Sulfopropanoic acid derivatives for treating neurodegenerative disorders: a patent spotlight.

The patent introduces a class of agents that target amyloid aggregation, and subsequently, reduce amyloid β-oligomer neurotoxicity. The class encompasses sulfopropanoic acid derivatives and is represented by tramiprosate and its prodrug ALZ-801 (valiltramiprosate). Clinical trials showed that ALZ-801 oral tablet is well tolerated and showed superior pharmacokinetic properties in healthy volunteers and Alzheimer's disease (AD) patients. Results from phase II & III trials of ALZ-801 in early AD have provided evidence of efficacy and to adjudicate the role of amyloid β-oligomers in AD pathogenesis. The confirmatory APOLLOE4 phase III trial of ALZ-801 in APOE4/4 homozygotes with early AD has been initiated. If ALZ-801 is approved, it will be among the first oral disease-modifying drugs for AD.