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KAF156 is an antimalarial clinical candidate with potential for use in prophylaxis, treatment, and prevention of disease transmission

Kuhen, Kelli L., Chatterjee, Arnab K., Rottmann, Matthias, Gagaring, Kerstin, Borboa, Rachel, Buenviaje, Jennifer, Chen, Zhong, Francek, Carolyn, Wu, Tao, Nagle, Advait, Barnes, S. Whitney, Plouffe, David, Lee, Marcus C.S., Fidock, David A., Graumans, Wouter, van de Vegte-Bolmer, Marga, van Gemert, Geert J., Wirjanata, Grennady, Sebayang, Boni, Marfurt, Jutta, Russell, Bruce, Suwanarusk, Rossarin, Price, Ric N., Nosten, Francois, Tungtaeng, Anchalee, Gettayacamin, Montip, Sattabongkot, Jetsumon, Taylor, Jennifer, Walker, John R., Tully, David, Patra, Kailash P., Flannery, Erika L., Vinetz, Joseph M., Renia, Laurent, Sauerwein, Robert W., Winzeler, Elizabeth A., Glynne, Richard J. and Diagana, Thierry T. (2014). KAF156 is an antimalarial clinical candidate with potential for use in prophylaxis, treatment, and prevention of disease transmission. Antimicrobial Agents and Chemotherapy,58(9):5060-5067.

Document type: Journal Article
Citation counts: Altmetric Score Altmetric Score is 13
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IRMA ID 75039815xPUB304
Title KAF156 is an antimalarial clinical candidate with potential for use in prophylaxis, treatment, and prevention of disease transmission
Author Kuhen, Kelli L.
Chatterjee, Arnab K.
Rottmann, Matthias
Gagaring, Kerstin
Borboa, Rachel
Buenviaje, Jennifer
Chen, Zhong
Francek, Carolyn
Wu, Tao
Nagle, Advait
Barnes, S. Whitney
Plouffe, David
Lee, Marcus C.S.
Fidock, David A.
Graumans, Wouter
van de Vegte-Bolmer, Marga
van Gemert, Geert J.
Wirjanata, Grennady
Sebayang, Boni
Marfurt, Jutta
Russell, Bruce
Suwanarusk, Rossarin
Price, Ric N.
Nosten, Francois
Tungtaeng, Anchalee
Gettayacamin, Montip
Sattabongkot, Jetsumon
Taylor, Jennifer
Walker, John R.
Tully, David
Patra, Kailash P.
Flannery, Erika L.
Vinetz, Joseph M.
Renia, Laurent
Sauerwein, Robert W.
Winzeler, Elizabeth A.
Glynne, Richard J.
Diagana, Thierry T.
Journal Name Antimicrobial Agents and Chemotherapy
Publication Date 2014
Volume Number 58
Issue Number 9
ISSN 0066-4804   (check CDU catalogue  open catalogue search in new window)
Scopus ID 2-s2.0-84906079854
Start Page 5060
End Page 5067
Total Pages 8
Place of Publication Washington, United States of America
Publisher American Society for Microbiology
HERDC Category C1 - Journal Article (DIISR)
Abstract Renewed global efforts toward malaria eradication have highlighted the need for novel antimalarial agents with activity against multiple stages of the parasite life cycle. We have previously reported the discovery of a novel class of antimalarial compounds in the imidazolopiperazine series that have activity in the prevention and treatment of blood stage infection in a mouse model of malaria. Consistent with the previously reported activity profile of this series, the clinical candidate KAF156 shows blood schizonticidal activity with 50% inhibitory concentrations of 6 to 17.4 nM against P. falciparum drug-sensitive and drug-resistant strains, as well as potent therapeutic activity in a mouse models of malaria with 50, 90, and 99% effective doses of 0.6, 0.9, and 1.4 mg/kg, respectively. When administered prophylactically in a sporozoite challenge mouse model, KAF156 is completely protective as a single oral dose of 10 mg/kg. Finally, KAF156 displays potent Plasmodium transmission blocking activities both in vitro and in vivo. Collectively, our data suggest that KAF156, currently under evaluation in clinical trials, has the potential to treat, prevent, and block the transmission of malaria.
DOI http://dx.doi.org/10.1128/AAC.02727-13   (check subscription with CDU E-Gateway service for CDU Staff and Students  check subscription with CDU E-Gateway in new window)
Additional Notes This is an Open Access article distributed under the terms of the Creative Commons Attribution License 3.0, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
Description for Link Link to CC Attribution 3.0 License
URL https://creativecommons.org/licenses/by/3.0/au


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