Composition for preventing or treating valvular calcification comprising 2,4-dihydroxyacetophenone

Small-molecule agent for valvular calcification targeting the RUNX2 inhibition mechanism

This technology is a composition for preventing and improving valvular calcification, featuring 2,4-dihydroxyacetophenone or its salts as an active ingredient. With rights secured for both pharmaceutical and food compositions, it can be commercialized as either a drug or a health functional food.

Aortic valve stenosis is a major cardiovascular disease with a high incidence in the elderly population. However, due to the lack of identified target substances to effectively prevent valvular calcification, there have been virtually no pharmacological treatment options. The only alternative, valve replacement surgery, is costly and presents challenges regarding procedural risks for elderly patients and long-term durability.

This technology utilizes a small-molecule compound that inhibits the expression of RUNX2, a protein marker for calcification. Its scope covers a broad range of calcification-related diseases, including valvulopathy, heart failure, angina, and aortic valve stenosis, and includes designs for combination therapy with other calcification inhibitors. It can be applied to the development of cardiovascular drug candidates, health functional foods for the elderly, and pre- and post-procedural management products, allowing for the capture of a new product category based on small-molecule agents in a field previously dominated by surgery.

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Key Features:

• Pharmaceutical composition for preventing or treating valvular calcification comprising 2,4-dihydroxyacetophenone or a pharmaceutically acceptable salt thereof as an active ingredient
• Pharmaceutical composition for treating valvular calcification targeting one or more of the following: valvulopathy, heart failure, myocardial ischemia, acute coronary syndrome, angina, and aortic valve stenosis
• Composition for preventing or treating valvular calcification that inhibits the calcification marker RUNX2 and may additionally include other valvular calcification inhibitors
• Food composition for preventing or improving calcification comprising 2,4-dihydroxyacetophenone or a food-grade acceptable salt thereof as an active ingredient

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This invention was developed with support from the Ministry of Science and ICT for the discovery of biomarkers and therapeutic targets to inhibit intractable aortic valve calcification using multi-omics data-based deep learning.

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