Drug intelligence / Profile preview

begacestat + donepezil

Development stage
Unknown
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

Begacestat + donepezil is an experimental combination of two small-molecule drugs studied in early-stage clinical trials, primarily for their potential in neurological disorders. Begacestat is a gamma-secretase inhibitor that reduces the formation of amyloid-beta peptides, which are implicated in the pathogenesis of Alzheimer's disease. Donepezil is a cholinesterase inhibitor approved for the symptomatic treatment of Alzheimer's disease; it works by preventing the breakdown of acetylcholine, thereby enhancing cholinergic neurotransmission in the brain. The co-administration of these agents aims to address both amyloid plaque accumulation (a disease-modifying approach via begacestat) and symptomatic cognitive impairment (via donepezil). Trials have focused primarily on safety, tolerability, and pharmacodynamic interactions in healthy subjects and the potential for combined use in Alzheimer’s disease[2][5]. There is no evidence that this combination is approved or marketed.

02

Targets

GSEC (Gamma-Secretase Complex)CTSB (Cathepsin B)Acetylcholinesterase

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