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Gwangju Institute of Science and Technology Researchers Unveil Innovative Drug Candidate for Fatty Liver Disease Treatment

Friday, April 05, 2024

Metabolic dysfunction-associated steatotic liver disease (MASLD) poses a significant global health challenge, placing strain on healthcare resources and endangering public health. It involves the accumulation of fat in the liver, increasing the risk of progressing to more severe conditions like metabolic dysfunction-associated steatohepatitis (MASH), characterized by inflammation and potential fibrosis.

To address this pressing need for effective treatments, researchers led by Prof. Jin Hee Ahn at the Gwangju Institute of Science and Technology (GIST) have developed compound 11c, a novel peripheral 5HT2A antagonist. Their work, published in Nature Communications on January 20, 2024, represents a significant therapeutic advancement. Preclinical studies have shown the compound's efficacy, positioning it as a leading candidate in the treatment of metabolic disorders.

Compound 11c demonstrates robust biological activity and a favorable safety profile. Dr. Haushabhau Shivaji Pagire, lead author and senior researcher at GIST's Medicinal Chemistry Laboratory, highlights its ability to significantly reduce inflammatory and fibrosis markers, indicating promising anti-inflammatory and fibrotic effects essential for MASH treatment.

The compound's development involved identifying Desloratadine, a peripheral agent, and using molecular docking techniques to refine it into compound 11c.

Prof. Ahn underscores 11c's potential based on its efficacy in vitro and in vivo, tissue distribution, DMPK, and tox profiles. Its excellent safety profile, including hepatocyte and plasma stability, minimal cytotoxicity, and low cytochrome P450 inhibition, as well as over 60% oral bioavailability, make it a compelling candidate for MASH treatment.

Currently, obesity-associated MASH ranks third in liver transplant causes, potentially surpassing hepatitis C. Compound 11c, positioned as a promising oral treatment, could revolutionize liver disease management. The upcoming Phase 1 clinical trial marks a significant milestone, offering insights into the compound's performance in humans and potentially transforming metabolic disorder treatments.

In conclusion, compound 11c presents a promising avenue for combating the growing MASLD epidemic. With its notable attributes and upcoming Phase 1 trial, it represents a significant opportunity in liver disease management.



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