Mean (± S.D.) plasma concentration of prasugrel metabolites in human plasma after a single 15-mg (100 μCi) p.o. dose of [14C]prasugrel
Metabolite | Prasugrel | ||||
|---|---|---|---|---|---|
| 0.5 h | 1.0 h | 2.0 h | |||
| ng-Eq/ml plasma | |||||
| 14C | 481 ± 182 | 432 ± 74 | 362 ± 94 | ||
| M1 (m/z 336) | 28.9 ± 18.2 | 24.9 ± 15.4 | 36.2 ± 12.4 | ||
| M2 (R-95913, m/z 332) | 62.6 ± 33.7 | 31.8 ± 8.0 | 21.7 ± 11.0 | ||
| M3 (R-138727, m/z 350)a | 82.8 ± 23.1 | 47.3 ± 12.2 | 23.6 ± 17.5 | ||
| M5 (R-106583, m/z 364) | 106.2 ± 63.7 | 116.0 ± 13.1 | 113.4 ± 35.6 | ||
| M6 (R-100932, m/z 364) | 33.8 ± 18.7 | 24.0 ± 13.2 | 26.6 ± 9.4 | ||
| M7 (R-119251, m/z 469) | 37.1 ± 13.3 | 20.3 ± 15.4 | 17.2 ± 14.3 | ||
| M9 (m/z 318) | 14.5 ± 7.7 | 17.0 ± 11.2 | 12.5 ± 3.9 | ||
| M10 (m/z 380) | 2.9 ± 2.3 | 7.5 ± 5.8 | 7.4 ± 7.3 | ||
| M11 (m/z 380) | 10.1 ± 16.9 | 7.7 ± 10.8 | 12.7 ± 11.6 | ||
| M13 (glucuronide, m/z 508) | 15.8 ± 9.1 | 16.9 ± 5.0 | 8.9 ± 8.8 | ||
| M14 (glucuronide, m/z 540) | 9.9 ± 8.9 | 10.5 ± 6.8 | 15.2 ± 14.4 | ||
| M15 (glucuronide, m/z 540) | 11.0 ± 12.7 | 3.9 ± 8.6 | 1.4 ± 3.2 | ||
| M16 (glucuronide, m/z 556) | 10.9 ± 6.0 | 19.0 ± 7.8 | 15.9 ± 4.8 | ||
↵ a Because of the instability of R-138727, values reported here were obtained from assay of derivatized R-138727 in plasma samples.