ERbeta-Selective Estrogenic Compounds for Menopausal Therapy
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Solution Overview
Problem
Current menopausal hormone therapy (MHT) options, such as traditional estrogen therapy, are associated with increased risks of breast cancer, stroke, venous thrombosis, and Alzheimer's disease, limiting their long-term use for treating menopausal symptoms.
Innovation Solution
Development of ERβ-selective estrogenic compounds, including Liquiritigenin, Apigenin, and others, which selectively modulate estrogen receptor beta (ERβ) activity without activating estrogen receptor alpha (ERα), potentially reducing the risks associated with traditional estrogen therapies.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If traditional estrogen therapy is used to treat menopausal symptoms, then therapeutic benefits are achieved, but the risk of breast cancer, stroke, venous thrombosis, and Alzheimer's disease increases
Solution Approach 1:
The patent segments the estrogen receptor system into two distinct targets: ERα and ERβ. By developing compounds that selectively modulate ERβ while sparing ERα, the invention divides the therapeutic action from the harmful effects, allowing treatment of menopausal symptoms without activating ERα-mediated cancer and thrombosis risks
Solution Approach 2:
The invention applies local quality by creating estrogenic compounds with tissue-selective activity. The compounds exhibit ERβ-selective modulation in specific tissues (providing therapeutic benefits) while maintaining ERα selectivity in sensitive tissues (avoiding harmful effects), thereby achieving different functional qualities in different biological contexts
2Object-affected harmful factors
If ERβ-selective compounds are used to reduce cancer risk, then safety is improved, but the complexity of the therapy increases
Solution Approach 1:
The patent changes the molecular parameter of receptor selectivity by designing compounds with specific chemical structures (e.g., 4-phenyl-1,2,4-triazole derivatives) that confer ERβ preference. This parameter change in molecular architecture translates to improved safety without requiring complex multi-component therapies
Data Source
AI summary
Estrogenic compounds, combinations, pharmaceutical compositions and methods are presented. The estrogenic compounds comprise ERβ-selective estrogenic compounds and combinations thereof. The novel compositions comprise one or more of the ERβ-selective estrogenic compounds, and may optionally comprise one or more excipients. The one or more excipients may be pharmaceutically acceptable. The one or more excipients may comprise at least one compound that does not occur in nature with estrogenic compounds. The method comprises administering a pharmaceutical composition comprising an estrogenic compound described herein to a patient in need of treatment with an estrogenic compound or combination, or a pharmaceutical composition comprising the estrogenic compound or combination.