Drug intelligence / Profile preview

E1018

Development stage
Unknown
Lead developer
Eisai
Modality
Small Molecules
Administration
Oral
01

Overview

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.

02

Targets

aaRS (Aminoacyl-tRNA synthetase family)

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