Table 3.
Navoximod and its abundant metabolites in human plasma, urine, and feces after a single oral administration of 200 mg/600 μCi [14C]‐navoximod to healthy subjects
| Analyte | Biotransformation | Plasma | Urine | Feces | Total | |
|---|---|---|---|---|---|---|
| % of TRA | AUC0–48‐h (μM/h)a | % of doseb | % of doseb | % of doseb | ||
| Navoximod | Unchanged parent | 7.00 | 4.40 | 1.66 | 3.79 | 5.45 |
| M1 (thiocyanate) | Ring cleavage | 5.54 | 3.54 | 0.614 | 0.138 | 0.752 |
| M17 | Oxidation (+ 34 Da) | D | D | 1.78 | 1.54 | 3.32 |
| M19 | Glucuronidation | 3.14 | 2.36 | 8.74 | ND | 8.74 |
| M28 | Glucuronidation | 57.5 | 36.4 | 59.7 | ND | 59.7 |
| M31 | Oxidation (+16 Da) | D | D | 1.71 | D | 1.71 |
| M38 | Glucuronidation | D | D | 1.76 | ND | 1.76 |
D, only detected by mass spectrometry; ND, not detected; TRA, total radioactivity.
a
Mean values from AUC 0–48 hour of pooled plasma (n = 8) adjusted with extraction recovery. The unextracted radioactivity accounted for 20.4% of the total radioactivity in the plasma sample.
b
Mean values from eight subjects.