Table 4.
Summary of plasma PK profiles for ALZ-801 (prodrug) and tramiprosate (active drug) after single dose oral administration of 100, 172 and 300 mg of ALZ-801 (capsule) in healthy human subjects in the phase I single ascending dose study (i.e. Study 1 in Table 1)
| PK parameters | ALZ-801 100 mg (equivalent to tramiprosate 58 mg) | ALZ-801 172 mg (equivalent to tramiprosate 100 mg) | ALZ-801 300 mg (equivalent to tramiprosate 175 mg) |
|---|---|---|---|
| ALZ-801 | |||
| T max (h) | 0.51 [0.25–2.00] [16] | 0.63 [0.50–1.02] [12] | 0.75 [0.48– 1.03] [11] |
| C max (ng/mL) | 3646 ± 1445 [16] | 5445 ± 1669 [12] | 8149 ± 3607 [11] |
| AUCt (ng/mL h) | 3611 ± 684 [16] | 5891 ± 1185 [12] | 9606 ± 2683 [11] |
| t ½ (h) | 0.70 ± 0.11 [13] | 0.87 ± 0.20 [12] | 0.81 ± 0.13 [9] |
| Tramiprosate | |||
| T max(h) | 1.05 [0.75–3.02] [16] | 2.00 [1.00–2.00] [12] | 2.00 [1.00–2.08] [11] |
| C max (ng/mL) | 418 ± 94.2 [16] | 628 ± 100 [12] | 1079 ± 339 [11] |
| AUCt (ng/mL h) | 1595 ± 391 [16] | 2680 ± 448 [12] | 4736 ± 1291 [11] |
| t ½ (h) | 13.4 ± 7.64 [8] | 14.9 ± 3.97 [10] | 17.8 ± 2.11 [10] |
Data are expressed as mean ± SD (N), except for T max, which is reported as median [range] (N)
t ½: the elimination kinetics in some subjects could not be determined, thus the n is different for some of the PK parameters
PK pharmacokinetic, C max maximum concentration, T max time to reach Cmax, AUC t area under the concentration–time curve from time zero to time t, t ½ half-life, SD standard deviation