Drug intelligence / Profile preview

awz1066s

Development stage
Discontinued
Lead developer
Liverpool School of Tropical Medicine
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules
Administration
Oral
01

Overview

AWZ1066S is a first-in-class, orally bioavailable small molecule drug candidate developed as a highly specific anti-Wolbachia agent. It is based on an azaquinazoline (thienopyrimidine/quinazoline) scaffold and was selected through lead optimization for its superior efficacy, safety, and pharmacokinetic properties. AWZ1066S targets the endosymbiotic bacterium *Wolbachia* within filarial nematodes, leading to depletion of *Wolbachia* populations in the worms. This results in permanent sterilization of adult female parasites and ultimately macrofilaricidal activity—killing adult worms responsible for diseases such as lymphatic filariasis and onchocerciasis. In preclinical models, short-course oral regimens (as brief as 5–7 days) achieved >90% depletion of *Wolbachia* with sustained sterilization effects. The drug has advanced to Phase 1 clinical trials to assess safety and pharmacokinetics in healthy volunteers. Developed by: Liverpool School of Tropical Medicine Primary Indications: Lymphatic filariasis, Onchocerciasis

Other names
anti-Wolbachia agent AWZ1066S
02

Targets

LeuRS (Leucyl-tRNA synthetase)

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