Multivalent Glyco-Complex for Cancer Imaging Contrast

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Solution Overview

Problem

Current cancer diagnosis methods using glucose analogs like 18F-FDG face challenges such as cumbersome preparation processes, high background signals in normal tissues like the brain and heart, and low specificity in differentiating between tumor and inflamed tissues.

Innovation Solution

A multivalent glyco-complex with a molecular structure containing three glucose molecules connected to a central nitrogen atom via a linker and a chelating group, which can be radiolabeled for improved cancer imaging discrimination.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Measurement precision

If 18F-FDG is used as a contrast agent for cancer diagnosis, then cancer detection capability is achieved, but background signals in normal tissues like brain and heart increase, reducing imaging discrimination

Engineering Contradiction:

Improvecancer detection capabilityVSAvoidbackground signals in normal tissues

Core Design Contradiction:

Measurement precisionVSObject-generated harmful factors

Solution Approach 1:

The patent divides the glucose analog structure into multiple segments: a core structure with multiple glucose units attached to a central chelating agent. This multivalent structure allows the compound to maintain glucose-like properties for tumor cell recognition while the chelating agent enables selective radionuclide attachment, thereby improving tumor-to-background contrast ratio

Inventive Principle:

Principle #1Segmentation

Solution Approach 2:

The patent creates a composite molecular structure combining multiple glucose units with a central chelating agent (such as DOTA or NOTA). This composite structure integrates the tumor-targeting capability of glucose analogs with the radionuclide-chelating functionality, achieving both high tumor uptake and reduced background signal through optimized radiotracer design

Inventive Principle:

Principle #40Composite materials

2Quantity of substance

If 18F-FDG preparation process is implemented, then radiotracer production is achieved, but preparation time and process complexity increase significantly

Engineering Contradiction:

Improveradiotracer productionVSAvoidpreparation time

Core Design Contradiction:

Quantity of substanceVSLoss of time

Solution Approach 1:

The patent extracts the fluorination step from the synthesis pathway by using pre-synthesized glucose analog precursors that can be directly radiolabeled. This eliminates the need for time-consuming nucleophilic fluorination and multiple purification steps required in traditional 18F-FDG synthesis, significantly reducing preparation time while maintaining radiotracer production capability

Inventive Principle:

Principle #2Taking out (Extraction)

Solution Approach 2:

The patent employs pre-synthesized glucose analog precursors with built-in chelating agents that are ready for direct radionuclide labeling. This preliminary preparation of modular precursors allows for rapid radiotracer production through simple radiolabeling steps, avoiding the lengthy multi-step synthesis and purification process of conventional 18F-FDG preparation

Inventive Principle:

Principle #10Preliminary action

3Measurement precision

If 18F-FDG is used for cancer diagnosis, then glucose-metabolizing tumors can be detected, but specificity decreases due to uptake in inflamed tissues

Engineering Contradiction:

Improvetumor detection capabilityVSAvoidspecificity in differentiating tumor and inflamed tissue

Core Design Contradiction:

Measurement precisionVSReliability

Solution Approach 1:

The patent modifies the local chemical structure by attaching multiple glucose units to a central chelating agent, creating a multivalent configuration. This structural modification changes the biological interaction profile, enhancing affinity for tumor cells while reducing non-specific uptake in inflamed tissues, thereby improving diagnostic specificity

Inventive Principle:

Principle #3Local quality

Solution Approach 2:

The patent changes the molecular parameters of the glucose analog by varying the number of glucose units, the type of central chelating agent, and the linker structures. These parameter modifications optimize the radiotracer's biological distribution, achieving higher tumor-to-background contrast and improved specificity for distinguishing tumor from inflammatory lesions

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

The multivalent glyco-complex demonstrates enhanced specificity and sensitivity in cancer imaging, reducing background signals in normal tissues and improving the contrast between tumor and normal tissues, thereby aiding in more accurate cancer diagnosis and treatment assessment.

Implementation Method 1

a chelating group G; wherein the linker contains at least a polyethylene glycol (PEG) molecule, and the chelating group G connects to the linker

Methodology Applied

Scientific EffectChelation:

Data Source

PatentUS20250135044A1Multivalent glyco-complex, imaging agent and uses thereof

Publication Date: 2025.05.01 NAT ATOMIC RES INST

AI summary

The present disclosure relates to a multivalent glyco-complex, an imaging agent and uses thereof. The multivalent glyco-complex includes a plurality of glucose molecules, each of which connects to a central nitrogen atom through a linker, and a chelating group G. The multivalent glyco-complex can be used as an imaging agent to diagnose cancers and to evaluate the therapeutic efficacy of cancers.