Selective Estrogen Receptor Beta Agonist for Menopause
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Current treatments for menopausal symptoms, particularly hot flashes, often come with risks such as increased cancer risk and side effects, and existing non-hormonal remedies have limited efficacy.
Innovation Solution
A composition comprising herbal extracts from Radix Rehmanniae, Fructus Corni Officinalis, Radix Dioscoreae Oppositae, Sclerotium Poriae Cocos, Cortex Moutan Radicis, Rhizoma Alismatis Orientalis, Anemarrhena Rhizome, Glycyrrhiza uralensis, and Atractylodis Macrocephalae Rhizoma, which acts as a selective estrogen receptor beta agonist, is used to treat menopausal symptoms without activating estrogen receptor alpha, thus minimizing cancer risks.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If hormone replacement therapy using estrogen is used to treat menopausal symptoms, then the efficacy in reducing hot flashes is improved, but the risk of uterine cancer, breast cancer and cardiovascular events increases
Solution Approach 1:
The invention segments the estrogen receptor system into two distinct pathways: ERα and ERβ. By designing a compound that selectively activates only ERβ while leaving ERα inactive, the treatment achieves therapeutic benefits through ERβ activation without the harmful effects mediated by ERα, thus resolving the contradiction between efficacy and safety
Solution Approach 2:
The patent applies local quality by creating a compound with differential binding properties to different estrogen receptor subtypes. The compound exhibits high selectivity for ERβ receptors in the brain (therapeutic target) while having minimal or no activity at ERα receptors (harmful pathway), thereby achieving localized therapeutic action without systemic harmful effects
2Reliability
If selective serotonin reuptake inhibitors are used to treat hot flashes, then some efficacy is achieved, but side effects occur that limit their use
Solution Approach 1:
The invention introduces a new intermediary mechanism by targeting estrogen receptor beta directly, bypassing the serotonin reuptake pathway entirely. This direct action on thermoregulatory centers through ERβ activation provides efficacy without the side effects associated with serotonin modulation, resolving the contradiction between benefit and harm
3Object-affected harmful factors
If non-hormonal remedies such as isoflavone, black cohosh, vitamin E are used, then some women use them, but their efficacy is less than hormone replacement therapies
Solution Approach 1:
The patent creates a composite chemical structure that combines the safety profile of non-hormonal remedies with the efficacy mechanism of hormone replacement therapy. The compound is a synthetic molecule designed to mimic beneficial estrogen effects selectively, achieving both high efficacy through ERβ activation and safety by avoiding ERα-mediated harmful effects and non-hormonal limitations
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
The composition significantly reduces the frequency and severity of hot flashes and nighttime awakenings, lowers cholesterol and LDL levels, and aids in weight reduction, with no significant adverse events or cancer risk, demonstrating its safety and effectiveness in treating menopausal symptoms.
Implementation Method 1
acts as a selective estrogen receptor beta agonist, is used to treat menopausal symptoms without activating estrogen receptor alpha
Data Source
AI summary
Provided herein are compositions comprising an herbal extract of a mixture of Radix Rehmanniae, Fructus Corni Officinalis, Radix Dioscoreae Oppositae, Sclerotium Poriae Cocos, Cortex Moutan Radicis, Rhizoma Alismatis Orientalis, Anemarrhena Rhizome, Glycyrrhiza uralensis, Radix Astragali, and Atractylodis Macrocephalae Rhizoma. The invention also relates to a method of treating hot flashes associated with peri-menopause, menopause, or post-menopause, a method of reducing total cholesterol and/or lowering low density lipoprotein (LDL) levels and a method of reducing weight and/or body mass index (BM I) using the above mentioned herbal extract.