Multivalent Saccharide Complex for Tumor Imaging Specificity

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Solution Overview

Problem

Current glucose analogues like 18F-FDG for cancer imaging are difficult to prepare, have high background uptake in normal tissues, and low specificity, making it challenging to distinguish tumors from normal or inflammatory tissues.

Innovation Solution

A multivalent saccharide complex comprising a chelator linked with glucose molecules and a radioactive isotope, such as gallium-68, which selectively accumulates in tumor cells, enhancing signal contrast and detection efficiency.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Measurement precision

If 18F-FDG is used for cancer imaging, then glucose metabolism can be detected, but the background uptake in normal tissues is very high making it difficult to distinguish tumors

Engineering Contradiction:

Improvetumor detection accuracyVSAvoidbackground uptake in normal tissues

Core Design Contradiction:

Measurement precisionVSObject-generated harmful factors

Solution Approach 1:

The patent modifies the glucose molecule by attaching multiple glucose units (multivalent saccharide) to a chelator, creating a compound with differentiated local properties. The multivalent glucose structure maintains affinity for glucose transporters while the chelator portion enables selective radioactive labeling, thereby improving tumor-specific accumulation and reducing non-specific background uptake in normal tissues.

Inventive Principle:

Principle #3Local quality

Solution Approach 2:

The invention creates a composite molecular structure combining multiple glucose units with a chelator molecule (such as DOTA or NOTA). This composite multivalent saccharide complex integrates the glucose-metabolism-targeting capability with enhanced radioactive labeling properties, resulting in improved tumor-to-background ratio and detection precision.

Inventive Principle:

Principle #40Composite materials

2Quantity of substance

If 18F-FDG is prepared using a cyclotron, then radioactive isotope can be produced, but the preparation process is complex and time consuming

Engineering Contradiction:

Improveradioactive isotope availabilityVSAvoidsynthesis time

Core Design Contradiction:

Quantity of substanceVSLoss of time

Solution Approach 1:

The patent introduces a chelator (such as DOTA or NOTA) as an intermediary component that facilitates easier and faster radioactive labeling. The chelator serves as a mediator between the multivalent glucose structure and radioactive isotopes, enabling more efficient isotope attachment compared to direct labeling of conventional glucose analogues, thereby reducing synthesis time.

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The multivalent saccharide complex is pre-synthesized with a chelator attached before radioactive labeling. This preliminary preparation of the non-radioactive complex allows for quicker and simpler subsequent radioactive labeling procedures, reducing the overall time from isotope production to final imaging agent preparation.

Inventive Principle:

Principle #10Preliminary action

3Adaptability or versatility

If 18F-FDG is used for imaging, then glucose metabolizing tissues can be visualized, but specificity is low making it difficult to distinguish tumors from normal or inflammatory tissues

Engineering Contradiction:

Improvetissue visualization capabilityVSAvoidtumor specificity

Core Design Contradiction:

Adaptability or versatilityVSMeasurement precision

Solution Approach 1:

The patent changes key parameters of the glucose analogue by creating a multivalent structure with multiple glucose units attached to a chelator. This structural modification alters the biochemical parameters, including affinity for glucose transporters and cellular uptake characteristics, thereby enhancing tumor specificity while maintaining the ability to visualize glucose metabolizing tissues.

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 saccharide complex improves tumor detection by reducing background uptake in normal tissues and increasing tumor-to-muscle ratios, allowing for more accurate imaging and therapeutic evaluation.

Implementation Method 1

a multivalent saccharide complex comprising a chelator and at least two molecules of glucose attached to the chelator

Methodology Applied

Scientific EffectChelation:

Implementation Method 2

a radioactive isotope labeled on the compound of Formula (1)... the radioactive isotope may be rhenium-188, technetium-99m, indium-111, lutetium-177, gallium-68, yttrium 90, flurine-18, or copper-64

Methodology Applied

Scientific EffectRadioactive decay: Radioactive Decay

Data Source

PatentUS10434196B2Multivalent saccharide complex, radioactive multivalent saccharide complex contrast agent, and use thereof

Publication Date: 2019.10.08 ATOMIC ENERGY COUNCIL INSTITUTE OF NUCLEAR ENERGY RESEARCH

AI summary

Disclosed herein are a multivalent saccharide complex, a radioactive multivalent saccharide complex contrast agent and use thereof. The multivalent saccharide complex has a chelator, a linker, and glucose, and is configured to diagnose and evaluate the therapeutic effect of cancers.