azeliragon

Ligand id: 8317

Name: azeliragon

Structure and Physico-chemical Properties

2D Structure
Calculated Physico-chemical Properties
Hydrogen bond acceptors 3
Hydrogen bond donors 0
Rotatable bonds 14
Topological polar surface area 39.52
Molecular weight 531.27
XLogP 9.44
No. Lipinski's rules broken 2

Molecular properties generated using the CDK

No information available.
Summary of Clinical Use
Azeliragon is being assessed in Phase III clinical trial as a potential treatment for mild Alzheimer's disease (AD). The US FDA has granted azeliragon fast track designation, to expedite its route to approval, based on positive clinical outcomes from a Phase II trial [1].
Mechanism Of Action and Pharmacodynamic Effects
Amyloid β (Aβ) uptake into the brain is dependent on RAGE [2]. Prolonged Aβ interaction with RAGE causes a chronic inflammation which is a crucial driver of amyloid plaque formation and chronic neuronal dysfunction. Thus RAGE is intimately linked to the pathogenesis of AD. Azeliragon antagonises the Aβ interaction with RAGE and is predicted to reduce Aβ accumulation in the brain, and has the potential to delay the formation of Aβ plaques.