Table 8.
Urinary drug clearance (CLr) and recovery of ALZ-801, tramiprosate, and NRM5074 following oral administration of ALZ-801 tablet (day 1, 265 mg once daily; days 2–6, 265 mg twice daily; and day 7, 265 mg once daily) in healthy human subjects (i.e. Cohort D of Study 2 in Table 1; n = 9)
| Time | Analytes | CLr (mL/min) | Plasma AUC24 (ng/mL h) | Mean Ae (mg) |
|---|---|---|---|---|
| Day 1 | ALZ-801 | 36.4 ± 10.7 | 10,300 ± 2830 | 22.5 |
| Tramiprosate | 201 ± 48.2 | 3650 ± 670 | 44.0 | |
| NRM5074 | 652 ± 161 | 1810 ± 348 | 70.8 | |
| Total recovery in urine | 137.3 | |||
| Day 7 | ALZ-801 | 35.9 ± 19.9 | 11,200 ± 1970 | 24.1 |
| Tramiprosate | 194 ± 85.1 | 5020 ± 859 | 58.4 | |
| NRM5074 | 575 ± 218 | 5470 ± 1030 | 188.7 | |
| Total recovery in urine | 271.3 | |||
Calculations were based on 24-h urine collections on days 1 and 7
CLr renal clearance, AUC 24 area under the concentration–time curve from time zero to 24 h, Ae amount of unchanged drug excreted into urine