h urine samples, an overall pool of methanolic extracts of a pooled feces sample and overall pool of a 3 h plasma sample, collected from four healthy male subjects
| Metabolite | Urine | Feces | ||||||
|---|---|---|---|---|---|---|---|---|
| % of Sample Radioactivity | % of Dose | % of Sample Radioactivity | % of Dose | Plasma % of Sample Radioactivity | ||||
| HPLC Run 1 | HPLC Run 2 | HPLC Run 1 | HPLC Run 2 | HPLC Run 1 | HPLC Run 2 | |||
| R115777-Glucuronide | 96.0 | 10.0 | N.D. | N.D. | N.D. | N.D. | 82.9 | 69.5 |
| R130525 | N.D. | N.D. | N.Q. | N.Q. | N.Q. | N.Q. | 4.5 | 4.1 |
| R115777 | N.D. | N.D. | 8.9 | 11.8 | 5.1 | 6.8 | 7.8 | 13.4 |
| R110127 | N.D. | N.D. | 15.3 | 15.0 | 8.8 | 8.6 | N.Q. | N.Q. |
| R101763 | N.D. | N.D. | 22.9 | 19.8 | 13.1 | 11.4 | 7.8 | 1.0 |
| R104209 | N.D. | N.D. | 12.9 | 14.0 | 7.4 | 8 | 1.2 | 1.1 |
| Total | 96.0 | 10.0 | 60.0 | 60.6 | 34.4 | 34.8 | 96.4 | 89.1 |
Fractions collected by HPLC as detailed in Figure 4. Metabolite profiles were determined by AMS of HPLC fractions. Relative abundances in urine and feces extract were converted to levels of excretion (expressed as % of dose). Values for urine are reported for one HPLC run. Values for feces and plasma are reported for two HPLC runs.
N.Q., Not quantifiable.
N.D., Not detected.