Mean percentages of urinary, fecal, and total metabolites of erlotinib in humans after a single 100-mg oral dose of [14C]erlotinib (n = 4)
Urine and feces samples were pooled for metabolite profiling. Each 100-ml urine pool was generated from the individual samples collected at 0 to 12 and 12 to 24 h postdose for each subject. Fecal homogenates containing the highest levels of excreted radioactivity were pooled. The ion chromatographic peak areas for fecal samples were corrected based on the weight of fecal homogenate for each subject.
Metabolite | Percentage Excreted | ||||
|---|---|---|---|---|---|
| Urine | Feces | Total | |||
| M2 | 0.1 ± 0.0 | 4.7 ± 1.0 | 4.9 ± 1.0 | ||
| M3 | 0.5 ± 0.1 | 1.1 ± 0.6 | 1.5 ± 0.7 | ||
| M6 | 0.4 ± 0.3 | 20.6 ± 4.4 | 21.0 ± 4.6 | ||
| M7 | 0.3 ± 0.1 | 1.6 ± 0.4 | 1.9 ± 0.3 | ||
| M8 | 0.2 ± 0.1 | N.D. | 0.2 ± 0.1 | ||
| M9 | 0.6 ± 0.3 | N.D. | 0.6 ± 0.3 | ||
| M10 | 0.1 ± 0.0 | N.D. | 0.1 ± 0.0 | ||
| M11 | 2.2 ± 0.9 | 27.2 ± 6.0 | 29.4 ± 6.1 | ||
| M12 | 0.1 ± 0.1 | 1.0 ± 0.3 | 1.1 ± 0.4 | ||
| M13 | 0.0 ± 0.0 | 1.7 ± 0.8 | 1.7 ± 0.8 | ||
| M14 | 0.2 ± 0.1 | 3.0 ± 1.1 | 3.2 ± 1.1 | ||
| M16 | N.D. | 9.6 ± 3.7 | 9.6 ± 3.7 | ||
| M17 | N.D. | 3.2 ± 0.8 | 3.2 ± 0.8 | ||
| M18 | 0.3 ± 0.1 | N.D. | 0.3 ± 0.1 | ||
| Erlotinib | 0.3 ± 0.2 | 1.0 ± 0.3 | 1.3 ± 0.5 | ||
| Total Dose Identified | 5.3 ± 1.6 | 75 ± 7.9 | 80 ± 8.8 | ||
| Total Dose Pooled | 5.9 | 79.5 | 85.4 | ||
a N.D., not detectable.