Drug intelligence / Profile preview

HEA-39

Development stage
Preclinical
Lead developer
Mayo Clinic
Modality
Small Molecules
01

Overview

HEA-39 is a hydroxyethylamine (HEA)-based piperazine derivative that acts as a broad-spectrum parasite hexose transporter (HT) inhibitor. Developed by researchers at the University of Delhi and the Mayo Clinic, HEA-39 targets the parasite hexose transporters PF3D7_0204700 (PfHT1) in Plasmodium falciparum and LdBPK_330310 in Leishmania donovani, which share high homology. By binding to the signature domains of these transporters, HEA-39 blocks glucose uptake, thereby depriving the parasites of their primary energy source. It has demonstrated potent in vitro anti-parasitic activity against P. falciparum and L. donovani with low nanomolar IC50 values, and in silico studies suggest potential activity against Toxoplasma and Trypanosoma species, without showing apparent cytotoxicity in human cell lines.

02

Targets

GLUT1 (Glucose transporter 1)

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