Table 6.
Steady-state T max, C max and AUC profiles for ALZ-801 (prodrug) and tramiprosate (active drug) after oral administration of ALZ-801 (capsule) over 14 days in fasted and fed healthy human subjects in the phase I multiple ascending dose study (i.e. Cohorts B and C of Study 2 in Table 1; n = 9 per group)
| Food status | Plasma analyte | Day | T max (h) | C max (ng/mL) | AUC12 (ng/mL h) | AUC24 (ng/mL h) |
|---|---|---|---|---|---|---|
| Fasted | ALZ-801 | 14 | 0.629 ± 0.229 | 10,400 ± 2880 | 13,800 ± 3350 | 13,800 ± 3350 |
| Tramiprosate | 14 | 1.634 ± 0.351 | 1480 ± 305 | 5470 ± 1220 | 6170 ± 1420 | |
| Fed | ALZ-801 | 14 | 0.944 ± 0.388 | 8830 ± 2660 | 13,800 ± 2220 | 13,800 ± 2220 |
| Tramiprosate | 14 | 1.778 ± 0.264 | 1180 ± 190 | 5230 ± 691 | 6300 ± 781 |
Dosing schedule: Days 1–7: 256.5 mg ALZ-801 capsule once daily on day 1 and twice daily on days 2–7; days 8–14: 340 mg ALZ-801 once daily
Data are expressed as mean ± SD
C max maximum concentration, T max time to reach Cmax, AUC area under the concentration–time curve, AUC 12 AUC from time zero to 12 h, AUC 24 AUC from time zero to 24 h, SD standard deviation