Introduction: Malaria is a major health problem in endemic countries and chemotherapy remains the most important tool in combating it. Treatment options are limited and essentially rely on a single drug class - the artemisinins. Efforts are ongoing to restrict the evolving threat of artemisinin resistance but declining sensitivity has been reported. Fueled by the ambitious aim of malaria eradication, novel antimalarial compounds, with improved properties, are now in the progressive phase of drug development.
Areas covered: Herein, the authors describe antimalarial compounds currently in Phase II clinical development and present the results of these investigations.
Expert opinion: Thanks to recent efforts, a number of promising antimalarial compounds are now in the pipeline. First safety data have been generated for all of these candidates, although their efficacy as antimalarials is still unclear for most of them. Of particular note are KAE609, KAF156 and DSM265, which are of chemical scaffolds new to malaria chemotherapy and would truly diversify antimalarial options. Apart from SAR97276, which also has a novel chemical scaffold that has had its development stopped, all other compounds in the pipeline belong to already known substance classes, which have been chemically modified. At this moment in time, there is not one standout compound that will revolutionize malaria treatment but several compounds that will add to its control in the future.
Keywords: AQ-13; DF02; DSM265; KAE609; KAF156; OZ439; Phase II; Plasmodium falciparum; Plasmodium vivax; SAR97276; artemisone; chemotherapy; drug development; ferroquine; fosmidomycin; methylene blue; sevuparin; tafenoquine.