N4 Chelating Agents for Tumor-Specific Radionuclide Imaging

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Solution Overview

Problem

Current radionuclide imaging techniques, such as PET and SPECT, face limitations in differentiating invasive lesions from edema, radiation necrosis, or gliosis, and require complex and time-consuming synthesis processes for tumor-specific imaging, particularly with 18F-FDG, which is costly and not easily accessible for simultaneous production of multiple agents.

Innovation Solution

Development of a simple chelation technique using N4 compounds and derivatives that can be chelated with various metallic isotopes, including 99mTc, for tissue-specific targeted radioimaging and radiotherapy, allowing for more efficient and specific tumor imaging and therapy.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Measurement precision

If complex synthesis processes are used for tumor-specific imaging (e.g., 18F-FDG), then imaging specificity is improved, but production time and cost increase

Engineering Contradiction:
Improvetumor imaging specificityVSAvoidsynthesis time
Core Design Contradiction:
Measurement precisionVSLoss of time

Solution Approach 1:

The patent changes the chemical parameters by using N4 compounds with specific structural features (tetraazacycloalkane rings with 4-7 atoms) that inherently provide high tumor specificity through nitrogen metabolism pathways, eliminating the need for complex multi-step synthesis processes required by traditional 18F-FDG methods

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The invention extracts and utilizes the natural nitrogen metabolism pathways in tumor cells by designing N4 compounds that mimic endogenous nitrogen-containing molecules, allowing direct uptake and retention in tumors without requiring complex external synthesis or multiple chemical modification steps

Inventive Principle:
Principle #2Taking out (Extraction)

2Adaptability or versatility

If multiple radiotracers are produced simultaneously, then imaging versatility is improved, but production complexity increases

Engineering Contradiction:
Improveimaging versatilityVSAvoidproduction complexity
Core Design Contradiction:
Adaptability or versatilityVSDevice complexity

Solution Approach 1:

The N4 compound platform serves multiple imaging functions by allowing attachment of different radionuclides (18F, 11C, 15O, 13N) to the same core molecular structure, enabling a single synthesis platform to produce multiple radiotracers for different imaging needs without requiring separate complex production lines for each tracer

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

3Measurement precision

If tumor-specific radiopharmaceuticals are developed, then diagnostic accuracy is improved, but manufacturing cost increases

Engineering Contradiction:
Improvediagnostic accuracyVSAvoidmanufacturing cost
Core Design Contradiction:
Measurement precisionVSEase of manufacture

Solution Approach 1:

The patent segments the radiopharmaceutical into a universal N4 compound core that can be synthesized once and reused, combined with different radionuclides as interchangeable components, reducing the overall manufacturing cost by eliminating redundant synthesis steps while maintaining high diagnostic accuracy through tumor-specific nitrogen metabolism targeting

Inventive Principle:
Principle #1Segmentation

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 N4 compounds enable improved tumor visualization with higher tumor-to-muscle ratios and faster synthesis times, enhancing the specificity and accessibility of tumor imaging while reducing production costs and time, thereby overcoming the limitations of existing radionuclide imaging methods.

Implementation Method 1

The present invention presents compounds and methods relating to a simple chelation technique for labeling agents using metallic isotopes

Methodology Applied
Scientific EffectChelation:

Data Source

PatentEP2013221B1Compositions and methods for cellular imaging and therapy
Publication Date: 2015.06.24 BOARD OF RGT THE UNIV OF TEXAS SYST
  • EP2013221B1 patent drawingFigure 1
  • EP2013221B1 patent drawingFigure 2
  • EP2013221B1 patent drawingFigure 3

AI summary

The present invention relates generally to the fields of chemistry and radionuclide imaging. More particularly, it concerns compositions, kits, and methods for imaging and therapy involving N4 compounds and derivatives.