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

Sarah Schleiferbock, Christian Scheurer, Masataka Ihara, Isamu Itoh, Ian C Bathurst, Jeremy Burrows, Pascal Fantauzzi, Julie Lotharius, Susan Ann Charman, Julia Morizzi, David Shackleford, Karen Louise White, Reto Brun, Sergio Wittlin

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8 Citations (Scopus)

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.
Original languageEnglish
Pages (from-to)1377 - 1384
Number of pages8
JournalDrug Design, Development and Therapy
Volume7
DOIs
Publication statusPublished - 2013

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