Abstract
AbstractBackgroundSpleen tyrosine kinase (Syk) is a cytosolic pro‐inflammatory signalling kinase that is associated with several neuroinflammatory conditions, including Alzheimer’s disease. We have developed structurally novel QED‐701, a brain‐penetrant, small molecule inhibitor of Syk that possesses excellent pharmacokinetic properties and displays anti‐inflammatory efficacy in vivo.MethodQED‐701 was administered to 5xFAD mice for 4‐months, beginning at 8‐weeks of age. At termination, the pro‐inflammatory profile in the brain was assessed by qPCR and histology was performed for amyloid, neuron health and microglial activation.ResultQED‐701 significantly reduced inflammation in the brain of 5xFAD mice, in a dose‐dependent manner that correlates to Syk inhibition in the CNS.ConclusionQED‐701 is a preclinical candidate for the treatment of Alzheimer’s disease and other neuroinflammatory conditions. It is a potent and selective inhibitor of Syk that readily enters the brain and displays anti‐inflammatory efficacy in the 5xFAD model of Alzheimer’s disease.
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