Average percentages of urinary and fecal metabolites of CP-122,721 in EM and PM human subjects following administration of a 30-mg (free dose) oral dose
Metabolite | m/z | Description | Percentage Dose for EMa (Mean ± S.D., n = 4) | Percentage Dose for PMa (Mean, n = 2) | ||||
|---|---|---|---|---|---|---|---|---|
| Urine | Feces | Urine | Feces | |||||
| M16 | 409 | Piperadinedione | 2.3 ± 0.3 | N.D. | 2.5 | N.D. | ||
| M1 | 475 | Hydroquinone + Gluc | 4.1 ± 5 | N.D. | N.D. | N.D. | ||
| M17 | 384 | Desmethyl + N-dealkyl + Gluc | 4.5 ± 1 | N.D. | 3.1 | N.D. | ||
| M18 | 402 | Desmethyl + oxidative deamination + Gluc | 10.9 ± 2 | N.D. | 9.5 | N.D. | ||
| M12 | 288 | Desmethyl + N-dealkyl + sulfation | 2.9 ± 1 | N.D. | 0.8 | N.D. | ||
| M2 | 573 | OH + Gluc | 7.3 ± 2 | N.D. | 2.7 | N.D. | ||
| M3 | 559 | Desmethyl + OH + Gluc | 5.5 ± 1 | N.D. | 6.8 | N.D. | ||
| M14 | 559 | Desmethyl + OH + Gluc | 5.3 ± 1 | N.D. | 10.7 | N.D. | ||
| M19 | 557 | Desmethyl + lactam + Gluc | 6.3 ± 2 | N.D. | 17.2 | N.D. | ||
| M4 | 543 | Desmethyl + Gluc | 27.5 ± 9 | N.D. | N.D. | N.D. | ||
| M20 | 573 | Desmethyl + lactam + OH + Gluc | 7.3 ± 3 | N.D. | 2.7 | N.D. | ||
| M15 (TFMSA) | 221 | Trifluoromethyoxy salicylic acid | 1.4 ± 0.2 | N.D. | 3.5 | N.D. | ||
| M7 | 383 | Desmethyl + OH | N.D. | 6.1* | N.D. | N.D. | ||
| M8 | 367 | Desmethyl | N.D. | 3.4* | N.D. | N.D. | ||
| CP-122, 721 | 381 | Parent | 0.4 ± 0.3 | N.D. | 1.9 | 4.63 | ||
| M9 | 381 | Desmethyl + lactam | N.D. | N.D. | N.D. | 2.27 | ||
| Totals |
|
| 95.2 | 68.4 | ||||