Danazol Modulation of Endothelial Cytoskeleton for Vascular Permeability Control
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Solution Overview
Problem
Current treatments for vascular hyperpermeability, which leads to conditions like macular edema and other adverse effects, are inadequate in preventing tissue and organ damage at early stages of diseases such as diabetes and hypertension.
Innovation Solution
Administration of a vascular hyperpermeability-inhibiting amount of danazol or its pharmaceutically acceptable salts, which modulates the cytoskeleton of endothelial cells to reduce permeability and stabilize the endothelial barrier, thereby preventing fluid leakage and tissue damage.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional treatments for vascularhyperpermeability are used, then some therapeutic effect is achieved, but tissue and organ damage occurs at early stages of diseases such as diabetes and hypertension
Solution Approach 1:
The patent applies preliminary action by administering danazol at early stages of diseases such as diabetes and hypertension, before significant tissue and organ damage occurs. The treatment targets vascularhyperpermeability in its initial phases, preventing the progression to severe complications like macular edema and cardiovascular events.
Solution Approach 2:
The patent utilizes parameter changes by employing significantly lower doses of danazol (0.1-10 mg/day) compared to conventional doses (200-800 mg/day). This dosage reduction represents a critical parameter change that achieves therapeutic effectiveness while minimizing harmful side effects and tissue damage.
2Reliability
If higher doses of danazol are administered to inhibit vascularhyperpermeability, then therapeutic effect is improved, but side effects increase
Solution Approach 1:
The patent fundamentally changes the dosage parameter of danazol from conventional high doses (200-800 mg/day) to significantly lower doses (0.1-10 mg/day). This parameter change maintains therapeutic effectiveness in inhibiting vascularhyperpermeability while dramatically reducing harmful side effects such as liver enzyme elevation and hormonal disturbances.
Solution Approach 2:
The patent applies partial action by using a reduced dosage of danazol that is sufficient to achieve the desired therapeutic effect of inhibiting vascularhyperpermeability, but excessive compared to what would be needed if the drug were perfectly efficient. This partial action approach balances effectiveness with safety.
3Ease of operation
If current treatments are used for vascularhyperpermeability, then some symptom relief is achieved, but prevention of tissue damage at early stages is inadequate
Solution Approach 1:
The patent implements preliminary action by treating vascularhyperpermeability at its earliest stages in diseases like diabetes and hypertension, before tissue damage becomes irreversible. This early intervention approach prevents the progression to severe complications while providing symptom relief.
Solution Approach 2:
The patent applies preliminary anti-action by administering danazol to counteract the developing vascularhyperpermeability before it causes significant tissue damage. This preventive approach opposes the pathological process at its inception, preventing rather than merely treating the harm.
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
Danazol effectively inhibits vascular hyperpermeability at significantly lower doses than previously reported, reducing the risk of tissue and organ damage in diseases mediated by increased permeability, including diabetic retinopathy and hypertension, with minimal side effects.
Implementation Method 1
danazol or a pharmaceutically acceptable salt thereof, wherein the danazol compound modulates the cytoskeleton of endothelial cells
Data Source
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AI summary
The invention provides a method of inhibiting vascular hyperpermeability in an animal in need thereof. The method comprises administering a vascular- hyperpermeability-inhibiting amount of a danazol compound to the animal. The invention also provides a method of modulating the cytoskeleton of an endothelial cell in an animal. The method comprises administering an effective amount of a danazol compound to the animal.