The GSM BPN-15606 as a Potential Candidate for Preventative Therapy in Alzheimer's Disease

J Alzheimers Dis. 2020;73(4):1541-1554. doi: 10.3233/JAD-190442.

Abstract

Background: In the amyloid hypothesis of Alzheimer's disease (AD), the dysregulation of amyloid-β protein (Aβ) production and clearance leads to amyloid deposits, tau tangles, neuronal loss, and cognitive dysfunction. Thus far, therapies targeting the enzymes responsible for Aβ production have been found ineffective or having significant side effects.

Objective: To test whether a γ-secretase modulator, BPN-15606, is an effective disease-modifying or preventative treatment in the PSAPP mouse model of AD.

Methods: We treated pre-plaque (3-month-old) and post-plaque (6-month-old) PSAPP AD transgenic mice for 3 months and examined behavioral, biochemical, and pathological end points.

Results: BPN-15606 attenuated cognitive impairment and reduced amyloid plaque load, microgliosis, and astrogliosis associated with the AD phenotype of PSAPP mice when administered to pre-plaque (3-month-old) but was ineffective when administered to post-plaque (6-month-old) mice. No treatment-related toxicity was observed.

Conclusion: BPN-15606 appears efficacious when administered prior to significant pathology.

Keywords: Alzheimer’s disease; BPN-15606; PSAPP; amyloid-β; cognitive deficits; preventative therapy; γ-secretase modulator.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alzheimer Disease / prevention & control*
  • Alzheimer Disease / psychology
  • Amyloid Precursor Protein Secretases / antagonists & inhibitors*
  • Amyloid beta-Protein Precursor / genetics
  • Animals
  • Behavior, Animal / drug effects
  • Cognitive Dysfunction / prevention & control
  • Cognitive Dysfunction / psychology
  • Gliosis
  • Humans
  • Maze Learning / drug effects
  • Memory / drug effects
  • Mice
  • Mice, Transgenic
  • Motor Activity / drug effects
  • Phenethylamines / adverse effects
  • Phenethylamines / therapeutic use*
  • Plaque, Amyloid / genetics
  • Plaque, Amyloid / prevention & control
  • Postural Balance / drug effects
  • Psychomotor Performance / drug effects
  • Pyridazines / adverse effects
  • Pyridazines / therapeutic use*

Substances

  • APP protein, human
  • Amyloid beta-Protein Precursor
  • BPN-15606
  • Phenethylamines
  • Pyridazines
  • Amyloid Precursor Protein Secretases