Phase 1 Program of ALZ-801, a Novel Prodrug of Tramiprosate with Improved Tolerability, Supports Bridging to Upcoming Phase 3 Program

Presented at the 9^th annual Clinical Trials on Alzheimer’s Disease (CTAD) conference,
held in San Diego, California

Introduction

ALZ-801 is a novel, orally bioavailable, small molecule prodrug of tramiprosate with substantially improved pharmaceutical properties. Tramiprosate, the active moiety released after administration of ALZ-801, is a β-amyloid (Aβ) anti-aggregation agent that inhibits the formation of Aβ oligomers and prevents neurotoxicity. A Phase 1 program for ALZ-801 was conducted to bridge to the extensive Phase 3 clinical safety and efficacy database of tramiprosate in Alzheimer’s disease (AD), with the objective of assessing the safety and tolerability of ALZ-801 at plasma concentrations that match the 150 mg BID dose of tramiprosate tested previously in Mild to Moderate AD patients. The Phase I program, comprising of approximately 170 subjects, evaluated the single and multiple ascending dose (14-day) safety and tolerability of ALZ-801, when administered with or without food. These bridging studies were conducted using two solid dose formulations: a loose- filled capsule and an immediate release tablet. The results demonstrate favorable safety and tolerability of ALZ-801 administered as a loose-filled capsule or tablet with marked improvements in pharmacokinetics (PK) and safety profile over oral tramiprosate.