Drug intelligence / Profile preview

donepezil + roflumilast

Development stage
Phase 1
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Oral
01

Overview

A combination therapy consisting of donepezil, a cholinesterase inhibitor, and roflumilast, a phosphodiesterase-4 (PDE4) inhibitor. This combination is being investigated for its potential to enhance cognitive function and reverse cognitive deficits, particularly in Alzheimer's disease. Donepezil works by inhibiting the acetylcholinesterase enzyme, thereby increasing acetylcholine levels in the brain, while roflumilast prevents the breakdown of cyclic adenosine monophosphate (cAMP), affecting cell signaling and protein phosphorylation. Studies suggest that combining sub-efficacious doses of roflumilast and donepezil may be fully effective in improving spatial memory.

02

Targets

AcetylcholinesterasePDE4 (Phosphodiesterase 4A1)

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