@article{32789,
  keywords = {Neglected tropical diseases (NTDs), Lymphatic filariasis (LF), Anti-Wolbachia, Drug Discovery, macrofilaricide, onchocerciasis},
  author = {Hong DW and Benayoud F and Nixon GL and Ford L and Johnston KL and Clare R and Cassidy A and Cook D and Siu A and Shiotani M and Webborn PJ H and Kavanagh S and Aljayyoussi G and Murphy E and Steven A and Archer J and Struever D and Frohberger S and Ehrens A and Hübner M and Hoerauf A and Roberts AP and Hubbard AT M and Tate E and Serwa RA and Leung SC and Qie L and Berry N and Gusovsky F and Hemingway J and Turner J and Taylor M and Ward S and O'Neill PM},
  title = {AWZ1066S, a highly specific anti- drug candidate for a short-course treatment of filariasis.},
  abstract = {<p>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 &gt;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.</p>
},
  year = {2019},
  journal = {Proceedings of the National Academy of Sciences of the United States of America},
  issn = {1091-6490},
  url = {https://www.pnas.org/content/pnas/early/2019/01/02/1816585116.full.pdf},
  doi = {10.1073/pnas.1816585116},
  language = {eng},
}