etomoxir

Etomoxir is a **small molecule** that acts as an **irreversible inhibitor of carnitine palmitoyltransferase 1 (CPT1)**, the enzyme responsible for facilitating the transport of long-chain fatty acids into mitochondria for β-oxidation[1][3][5][6]. Its main mechanism results in inhibition of fatty acid oxidation, decreasing ketogenesis and gluconeogenesis, while increasing glucose oxidation in muscles and lowering triglyceride levels[1][2]. Etomoxir is metabolized intracellularly to its active CoA ester. It has also been described as a direct agonist of PPARα and has off-target effects at high concentrations, including disruption of CoA metabolism and inhibition of mitochondrial complex I[1][3]. Originally developed by Byk Gulden Lomberg for metabolic diseases like type 2 diabetes, it later underwent investigation for congestive heart failure, hyperlipidemia, various cancers, neuroinflammatory, and neurodegenerative diseases (notably malignant glioma, ALS, and Parkinson's disease), but clinical development was discontinued due to hepatotoxicity[1][2][4][6]. Recent interest persists for oncology and neurodegeneration[1][6].

Other names

rac-ethyl 2-[6-(4-chlorophenoxy)hexyl]oxirane-2-carboxylate