CCR2 PET Imaging Agents for Non-Invasive Receptor Detection
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Solution Overview
Problem
Current methods lack non-invasive imaging techniques for detecting CCR2 receptors, which are associated with various diseases and conditions such as atherosclerosis, inflammatory disorders, and cancer, highlighting the need for effective imaging agents and methods to detect, monitor, and evaluate conditions associated with CCR2 upregulation or overexpression.
Innovation Solution
Development of imaging agents comprising a CCR2 binding peptide, a radiolabel, and a nanoparticle or chelator, specifically designed for positron emission tomography (PET) imaging, to detect and monitor CCR2 receptors in tissues, with the ability to administer and detect signals at different time points to assess disease progression.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Difficulty of detecting and measuring
If conventional imaging methods are used, then existing disease detection capabilities are maintained, but the ability to non-invasively detect CCR2 receptors is lacking
Solution Approach 1:
The patent employs a radiolabeled peptide binder as an intermediary substance that selectively binds to CCR2 receptors on the surface of monocytes and macrophages. This intermediary enables the imaging agent to detect CCR2 receptors indirectly through their binding interaction, transforming an undetectable receptor into a detectable signal via the radiolabeled compound.
Solution Approach 2:
The patent replaces traditional mechanical or invasive detection methods with a radiological imaging approach. By using positron emission tomography (PET) scanning to detect the radiolabeled peptide binder, the system substitutes physical invasion or direct observation with non-invasive radiological detection, enabling remote measurement of CCR2 receptor distribution.
2Ease of operation
If imaging agents are developed to detect CCR2 receptors, then non-invasive detection is achieved, but the complexity of the imaging agent composition increases
Solution Approach 1:
The imaging agent is segmented into distinct functional components: a peptide binder (ECL1i) that provides target specificity, a chelator (DOTA) that enables radiolabeling, and a radiolabel (64Cu) that provides detectability. This segmentation allows each component to be optimized independently while maintaining overall functionality, making the complex agent manageable and manufacturable.
Solution Approach 2:
The imaging agent is a composite material combining organic peptide components with inorganic radiometals. The composite structure integrates the biological specificity of the peptide binder with the detectability of the radiolabel, creating a multifunctional agent that achieves non-invasive imaging while managing compositional complexity through established conjugation chemistry.
3Measurement precision
If multiple timepoints are used to monitor disease progression, then disease monitoring accuracy is improved, but the frequency of administration and signal detection increases
Solution Approach 1:
The patent implements a feedback-based monitoring approach where imaging agents are administered at multiple timepoints to track disease progression. The PET scan results provide feedback on CCR2 receptor expression changes, allowing clinicians to assess whether disease is improving, worsening, or stable. This feedback mechanism enables precise disease monitoring while the repeated administration is justified by the clinical need for progression assessment.
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 imaging agents provide sensitive and specific detection of CCR2 receptors, enabling non-invasive monitoring of inflammation and disease progression, as demonstrated in animal models and human tissues, laying the groundwork for clinical applications.
Implementation Method 1
a method of detecting CCR2 receptors in a subject having atherosclerosis is provided. The method comprises: administering a CCR2-specific imaging agent to the subject; and detecting a first signal from the CCR2-specific imaging agent
Implementation Method 2
the CCR2-specific imaging agent comprises a CCR2 binding peptide comprising a TFLK sequence, a radiolabel, and a chelator; the CCR2 binding peptide is no more than 200 amino acids in length; the chelator is conjugated to the CCR2 binding peptide; and the radiolabel is bound to the chelator
Data Source
AI summary
Among the various aspects of the present disclosure is the provision of compositions of imaging agents and methods for use in detecting, monitoring, and evaluating CCR2 associated diseases, disorders, and conditions.