Table 3.
Mean radioactivity contributions of [14C]-trofinetide and metabolites in humans after oral administration (0 to 12 h [plasma and blood] or 0 to 48 h [urine and feces])
| Compound | Modification | Plasma | Blood | Urine (80.1% of dose) | Feces (14.8% of dose) | Total urine + feces (94.9% of dose) |
|---|---|---|---|---|---|---|
| %AUC0–12 | %AUC0–12 | %Dose | %Dose | %Dose | ||
| Trofinetide | None (parent) | 93.1 | 88.4 | 73.3 | 7.80 | 81.1 |
| M129/1 | Double hydrolysis | ND | ND | ND | 0.84 | 0.84 |
| M186/1 | Hydrolysis | 1.61 | 1.25 | 1.43 | 2.41 | 3.84 |
| M168/1 | Hydrolysis + intramolecular cyclization | 2.24 | 0.42 | 1.17 | 0.59 | 1.76 |
| Total | 97.0 | 90.1 | 75.9 | 11.6 | 87.5 | |
%AUC0–12 percentage of total radioactivity in the area under the radioactivity-time from 0 to 12 h; %Dose percentage of the administered dose; ND not detected