Peak | Compound/Metabolite | AUC0–120 h | % of Total [14C] |
---|---|---|---|
M3 | Glucuronide of M5 | 1850 ± 268 | 18.4 ± 5.11 |
M5 | Formed by hydroxylation | 156 ± 29.0 | 1.51 ± 0.34 |
M6 | Formed by hydroxylation | 170 ± 39.9 | 1.63 ± 0.33 |
M7 | Formed by hydroxylation | 282 ± 87.8 | 2.75 ± 1.11 |
P29.6 | Unknown | 378 ± 103 | 3.72 ± 1.49 |
P30.5 | Unknown | 192 ± 57.4 | 1.82 ± 0.47 |
P73.0 | Formed during sample processing | 190 ± 91.7 | 1.74 ± 0.62 |
Siponimod | Parent drug | 6320 ± 2920 | 57.1 ± 5.91a |
Sum of unknown trace metabolites | 204 ± 29.8 | 2.02 ± 0.59 | |
Lost during sample processing and HPLCb | 1040 ± 578 | 9.30 ± 2.10 | |
Total [14C]c | 10800 ± 3700 | 100 ± (NC) |
AUC0–120 h, area under the concentration-time curve from 0 to 120 h; NC, not calculable, not meaningful.
↵a Here, 58.8%, including P73 formed by methyl-esterification of parent drug during sample preparation.
↵b This might be due to the formation of metabolite M17, which has a long half-life.
↵c Total of radiolabeled components.