CD163-Targeted Agents for Macrophage Delivery
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Solution Overview
Problem
Current therapies face challenges in specifically targeting macrophages for the treatment of autoimmune, inflammatory, and malignant diseases due to the lack of effective agents that can selectively bind to the CD163 receptor, limiting the therapeutic index and efficacy of drugs.
Innovation Solution
Development of agents with a binding moiety that exhibits specificity for the SRCR domain 1 of the CD163 receptor, allowing for targeted delivery of drugs to macrophages, which can be internalized by the cells, thereby enhancing the therapeutic impact on diseases such as rheumatoid arthritis, TB, HIV, and histiocytic sarcoma.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If drugs are administered systemically to treat diseases affecting macrophages, then the drugs can reach macrophages, but the drugs also affect other cells in the body, reducing the therapeutic index
Solution Approach 1:
The patent uses the CD163 receptor as an intermediary to deliver drugs specifically to macrophages. The binding moiety targets CD163, which is highly expressed on macrophages, allowing the drug to be transported selectively to these cells via receptor-mediated endocytosis, thereby avoiding systemic side effects while maintaining therapeutic efficacy
Solution Approach 2:
The patent applies local quality by concentrating the drug delivery mechanism specifically at macrophages through the CD163 binding moiety. The binding moiety is designed to recognize and bind to CD163 on macrophage surfaces, creating a localized drug delivery system that spares other cell types from exposure to the therapeutic agent
2Reliability
If drugs are targeted to macrophages using CD163 binding, then the therapeutic impact on macrophage-related diseases is enhanced, but the complexity of the drug delivery system increases
Solution Approach 1:
The patent creates a composite drug delivery system consisting of the binding moiety (designed to target CD163) combined with the therapeutic drug. This composite structure leverages the natural endocytic pathway of CD163 to achieve targeted delivery, combining the simplicity of natural biological mechanisms with targeted therapeutic delivery to enhance efficacy without excessive complexity
Solution Approach 2:
The patent exploits the self-service capability of macrophages, which naturally express CD163 and perform receptor-mediated endocytosis as part of their normal physiological function. By targeting this existing cellular mechanism, the drug delivery system utilizes the cell's own machinery for internalization, reducing the need for complex external delivery mechanisms while maintaining high therapeutic efficacy
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 agents effectively target macrophages, reducing inflammatory cytokine production, killing intracellular organisms, or eliminating malignant cells, thereby improving treatment outcomes for specific diseases with minimal impact on other cells, increasing the therapeutic index.
Implementation Method 1
an agent comprising a binding moiety with binding specificity for SRCR domain 1 of the CD163 receptor
Implementation Method 2
the endocytic properties of CD163 furthermore ensures that drugs linking to the receptor will be taken up by the cell and carried inside the cell to the lysosomes
Data Source
AI summary
The present invention relates to agents comprising a binding moiety with binding specificity for SRCR domain 1 of the CD163 receptor, for use in medicine. The invention also relates to methods, uses, kits and compositions comprising such agents.