In vitro activity: Azeliragon (also known as TTP488 and PF-04494700) is a potent and orally bioactive RAGE (Receptor for Advanced Glycation End products) inhibitor that has the potential for the treatment of mild-to-moderate Alzheimer's disease and cerebral amyloid angiopathy. RAGE is a pattern recognition receptor that affects the movement of amyloid (a biomarker for Alzheimer's disease) into the brain. In preclinical studies, azeliragon decreased brain amyloid in mice and improved their performance on behavior tests. Azeliragon has been shown to be involved in adaptive immune responses. It is currently in Phase 3 clinical trial.

Cell Assay: Azeliragon is an orally active, centrally acting antagonist of RAGE-RAGE ligand interaction. Chronic oral dosing of Azeliragon in AD transgenic mice led to a reduction of amyloid load in the brain, improves performance on behavioral testing and normalization of electrophysiological recordings from hippocampal slices.