Integrin Targeting Agents for Multi-Modality Imaging

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Solution Overview

Problem

Current imaging techniques for assessing molecular endpoints in diseases are invasive and lack sensitivity, necessitating the development of noninvasive methods that can visualize specific molecular targets and pathways for enhanced diagnosis and treatment efficacy.

Innovation Solution

Development of integrin targeting agents with fluorescent and/or magnetic properties that selectively bind to αvβ3 integrin, enabling optical and multi-modality imaging, including optical imaging, magnetic resonance imaging, and nuclear imaging, to visualize angiogenesis and other physiological processes.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Measurement precision

If current imaging techniques (MRI, CT, ultrasound) are used, then anatomical and physiological information can be obtained, but the sensitivity and specificity for molecular targets are insufficient

Engineering Contradiction:
Improvemolecular target detection sensitivityVSAvoidimaging system complexity
Core Design Contradiction:
Measurement precisionVSDevice complexity

Solution Approach 1:

The patent combines multiple imaging modalities (optical imaging with fluorescent probes, magnetic resonance imaging with paramagnetic agents, and nuclear imaging with radioactive isotopes) into a single multi-modality imaging agent. This merging approach enables simultaneous acquisition of molecular specificity from optical imaging, anatomical context from MRI, and functional information from nuclear imaging, thereby resolving the contradiction between measurement precision and device complexity.

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The imaging agent is designed as a composite structure containing multiple functional components: a molecular targeting ligand (for specific binding to integrins or other molecular targets), a fluorescent probe (for optical detection), a paramagnetic agent (for MRI contrast), and a radioactive isotope (for nuclear imaging). This composite material approach allows a single agent to provide high sensitivity and specificity across multiple imaging modalities simultaneously.

Inventive Principle:
Principle #40Composite materials

2Measurement precision

If invasive tissue sampling and surgery are performed, then molecular endpoint assessment is possible, but patient morbidity and procedural complexity increase

Engineering Contradiction:
Improvemolecular endpoint assessment accuracyVSAvoidpatient morbidity
Core Design Contradiction:
Measurement precisionVSObject-affected harmful factors

Solution Approach 1:

The patent replaces invasive mechanical procedures (tissue biopsy, surgical sampling) with noninvasive imaging techniques. The multi-modality imaging agent can be administered systemically and will accumulate at molecular targets in vivo, allowing molecular endpoint assessment through external imaging detection without mechanical tissue disruption. This substitution eliminates patient morbidity while maintaining measurement precision.

Inventive Principle:
Principle #28Mechanics substitution (Replace mechanical system)

Solution Approach 2:

The imaging agent serves as an intermediary substance that bridges the gap between internal molecular processes and external detection. The agent specifically binds to molecular targets (such as integrins in angiogenesis) and carries multiple imaging reporters, translating invisible molecular events into detectable signals across multiple modalities without requiring direct tissue sampling.

Inventive Principle:
Principle #24Intermediary (Mediator)

3Productivity

If optical imaging in the visible region is used, then imaging speed and cost-effectiveness are improved, but penetration depth and sensitivity are limited

Engineering Contradiction:
Improveimaging scan speedVSAvoiddetection sensitivity
Core Design Contradiction:
ProductivityVSMeasurement precision

Solution Approach 1:

The patent utilizes fluorophores with emission wavelengths in the red and near-infrared region (600-900 nm) rather than visible wavelengths. This parameter change in the optical spectrum is critical because biological tissues have minimal absorption and scattering in this wavelength range, allowing deep penetration while maintaining high detection sensitivity. The imaging can be performed rapidly (seconds to minutes) while achieving both deep tissue penetration and molecular-level sensitivity.

Inventive Principle:
Principle #35Parameter changes

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

These agents provide stable, biocompatible solutions for in vivo and in vitro imaging, allowing for real-time molecular and functional information, enhancing the ability to diagnose and monitor disease states with improved sensitivity and specificity.

Implementation Method 1

optical probes can be designed as dynamic molecular imaging agents that may alter their reporting profiles in vivo to provide molecular and functional information in real time

Methodology Applied
Scientific EffectFluorescence: Fluorescence

Implementation Method 2

integrin targeting agents that can have fluorescent properties and/or magnetic properties (for example, paramagnetic or superparamagnetic properties) that can be used as MRI or multi-modality imaging agents

Methodology Applied
Scientific EffectMagnetic resonance: Magnetic Field

Data Source

PatentEP3673922A1Integrin targeting agents and methods of using same
Publication Date: 2020.07.01 VISEN MEDICAL INC
  • EP3673922A1 patent drawingFigure 1A~1B
  • EP3673922A1 patent drawingFigure 2A~2B
  • EP3673922A1 patent drawingFigure 3A~3D

AI summary

The invention provides a family of agents that target integrins, which can be used as imaging agents and/or therapeutic agents. The agents can be used to image angiogenesis, inflammation or other physiological processes in a subject.