Table 2.
Overview of the zotarolimus metabolites that were identified. Please see the Supplementary Materials for more detail. Four distinct hydroxy piperidine metabolites were detected. These were chromatographically separated indicating hydroxylation at different positions of the piperidine ring. However, since no fragments of the piperidine ring were detected, the exact hydroxylation positions could not be identified.
| Desmethyl Metabolites | Exact Mass | |
|---|---|---|
| 1 | 16-O-Desmethyl Zotarolimus | 974.54609 |
| 2 | 27-O-Desmethyl Zotarolimus | |
| 3 | 39-O-Desmethyl Zotarolimus | |
| Di-Desmethyl Metabolites | ||
| 4 | 16, 39-O-Didesmethyl Zotarolimus | 960.53044 |
| 5 | 27, 39-O-Didesmethyl Zotarolimus | |
| 6 | 16, 27-O-Didesmethyl Zotarolimus | |
| Hydroxy Metabolites | ||
| 7 | 45 and 46-Hydroxy Zotarolimus | 1004.55666 |
| 8 | 24-Hydroxy Zotarolimus | |
| 9 | 11-Hydroxy Zotarolimus | |
| 10 | 12-HydroxyZotarolimus | |
| 11 | 25-Hydroxy Zotarolimus | |
| 12 | 3/4/5/6 Hydroxy-piperidine Zotarolimus | |
| 13 | 23-Hydroxy Zotarolimus | |
| 14 | 14-Hydroxy Zotarolimus | |
| 15 | 49-Hydroxy Zotarolimus | |
| Hydroxy, Desmethyl Metabolites | ||
| 16 | 23/24-hydroxy, 16-O-desmethyl Zotarolimus | 990.54101 |
| 17 | 23/24-hydroxy, 39-O-desmethyl Zotarolimus | |
| 18 | 25-hydroxy, 39-O-desmethyl Zotarolimus | |
| 19 | 11-hydroxy, 39-O-desmethyl Zotarolimus | |
| 20 | Hydroxy-piperidine, 39-O-desmethyl Zotarolimus | |
| 21 | 45/46-hydroxy, 27-O-desmethyl Zotarolimus | |
| Di-Hydroxy Metabolites | ||
| 22 | 11,24-Dihydroxy Zotarolimus | 1020.55157 |
| 23 | 12,24-Dihydroxy Zotarolimus | |
| 24 | 11,47/48-Dihydroxy Zotarolimus |