Dextran-Mannose Therapeutic Compounds for Specific Macrophage Targeting

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Solution Overview

Problem

Current methods for targeting and treating diseases mediated by mannose-binding C-type lectin receptor-high expressing cells, such as macrophages, are limited in specificity and efficacy, particularly in conditions like autoimmune diseases, inflammatory diseases, and cancers.

Innovation Solution

Development of compounds comprising a dextran backbone with mannose-binding C-type lectin receptor targeting moieties and therapeutic agents, which selectively target and bind to cells like macrophages, allowing for diagnostic and therapeutic applications.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional therapeutic agents are used, then treatment can be provided, but specificity and efficacy in targeting macrophages is limited

Engineering Contradiction:
ImprovespecificityVSAvoidcompound structure
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The compound is divided into distinct functional segments: a dextran backbone providing structural framework, mannose moieties providing target-specific binding to CD206 receptors on macrophages, and therapeutic agent moieties providing treatment function. This segmentation allows each component to perform its specialized function, achieving high specificity for macrophage targeting while maintaining manageable structural complexity through modular design.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The invention creates a composite compound combining dextran (a polysaccharide), mannose (a monosaccharide), and therapeutic agents (various pharmacological compounds). This composite structure leverages the specific properties of each material: dextran provides solubility and stability, mannose provides selective binding to macrophage CD206 receptors, and the therapeutic agents provide disease-treating activity. The composite nature enables simultaneous achievement of specificity and efficacy.

Inventive Principle:
Principle #40Composite materials

2Reliability

If conventional therapeutic agents are used, then treatment can be provided, but efficacy in treating diseases mediated by macrophages is limited

Engineering Contradiction:
ImproveefficacyVSAvoidcompound structure
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The compound exhibits local quality through the strategic placement of mannose moieties at specific locations on the dextran backbone. These mannose units are positioned to maximize interaction with CD206 receptors on macrophage surfaces. The therapeutic agents are also strategically attached to ensure delivery to the target cells. This localized functional arrangement enhances efficacy by concentrating the therapeutic action precisely where needed - at the macrophage cell surface and interior - while the overall compound structure remains systematically organized.

Inventive Principle:
Principle #3Local quality

3Measurement precision

If non-specific therapeutic agents are used, then treatment coverage is broad, but targeting precision for mannose-binding C-type lectin receptor-high expressing cells is insufficient

Engineering Contradiction:
Improvetargeting precisionVSAvoiddisease treatment range
Core Design Contradiction:
Measurement precisionVSAdaptability or versatility

Solution Approach 1:

The compound achieves universality by combining a universal targeting mechanism (mannose binding to CD206 receptors) with multiple potential therapeutic agent options. The dextran-mannose core structure provides universal macrophage targeting capability that can be applied across different diseases. Meanwhile, the therapeutic agent portion can be customized from various pharmacological compounds depending on the specific disease indication, such as anti-inflammatory agents for autoimmune diseases, anti-cancer agents for malignancies, or anti-infective agents for infections. This multi-functional design enables both high targeting precision and broad disease treatment range.

Inventive Principle:
Principle #6Universality (Multi-functionality)

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 compounds effectively diagnose and treat diseases by selectively targeting mannose-binding C-type lectin receptor-high expressing cells, providing therapeutic agents that can induce apoptosis in these cells and improve disease outcomes.

Implementation Method 1

Tilmanocept has a small molecular size (7 nanometers) and carries multiple units of mannose. This mannose component has a high affinity for mannose-binding C-type lectin receptor proteins, such as CD206 and CD209, which are found in high concentrations on the surface of macrophages, dendritic cells and other cells. By tightly binding to these mannose receptors, Tilmanocept accumulates in lymphatic tissue within minutes and localizes in tumor-draining lymph nodes.

Methodology Applied
Scientific EffectMannose-binding C-type lectin receptor binding: Adsorption

Data Source

PatentUS20250228985A1Compounds and compositions for targeting macrophages and other mannose-binding c-type lectin receptor high expressing cells and methods of treating and diagnosis using same
Publication Date: 2025.07.17 CARDINAL HEALTH 414 LLC
  • US20250228985A1 patent drawing
  • US20250228985A1 patent drawing
  • US20250228985A1 patent drawing

AI summary

Provided are compounds and compositions for targeting macrophages and other mannose-binding c-type lectin receptor high expressing cells and methods of treatment and diagnosis using such compounds and compositions.