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PF-06751979

Development stage: Phase 1
Lead developer: Pfizer
Modality: Small Molecules
Administration: Oral

Overview

PF-06751979 is a potent, brain-penetrant small molecule inhibitor of β-site amyloid precursor protein cleaving enzyme 1 (BACE1), developed by Pfizer for the treatment of Alzheimer's disease. It was designed to achieve high selectivity for BACE1 over related aspartyl proteases such as Cathepsin D and BACE2, addressing safety concerns like hypopigmentation associated with nonselective BACE inhibition. Preclinical and clinical studies demonstrated excellent brain penetration and in vivo efficacy without evidence of depigmentation side effects seen in other BACE inhibitors. The drug advanced to Phase 1 clinical trials but development has since been discontinued[2][4][5][7][9].

Other names: compound 64compound64compound-64

Targets

BACE1 (Beta-site APP-cleaving enzyme 1)

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