BibTex format
@article{Hong:2019:10.1073/pnas.1816585116,
author = {Hong, WD and Benayoud, F and Nixon, GL and Ford, L and Johnston, KL and Clare, RH and Cassidy, A and Cook, DAN and Siu, A and Shiotani, M and Webborn, PJH and Kavanagh, S and Aljayyoussi, G and Murphy, E and Steven, A and Archer, J and Struever, D and Frohberger, SJ and Ehrens, A and Huebner, MP and Hoerauf, A and Roberts, AP and Hubbard, ATM and Tate, EW and Serwa, RA and Leung, SC and Qie, L and Berry, NG and Gusovsky, F and Hemingway, J and Turner, JD and Taylor, MJ and Ward, SA and O'Neill, PM},
doi = {10.1073/pnas.1816585116},
journal = {Proceedings of the National Academy of Sciences of the United States of America},
pages = {1414--1419},
title = {AWZ1066S, a highly specific anti-Wolbachia drug candidate for a short-course treatment of filariasis},
url = {http://dx.doi.org/10.1073/pnas.1816585116},
volume = {116},
year = {2019}
}
RIS format (EndNote, RefMan)
TY - JOUR
AB - 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, Wolbachia, using antibiotics, can lead to permanent sterilization of adult female parasites and a safe macrofilaricidal outcome. AWZ1066S is a highly specific anti-Wolbachia 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-Wolbachia 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.
AU - Hong,WD
AU - Benayoud,F
AU - Nixon,GL
AU - Ford,L
AU - Johnston,KL
AU - Clare,RH
AU - Cassidy,A
AU - Cook,DAN
AU - Siu,A
AU - Shiotani,M
AU - Webborn,PJH
AU - Kavanagh,S
AU - Aljayyoussi,G
AU - Murphy,E
AU - Steven,A
AU - Archer,J
AU - Struever,D
AU - Frohberger,SJ
AU - Ehrens,A
AU - Huebner,MP
AU - Hoerauf,A
AU - Roberts,AP
AU - Hubbard,ATM
AU - Tate,EW
AU - Serwa,RA
AU - Leung,SC
AU - Qie,L
AU - Berry,NG
AU - Gusovsky,F
AU - Hemingway,J
AU - Turner,JD
AU - Taylor,MJ
AU - Ward,SA
AU - O'Neill,PM
DO - 10.1073/pnas.1816585116
EP - 1419
PY - 2019///
SN - 0027-8424
SP - 1414
TI - AWZ1066S, a highly specific anti-Wolbachia drug candidate for a short-course treatment of filariasis
T2 - Proceedings of the National Academy of Sciences of the United States of America
UR - http://dx.doi.org/10.1073/pnas.1816585116
UR - http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcApp=PARTNER_APP&SrcAuth=LinksAMR&KeyUT=WOS:000456336100049&DestLinkType=FullRecord&DestApp=ALL_WOS&UsrCustomerID=1ba7043ffcc86c417c072aa74d649202
UR - http://hdl.handle.net/10044/1/67498
VL - 116
ER -