Radiolabeled Dabigatran Derivatives for Atherosclerotic Plaque Imaging
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Solution Overview
Problem
Current imaging technologies lack sensitive and specific methods for non-invasive visualization of atherosclerotic lesions, which are crucial for early detection and monitoring of cardiovascular diseases, leading to high mortality and economic burden.
Innovation Solution
Development of dabigatran derivatives radiolabeled with PET and SPECT labels, such as 131I, 125I, 123I, 99mTc, 18F, and others, which directly bind to thrombin and accumulate in forming plaques or thrombi, enabling effective imaging and treatment of atherosclerotic plaque and thrombus.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Measurement precision
If conventional imaging modalities (IVUS, OCT, CT, MR, arteriography) are used to visualize atherosclerotic lesions, then structural information can be obtained, but non-invasive detection with high sensitivity and specificity remains limited
Solution Approach 1:
The patent uses radiolabeled antibodies as intermediary agents that specifically bind to antigens expressed by smooth muscle cells in atherosclerotic plaques. These antibodies serve as mediators between the imaging system and the target lesions, enabling sensitive and specific non-invasive detection through SPECT or PET imaging of the radiolabeled complexes
Solution Approach 2:
The patent changes the detection parameter from structural imaging to molecular imaging by using radiolabeled antibodies that target specific molecular markers (antigens) on smooth muscle cells. This parameter change enables detection of early atherosclerotic lesions with higher sensitivity and specificity before structural changes become apparent on conventional imaging
2Reliability
If radiolabeled antibodies targeting smooth muscle cell antigens are used, then early atherosclerotic lesions can be detected non-invasively, but the imaging method requires complex radiolabeling and antibody production
Solution Approach 1:
The patent develops universal radiolabeled antibody reagents that can detect multiple aspects of atherosclerosis through a single platform. The radiolabeled antibodies serve multiple functions: specific targeting of smooth muscle cells, non-invasive imaging capability, and potential for both diagnosis and monitoring of therapeutic response
Solution Approach 2:
The patent performs preliminary radiolabeling of antibodies in advance, creating stable radiolabeled reagents that can be stored and used for multiple imaging studies. This preliminary action simplifies the actual imaging procedure by eliminating the need for complex on-site radiolabeling equipment and procedures
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 use of dabigatran derivatives provides highly specific and sensitive imaging and treatment options for atherosclerotic plaque and thrombus, facilitating early detection, monitoring, and therapy efficacy assessment, thereby reducing cardiovascular disease-related mortality and healthcare costs.
Implementation Method 1
radiolabeled with PET and SPECT labels, such as 131I, 125I, 123I, 99mTc, 18F, and others
Implementation Method 2
directly bind to thrombin and accumulate in forming plaques or thrombi
Data Source
AI summary
The invention provides cardiovascular imaging agents comprising an anticoagulant (e.g., dabigatran derivatives) with a label (e.g., radiolabeled, fluorinated or radiofluorinated). Methods for using the cardiovascular imaging agents and kits containing the cardiovascular imaging agents or components suitable for production of the cardiovascular imaging agents are also provided.