Quantitative profile of metabolites observed in medium after incubation of [14C]faldaprevir (5 μM) with human HepatoPac for 96 hours and comparison with in vivo metabolite profile of fecal samples from the human [14C] ADME study
| Metabolic Profile | Medium Samples from HepatoPac Incubation | Fecal Samples from Human [14C] ADME Study | ||
|---|---|---|---|---|
| % of Total Analytes (Including Faldaprevir) | % of Total Metabolitesa | % of Total Analytes (Including Faldaprevir)b | % of Total Metabolites | |
| Faldaprevir | 76.7 | – | 51.9 | – |
| M2a | 4.86 | 21 | 22.4 | 46 |
| M2b | 10.4 | 45 | 20.2 | 42 |
| Faldaprevir glucuronide | 2.20 | 9.4 | – | – |
| M3 | 1.37 | 5.9 | 1.7c | 3.5 |
| M12 | 2.41 | 10.3 | 0.7 | 1.4 |
| M14 | 2.07 | 8.9 | 1.3 | 2.7 |
| Other metabolites | – | – | 2.0d | 4.1 |
| Total | 100 | – | 100 | – |
–Not applicable or could not be calculated because analyte was not observed.
↵a Calculated by dividing the metabolite level by the sum of the total metabolites observed.
↵b Chen et al., 2014.
↵c M3 and another in vivo metabolite, M13, coeluted.
↵d M11 + other low-level metabolites that were not assigned a structure.