Drug intelligence / Profile preview

E121

Development stage
Preclinical
Lead developer
Kuwait University
Modality
Small Molecules
Administration
Parenteral
01

Overview

E121 is a novel small molecule enaminone derivative with anti-inflammatory properties. It has been investigated primarily for its potential in treating inflammatory bowel diseases (IBD), including Crohn's disease and ulcerative colitis. In preclinical studies using the murine Dextran Sulfate Sodium (DSS) model, E121 demonstrated the ability to reduce colitis severity at both gross and histological levels when administered at doses of 30–60 mg/kg. It serves as the parental compound for the JOAB series of compounds, which are modified enaminones designed to enhance potency and inhibit chemokine signaling through CCR2. E121 exerts its effects by modulating the production of pro-inflammatory cytokines, although it is less potent than some of its newer derivatives in certain treatment models.

Other names
enaminone E121
02

Targets

IL1B (Interleukin-1 beta)IL-6 (Interleukin 6)TNFA (Tumor necrosis factor alpha (soluble))

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