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(1-hydroxy-2-oxopiperidin-3-yl)phosphonic acid
- Development stage
- Preclinical
- Lead developer
- Methodist Hospital Research Institute
- Modality
- Small Molecules
- Administration
- Intranasal
01
Overview
(1-hydroxy-2-oxopiperidin-3-yl)phosphonic acid, also known as HEX, is a small molecule investigational drug that acts as a potent inhibitor of enolase enzymes. It has demonstrated strong inhibitory activity against *Naegleria fowleri* enolase (NfENO), with an IC50 of 0.14 μM and toxicity to trophozoites at low micromolar concentrations. HEX disrupts glycolysis in the pathogen by binding to the active site of NfENO, leading to accumulation of upstream glycolytic intermediates and parasite death. In preclinical studies, intranasal administration increased survival in rodent models infected with *N. fowleri* but was not fully curative. The compound is also being explored for its potential in targeting ENO1-deleted cancers due to selective inhibition of ENO2[5][8].
- Other names
- phosphonic acid, p-(1-hydroxy-2-oxo-3-piperidinyl)-[(3S)-1-hydroxy-2-oxopiperidin-3-yl]phosphonic acid
02
Targets
ENO (Alpha-enolase)
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