Table 1.
Overview of the completed ALZ-801 phase I clinical program
| Study | Design | Treatments | Subjects | Objectives |
|---|---|---|---|---|
| Study 1: ALZ-801 SAD |
Double-blind, placebo-controlled, single ascending dose (14-day washout) | Substudy 1: Two-way crossover study to compare ALZ-801 (100 mg in a loose-filled capsule) and tramiprosate (equimolar dose of 58 mg in a loose-filled capsule) | 8 healthy adult males and 8 healthy elderly males/females | Safety, tolerability, and PK of single doses |
| Substudy 2: Designed to evaluate up to four doses of ALZ-801 loose-filled capsule in four sequential groups (only 300 mg was conducted) | 15 healthy elderly males/females | |||
| Substudy 3: Double-dummy, parallel study to compare ALZ-801 (172 mg in a loose-filled capsule) and tramiprosate (equimolar dose of 100 mg in a capsule or modified-release tablet) | 36 healthy elderly males/females randomized to each treatment in a 1:1:1 fashion | |||
| Study 2: ALZ-801 MAD |
Double-blind, placebo-controlled, multiple ascending dose |
Cohort A: Days 1–7: 171 mg ALZ-801 loose capsule or placebo once daily on day 1 and twice daily on days 2–7 Days 8–14: 256.5 mg ALZ-801 or placebo once daily; fasted |
9 healthy males/females received the drug; 3 healthy males/females received placebo |
Safety, tolerability, and PK of multiple doses |
|
Cohort B: Days 1–7: 256.5 mg ALZ-801 loose capsule or placebo once daily on day 1 and twice daily on days 2–7 Days 8–14: 340 mg ALZ-801 or placebo once daily; fasted |
9 healthy males/females received the drug; 3 healthy males/females received placebo |
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|
Cohort C: Days 1–7: 256.5 mg ALZ-801 loose capsule or placebo once daily on day 1 and twice daily on days 2–7 Days 8–14: 340 mg ALZ-801 or placebo once daily; fed |
9 healthy males/females received the drug; 3 healthy males/females received placebo |
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|
Cohort D: Days 1–6: 265 mg ALZ-801 tablet or placebo once daily on day 1 and twice daily on days 2–6 Day 7: 265 mg ALZ-801 tablet or placebo once daily; fed |
9 healthy males/females received the drug; 3 healthy males/females received placebo |
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| Study 3: ALZ-801 tablet PK and food effect | Open label, four-period, sequential, single ascending dose (14-day washout) | ALZ-801 tablet, single dose: (a) 171 mg, fasted (b) 205 mg, fasted (c) 205 mg, fed (d) 342 mg, fed |
12 healthy adult and elderly, male and female subjects | Safety, tolerability, and PK of immediate-release tablet; food effect |
SAD single ascending dose, MAD multiple ascending dose, PK pharmacokinetics