A randomized study of H3 antagonist ABT-288 in mild-to-moderate Alzheimer's dementia

J Alzheimers Dis. 2014;42(3):959-71. doi: 10.3233/JAD-140291.

Abstract

Background: ABT-288, a highly selective histamine-3 receptor antagonist, demonstrated efficacy across several preclinical cognitive domains, and safety in healthy subjects and elderly volunteers.

Objective: Evaluate the efficacy and safety of ABT-288 in subjects with mild-to-moderate Alzheimer's dementia.

Methods: The study used a randomized, double-blind, placebo- and active-controlled, parallel group design with pre-defined futility criteria to permit early study termination. A total of 242 subjects were randomized in an equal ratio to ABT-288 1 mg or 3 mg, donepezil 10 mg, or placebo once daily for 12 weeks. The primary efficacy endpoint was the change from baseline to final evaluation on the 13-item Alzheimer's Disease Assessment Scale-cognitive subscale (ADAS-Cog) total score.

Results: The study was prematurely terminated because futility criteria were met. Point estimates on the ADAS-Cog scores for both ABT-288 dose groups were numerically inferior to placebo but no statistical differences were detected. Donepezil demonstrated statistically significant improvement. Adverse events were generally mild and self-limiting.

Conclusion: ABT-288 did not demonstrate efficacy in the symptomatic treatment of Alzheimer's dementia.

Keywords: ABT-288; Alzheimer's dementia; H3 antagonists; cognition; drug therapy; humans.

Publication types

  • Clinical Trial, Phase II
  • Randomized Controlled Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aged
  • Aged, 80 and over
  • Alzheimer Disease / drug therapy*
  • Analysis of Variance
  • Donepezil
  • Dose-Response Relationship, Drug
  • Double-Blind Method
  • Female
  • Follow-Up Studies
  • Histamine H3 Antagonists / pharmacokinetics
  • Histamine H3 Antagonists / therapeutic use*
  • Humans
  • Indans / therapeutic use
  • Male
  • Middle Aged
  • Nootropic Agents / therapeutic use
  • Piperidines / therapeutic use
  • Psychiatric Status Rating Scales
  • Pyridazines / pharmacokinetics
  • Pyridazines / therapeutic use*
  • Pyrroles / pharmacokinetics
  • Pyrroles / therapeutic use*
  • Treatment Outcome

Substances

  • 2-(4'-(5-methylhexahydropyrrolo(3,4-b)pyrrol-1-yl)biphenyl-4-yl)-2H-pyridazin-3-one
  • Histamine H3 Antagonists
  • Indans
  • Nootropic Agents
  • Piperidines
  • Pyridazines
  • Pyrroles
  • Donepezil