Drug intelligence / Profile preview

eptastigmine

Development stage
Discontinued
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Oral, Intranasal
01

Overview

Eptastigmine (NXX-066) is a long-acting, carbamate-based acetylcholinesterase (AChE) inhibitor and a derivative of physostigmine. It was developed as a potential treatment for Alzheimer's disease to address the cholinergic deficit characteristic of the condition. Unlike physostigmine, which has a short half-life, eptastigmine was designed to provide more sustained enzyme inhibition. It was investigated in clinical trials by companies including Zeneca (as NXX-066) and Merck (as L-693,487). However, its development was terminated during Phase III clinical trials due to the occurrence of severe adverse effects, specifically hematological toxicity including leukopenia and agranulocytosis.

Other names
heptyl-physostigmineheptylphysostigmineheptyl physostigmine
02

Targets

Acetylcholinesterase

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