Drug intelligence / Profile preview

ET2.39

Development stage
Preclinical
Lead developer
University of New South Wales
Modality
Small Molecules
Administration
Oral
01

Overview

ET2.39 is a novel, small-molecule ceramide synthase (CerS) inhibitor targeting TLC domain-containing protein 3B (TLCD3B), a non-canonical ceramide synthase. Developed by the Victor Chang Cardiac Research Institute and the University of New South Wales (UNSW Sydney), ET2.39 is designed to selectively inhibit the production of deleterious ceramides (specifically C16:0 and C18:0 ceramides) that are associated with cardiometabolic diseases, insulin resistance, and obesity. In preclinical mouse models of high-fat diet (HFD)-induced obesity, oral administration of ET2.39 significantly prevented weight gain, slowed fat mass accretion, and reduced the accumulation of C18:0 ceramides in key metabolic tissues such as skeletal muscle and heart without affecting cell viability.

02

Targets

Sphingolipid (Sphingolipid metabolism)

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