Drug intelligence / Profile preview

GSK2194069

Development stage
Preclinical
Lead developer
GSK
Modality
Small Molecules
Administration
Oral
01

Overview

GSK2194069 is a potent and selective small molecule inhibitor of the ketoacyl synthase (KS) domain of human fatty acid synthase (FAS). FAS is a multi-enzyme complex that plays a central role in de novo lipogenesis by converting acetyl-CoA and malonyl-CoA into long-chain saturated fatty acids, such as palmitate. GSK2194069 was developed by GSK to investigate the therapeutic potential of FAS inhibition in metabolic and oncological indications. In preclinical studies, it has been shown to reduce lipid accumulation in various cell types. Recent research presented at the AHA 2024 meeting highlights its ability to attenuate the formation of macrophage-derived foam cells, suggesting a potential therapeutic role in managing atherosclerosis and related vascular diseases.

02

Targets

FASN (Fatty acid synthase)

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