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E1018 is an investigational small molecule antimalarial drug developed by Eisai in collaboration with the Broad Institute. It functions as a selective inhibitor of Phenylalanine tRNA synthetase (PheRS), an enzyme essential for protein synthesis in the malaria parasite *Plasmodium falciparum*. Discovered through the screening of the Broad Institute's Diversity Oriented Synthesis (DOS) library, E1018 exhibits a multi-stage activity profile, targeting the parasite during its liver, asexual blood, and transmission stages (corresponding to MMV Target Candidate Profiles TCP-1, TCP-4, and TCP-5). This broad activity makes it a promising candidate for both the treatment and prevention of malaria, as well as for blocking transmission to support eradication efforts. E1018 is currently in Phase 1 clinical development, with studies evaluating its safety, tolerability, and pharmacokinetics in healthy adult volunteers following oral administration.
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