Drug intelligence / Profile preview

donepezil + intepirdine

Development stage
Discontinued
Lead developer
Sio Gene Therapies
Modality
Small Molecules
Administration
Oral
01

Overview

Donepezil + intepirdine is an investigational oral combination therapy developed for the treatment of Alzheimer's disease. Donepezil is a cholinesterase inhibitor that works by reversibly inhibiting acetylcholinesterase, thereby increasing acetylcholine levels in the brain and improving cognitive function in Alzheimer's patients[6][8][10]. Intepirdine (RVT-101) is a selective 5-hydroxytryptamine 6 (5-HT6) receptor antagonist designed to enhance neurotransmitter release and further improve cognition when added to standard donepezil therapy[3][5]. The rationale behind this combination was that targeting both cholinergic and serotonergic pathways could provide additive or synergistic benefits in slowing cognitive decline. However, large phase III clinical trials failed to demonstrate significant improvement over donepezil alone in patients with mild-to-moderate Alzheimer’s disease[2][4][7].

Other names
donepezil + intepirdineAricept + intepirdine
02

Targets

AcetylcholinesteraseHTR6 (5-hydroxytryptamine receptor 6)SIGMAR1 (Sigma non-opioid intracellular receptor 1)

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