Drug intelligence / Profile preview

VAV-8

Development stage
Preclinical
Modality
Small Molecules
01

Overview

VAV-8 is a novel 4-N-substituted-2-phenylquinazoline derivative designed as a multi-target directed ligand (MTDL) for the treatment of Alzheimer's disease. It functions through the dual inhibition of Acetylcholinesterase (AChE) and Monoamine oxidase B (MAO-B) enzymes, and also exhibits moderate inhibition of Amyloid-beta 42 (Aβ42) aggregation. Additionally, VAV-8 demonstrates moderate reactive oxygen species (ROS) inhibition and neuroprotective potential. The compound has shown good thermodynamic stability at enzyme binding pockets and is permeable to the blood-brain barrier. In preclinical in vivo studies using a zebrafish model, VAV-8 was effective in reducing scopolamine-induced cognitive deterioration, neurodegeneration, and oxidative stress.

02

Targets

AcetylcholinesteraseAβ (Amyloid-beta peptides and aggregates)MAOB (Monoamine oxidase B)

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