Drug for the treatment of steatohepatitis
Fatty liver and its progression towards more severe and potentially fatal clinical conditions such as steatohepatitis, hepatic fibrosis and cirrhosis, is now one of the most significant emerging diseases in Western societies. Its association with diabetes and high cardiovascular risk makes it even more relevant, constituting a serious public-health issue that demands relevant therapeutic intervention. There are currently no specific treatments for steatohepatitis. Clinical trials are being developed to market new drugs or nutraceutical products, including:
- Natural PPAR alpha receptor agonists, consisting of polyunsaturated fatty acids present in fish oil.
- Antioxidants and liposoluble vitamins, including vitamin D and resveratrol.
The research group has developed, as a completely novel alternative treatment, a new set of fatty-acid amides with phenylankylamines (amphetamines, dopamine, etc.), which exploit a new action mechanism based on reducing ingestion, antagonizing oxidative stress and activating the metabolism of fats and reducing their deposits.
- Activates PPAR alpha, with greater affinity than fibrates, to assure deep hypolipidemic effects and activators of the metabolism of fats.
- Reduces the depositing of fat in the liver. Inhibits the expression of an enzyme that has a fundamental mechanism in steatohepatitis.
- Has the capacity to reduce ingestion, thereby adding anti-obesity to their antisteatosic profile.
In the in vivo trails carried out (both chronic and acute), evidence has been found of activity against steatohepatitis, showing a reduction in the liver’s fatty mass and plasma triglyceride levels. Also the experiments have shown an improvement in kidney function by reducing the increase in urea plasma levels and the profile of hepatic transaminases in plasma.
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They are small molecules that are easy to synthesise.
These compounds are accepted according to Lipinsky’s rule.
Safe pharmacological profile, no interaction with hERG and doesn’t present or has only mild effects on the activity of the different isoforms of the hepatic cytochrome P450.
New therapeutic entities for one of the most prevalent emerging metabolic pathologies.
- Metabolic diseases and Endocrinology
- Digestive system