Quantitation of INCB018424 and metabolites in pooled plasma for individual subjects after an oral dose of [14C]INCB018424
The identities of M7, M8, M9, M11, M16, M27, and M49 were confirmed by NMR. Other identified metabolites are putative based on retention time and mass spectra. Plasma samples were pooled equally by time point for the six subjects at predose and 1, 2, 6, 12, 24, and 36 h postdose. Metabolites not observed in a given subject were denoted as not detectable and assigned a value of 0 for calculations.
| Metabolite | %Radioactivity in Plasma for Subjects | ||||||
|---|---|---|---|---|---|---|---|
| 001 | 002 | 003 | 004 | 005 | 006 | Mean ± S.D. | |
| M7 (m/z 323) | N.D. | 7.8 | 3.8 | 6.0 | 3.7 | N.D. | 3.6 ± 3.1 |
| M8 (m/z 323) | N.D. | 3.7 | 8.5 | 6.3 | 4.2 | 5.8 | 4.8 ± 2.9 |
| M9 (m/z 321) | N.D. | N.D. | N.D. | 1.9 | 6.8 | 2.3 | 1.8 ± 2.7 |
| M11 (m/z 321) | 4.8 | N.D. | 5.4 | 5.9 | 4.6 | 6.8 | 4.6 ± 2.4 |
| M16/M27 (m/z 323)a | 11 | 12 | 4.4 | 6.0 | 5.0 | 8.5 | 7.7 ± 4.7 |
| M18 (m/z 323) | 16 | 17 | 12 | 7.7 | 11 | 8.0 | 12 ± 4.0 |
| M38 (m/z 339) | N.D. | N.D. | N.D. | 2.2 | N.D. | N.D. | 0.4 ± 0.9 |
| M49 (m/z 339) | 2.0 | 1.6 | 1.9 | 1.9 | 1.9 | 2.0 | 1.9 ± 0.2 |
| Parent (m/z 307) | 67 | 52 | 64 | 62 | 63 | 67 | 63 ± 5.5 |
N.D., not detectable.
↵a Coeluting stereoisomers.