4-Hydroxybenzoic Acid-Bound Gadolinium Compound for Amyloid-Beta MRI
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Solution Overview
Problem
Current MRI contrast agents are non-specific and lack efficacy in diagnosing degenerative brain diseases such as Alzheimer's and Parkinson's, and there is a need for agents that can target amyloid beta polymers to enable early detection and treat neuroinflammatory diseases.
Innovation Solution
A gadolinium-based compound that specifically binds to amyloid beta polymers, allowing for targeted MRI contrast agents and pharmaceutical compositions to diagnose and treat neuroinflammatory diseases.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Measurement precision
If conventional gadolinium-based contrast agents are used, then MRI imaging is performed, but the contrast agents are non-specific and cannot target amyloid beta polymers for early diagnosis of degenerative brain diseases
Solution Approach 1:
The patent modifies the gadolinium contrast agent to have specific local properties through the introduction of a targeting moiety that specifically binds to amyloid beta polymers. This allows the contrast agent to concentrate at specific pathological sites (amyloid deposits) rather than distributing uniformly, thereby achieving both high measurement precision for disease detection and specific adaptability to target the pathological substrate.
2Adaptability or versatility
If non-specific contrast agents are used, then extracellular fluid distribution is achieved, but specific targeting of neuroinflammatory markers is not possible
Solution Approach 1:
The patent introduces a targeting moiety as an intermediary component that mediates between the gadolinium-based contrast agent and the amyloid beta polymers. This intermediary enables specific recognition and binding to the target, allowing the contrast agent to accumulate at the pathological site in sufficient quantities while maintaining the beneficial properties of the gadolinium core.
3Measurement precision
If early detection of degenerative brain diseases is pursued, then sensitivity to amyloid beta polymer concentration changes is needed, but current contrast agents lack this capability
Solution Approach 1:
The patent creates a composite contrast agent structure combining the gadolinium-based MRI active component with a targeting moiety specific to amyloid beta polymers. This composite material integrates the imaging functionality with the targeting capability, enabling sensitive detection of amyloid beta polymer concentration changes while maintaining a structure that can be synthesized and manufactured.
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 compound effectively crosses the blood-brain barrier, enhances MRI contrast for diagnosing degenerative brain diseases, and exhibits anti-inflammatory properties by reducing NLRP3, a key inflammatory factor, thus aiding in disease diagnosis and treatment.
Implementation Method 1
The contrast agent uses a paramagnetic or superparamagnetic material to affect the relaxation action to enhance the difference in relaxation between tissues and thus induce change in the MRI signal
Implementation Method 2
when the compound is injected intravenously, the compound may flow through a blood-brain-barrier (BBB)
Data Source
AI summary
Disclosed is a gadolinium-based compound, and an MRI contrast agent including same. The gadolinium-based compound may be a DO3A-based gadolinium compound to which 4-hydroxybenzoic acid is bound. The MRI contrast agent may include the compound. Also disclosed is a pharmaceutical composition for preventing or treating neuroinflammatory diseases, wherein the composition comprises the compound or a pharmaceutically acceptable salt thereof.