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In vitro and in vivo characterization of the antimalarial lead compound SSJ-183 in Plasmodium models

Authors Schleiferböck S, Scheurer C, Ihara M, Itoh I, Bathurst I, Burrows JN, Fantauzzi P, Lotharius J, Charman SA, Morizzi J, Shackleford DM, White KL, Brun R, Wittlin S

Received 10 July 2013

Accepted for publication 23 August 2013

Published 15 November 2013 Volume 2013:7 Pages 1377—1384


Checked for plagiarism Yes

Review by Single anonymous peer review

Peer reviewer comments 4

Sarah Schleiferböck,1,2 Christian Scheurer,1,2 Masataka Ihara,3,4 Isamu Itoh,3,4 Ian Bathurst,5,† Jeremy N Burrows,5 Pascal Fantauzzi,5 Julie Lotharius,5 Susan A Charman,6 Julia Morizzi,6 David M Shackleford,6 Karen L White,6 Reto Brun,1,2 Sergio Wittlin1,2

1Swiss Tropical and Public Health Institute, Basel, 2University of Basel, Basel, Switzerland; 3Drug Discovery Science Research Center, Hoshi University, Shinagawa, Tokyo, Japan; 4Synstar Japan Co, Ltd, Odawara, Japan; 5Medicines for Malaria Venture, Geneva, Switzerland; 6Centre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Parkville, VIC, Australia

†Ian Bathurst passed away on 26 June 2011

Abstract: The objective of this work was to characterize the in vitro (Plasmodium falciparum) and in vivo (Plasmodium berghei) activity profile of the recently discovered lead compound SSJ-183. The molecule showed in vitro a fast and strong inhibitory effect on growth of all P. falciparum blood stages, with a tendency to a more pronounced stage-specific action on ring forms at low concentrations. Furthermore, the compound appeared to be equally efficacious on drug-resistant and drug-sensitive parasite strains. In vivo, SSJ-183 showed a rapid onset of action, comparable to that seen for the antimalarial drug artesunate. SSJ-183 exhibited a half-life of about 10 hours and no significant differences in absorption or exposure between noninfected and infected mice. SSJ-183 appears to be a promising new lead compound with an attractive antimalarial profile.

Keywords: antimalarial studies, cross-resistance, stage-specificity, Plasmodium falciparum

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