Etomoxir

Etomoxir is a drug that was primarily developed for the treatment of heart failure. It acts by irreversibly inhibiting carnitine palmitoyltransferase-1 (CPT-1) on the outer mitochondrial membrane, thereby preventing long-chain fatty acids from entering the mitochondria and being metabolized. This forces the cells to switch to glucose oxidation, which is thought to be more efficient.

Mechanism of action

Etomoxir works by inhibiting the enzyme carnitine palmitoyltransferase-1 (CPT-1), which is located on the outer mitochondrial membrane. This enzyme is responsible for the transport of long-chain fatty acids into the mitochondria, where they are oxidized to produce energy. By inhibiting CPT-1, etomoxir prevents the oxidation of fatty acids, forcing the cells to switch to glucose oxidation.

Clinical use

Etomoxir was initially developed for the treatment of heart failure. The rationale behind this was that the heart in heart failure patients tends to rely more on fatty acid oxidation for energy production, which is less efficient than glucose oxidation. By forcing the heart to switch to glucose oxidation, it was hoped that etomoxir could improve heart function.

However, clinical trials with etomoxir have shown mixed results. Some studies have shown improvements in heart function, while others have shown no benefit or even harm. As a result, etomoxir is not currently approved for the treatment of heart failure.

Side effects

The most common side effects of etomoxir include nausea, vomiting, and abdominal pain. In some cases, etomoxir can also cause liver damage.

Research

Research is ongoing into the potential use of etomoxir in other conditions, such as cancer, diabetes, and neurodegenerative diseases. In these conditions, the metabolic switch induced by etomoxir could potentially have therapeutic benefits.

See also

• Carnitine palmitoyltransferase-1
• Heart failure
• Metabolic switch

References

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