Efficacy and safety evaluation of HSD-1 inhibitor ABT-384 in Alzheimer's disease

Alzheimers Dement. 2014 Oct;10(5 Suppl):S364-73. doi: 10.1016/j.jalz.2013.09.010. Epub 2014 Jan 10.

Abstract

Background: In this study we assessed increased cortisol in Alzheimer's disease (AD) patients. The selective 11-β-hydroxysteroid dehydrogenase type 1 (HSD-1) inhibitor ABT-384 blocked regeneration of active cortisol and this tests the hypothesis that intracellular hypercortisolism contributes to cognitive impairment.

Methods: In this double-blind, placebo- and active-controlled phase II study we examine the efficacy and safety of ABT-384 given 10 mg or 50 mg once daily, donepezil 10 mg once daily, or placebo for 12 weeks in subjects with mild-to-moderate AD. The primary efficacy end point 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 terminated for futility after randomization of 267 subjects. ABT-384 did not improve ADAS-Cog scores or any secondary end point; however, donepezil significantly improved both cognition and functional end points. Overall incidence of adverse events was similar among treatment groups.

Conclusion: ABT-384, when tested at doses associated with complete brain HSD-1 inhibition, did not produce symptomatic improvement in AD.

Trial registration: ClinicalTrials.gov NCT01137526.

Keywords: 11-β-hydroxysteroid dehydrogenase; Alzheimer's disease; Clinical trial; Cognition; Cortisol; Dementia; Donepezil; Enzyme inhibitor; Glucocorticoids; Hypothalamic–pituitary–adrenal axis.

Publication types

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

MeSH terms

  • Adamantane / adverse effects
  • Adamantane / analogs & derivatives*
  • Adamantane / therapeutic use
  • Aged
  • Alzheimer Disease / drug therapy*
  • Donepezil
  • Double-Blind Method
  • Female
  • Humans
  • Indans / adverse effects
  • Indans / therapeutic use
  • Male
  • Neuropsychological Tests
  • Nootropic Agents / adverse effects
  • Nootropic Agents / therapeutic use*
  • Piperazines / adverse effects
  • Piperazines / therapeutic use*
  • Piperidines / adverse effects
  • Piperidines / therapeutic use
  • Treatment Outcome

Substances

  • Indans
  • N-(5-(aminocarbonyl)tricyclo(3.3.1.13,7)dec-2-yl)-alpha,alpha-dimethyl-4-(5-(trifluoromethyl)-2-pyridinyl)-1-piperazineacetamide
  • Nootropic Agents
  • Piperazines
  • Piperidines
  • Donepezil
  • Adamantane

Associated data

  • ClinicalTrials.gov/NCT01137526