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AWZ1066S, a highly specific anti- drug candidate for a short-course treatment of filariasis.

Abstract

Onchocerciasis and lymphatic filariasis are two neglected tropical diseases that together affect ∼157 million people and inflict severe disability. Both diseases are caused by parasitic filarial nematodes with elimination efforts constrained by the lack of a safe drug that can kill the adult filaria (macrofilaricide). Previous proof-of-concept human trials have demonstrated that depleting >90% of the essential nematode endosymbiont bacterium, , using antibiotics, can lead to permanent sterilization of adult female parasites and a safe macrofilaricidal outcome. AWZ1066S is a highly specific anti- candidate selected through a lead optimization program focused on balancing efficacy, safety and drug metabolism/pharmacokinetic (DMPK) features of a thienopyrimidine/quinazoline scaffold derived from phenotypic screening. AWZ1066S shows superior efficacy to existing anti- therapies in validated preclinical models of infection and has DMPK characteristics that are compatible with a short therapeutic regimen of 7 days or less. This candidate molecule is well-positioned for onward development and has the potential to make a significant impact on communities affected by filariasis.

More information

Type
Journal Article
Author
Hong DW
Benayoud F
Nixon GL
Ford L
Johnston KL
Clare R
Cassidy A
Cook D
Siu A
Shiotani M
Webborn PJ H
Kavanagh S
Aljayyoussi G
Murphy E
Steven A
Archer J
Struever D
Frohberger S
Ehrens A
Hübner M
Hoerauf A
Roberts AP
Hubbard AT M
Tate E
Serwa RA
Leung SC
Qie L
Berry N
Gusovsky F
Hemingway J
Turner J
Taylor M
Ward S
O'Neill PM