Effects of Chronic Masitinib Treatment in APPswe/PSEN1dE9 Transgenic Mice Modeling Alzheimer's Disease

J Alzheimers Dis. 2020;76(4):1339-1345. doi: 10.3233/JAD-200466.

Abstract

Background: Masitinib is a selective tyrosine kinase inhibitor that modulates mast cells activity. A previous phase II study reported a cognitive effect of masitinib in patients with Alzheimer's disease.

Objective: We aimed to shed light on the mode of action of masitinib in Alzheimer's disease.

Methods/results: We demonstrated here that chronic oral treatment of APPswe/PSEN1dE9 transgenic mice modeling Alzheimer's disease restored normal spatial learning performance while having no impacts on amyloid-β loads nor on neuroinflammation. However, masitinib promoted a recovery of synaptic markers. Complete genetic depletion of mast cells in APPswe/PSEN1dE9 mice similarly rescued synaptic impairments.

Conclusion: These results underline that masitinib therapeutic efficacy might primarily be associated with a synapto-protective action in relation with mast cells inhibition.

Keywords: Alzheimer’s disease; cognition; drug evaluation; masitinib; mast cells; preclinical; synapses.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alzheimer Disease / drug therapy*
  • Alzheimer Disease / genetics
  • Amyloid beta-Peptides / pharmacology
  • Amyloid beta-Protein Precursor / genetics
  • Animals
  • Benzamides
  • Cognition / drug effects*
  • Disease Models, Animal
  • Male
  • Mice, Transgenic
  • Piperidines
  • Presenilin-1 / genetics
  • Presenilin-1 / pharmacology
  • Pyridines
  • Synapses / drug effects*
  • Thiazoles / administration & dosage
  • Thiazoles / pharmacology*

Substances

  • Amyloid beta-Peptides
  • Amyloid beta-Protein Precursor
  • Benzamides
  • Piperidines
  • Presenilin-1
  • Pyridines
  • Thiazoles
  • masitinib