Peptide-Enzyme Composition for MSU Crystal Removal in Gout

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Solution Overview

Problem

Current treatments for gout primarily focus on alleviating symptoms rather than addressing the root cause, and they often come with side effects such as immune rejection reactions and inflammatory responses, lacking a fundamental solution for eliminating monosodium urate (MSU) crystals.

Innovation Solution

A pharmaceutical composition comprising peptides specifically coupling to MSU crystals and enzymes like uricase, rasburicase, or urease, which are coupled to a support or linker to target and dissolve MSU crystals in the joint fluid, minimizing damage to other proteins and avoiding immune reactions.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Object-affected harmful factors

If conventional pain relievers or anti-inflammatory agents are administered, then acute gout symptoms are alleviated, but the fundamental cause (MSU crystals) is not removed and side effects occur

Engineering Contradiction:
Improvegout symptomsVSAvoidfundamental treatment effectiveness
Core Design Contradiction:
Object-affected harmful factorsVSReliability

Solution Approach 1:

The invention extracts and removes the harmful MSU crystals from the joint cavity through enzymatic degradation (using uricase or urease to convert MSU to soluble substances) and physical extraction methods, rather than merely suppressing symptoms. This directly eliminates the root cause of gout attacks.

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The invention introduces enzymatic agents (uricase, urease) or chelating agents as intermediaries that facilitate the conversion and removal of MSU crystals. These intermediaries enable the transformation of insoluble MSU into soluble forms that can be safely excreted, providing a bridge between the harmful crystal and safe elimination.

Inventive Principle:
Principle #24Intermediary (Mediator)

2Reliability

If lifestyle changes are implemented to lower urea concentration, then fundamental treatment is achieved, but treatment time is excessively long and dramatic effect cannot be expected for acute gout

Engineering Contradiction:
Improvefundamental treatment effectivenessVSAvoidtreatment duration
Core Design Contradiction:
ReliabilityVSLoss of time

Solution Approach 1:

The invention performs preliminary enzymatic conversion of MSU crystals to soluble substances before excretion, preparing the harmful crystals for rapid elimination. This preliminary action accelerates the natural process that would otherwise take extended time through lifestyle modifications alone.

Inventive Principle:
Principle #10Preliminary action

Solution Approach 2:

The invention changes the chemical parameters of MSU crystals through enzymatic reactions (converting insoluble MSU to soluble allantoin or other metabolites), fundamentally altering the solubility and excretability of the crystals. This parameter change enables rapid removal rather than slow gradual reduction.

Inventive Principle:
Principle #35Parameter changes

3Reliability

If external enzymes are introduced to dissolve MSU crystals, then crystal removal is achieved, but immune rejection reactions and inflammatory responses occur

Engineering Contradiction:
ImproveMSU crystal removal effectivenessVSAvoidimmune rejection reaction
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The invention modifies the source and characteristics of enzymes used, transitioning from non-human sources that trigger immune responses to human-derived or human-compatible enzymatic agents. This parameter change in enzyme origin and compatibility reduces immunogenicity while maintaining crystalline degradation effectiveness.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The invention uses human-derived enzymes or enzymes with sequences similar to human endogenous enzymes, creating a biological copy that the immune system recognizes as self rather than foreign. This copying approach eliminates immune rejection while preserving the desired enzymatic function.

Inventive Principle:
Principle #26Copying

4Reliability

If enzymes are administered to remove MSU crystals, then crystal dissolution is achieved, but enzymes may damage other proteins in the body

Engineering Contradiction:
ImproveMSU crystal dissolution effectivenessVSAvoiddamage to other proteins
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The invention employs localized administration of enzymes directly into the affected joint cavity, ensuring high concentration of enzymatic activity precisely where MSU crystals are present. This local quality approach concentrates the therapeutic effect at the target site while minimizing systemic exposure and potential damage to other proteins throughout the body.

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The invention introduces targeting moieties or uses physical containment strategies as intermediaries to guide enzymes specifically to MSU crystals. This intermediary mechanism ensures enzymes act selectively on the intended target (MSU) rather than indiscriminately degrading other proteins in the joint or systemically.

Inventive Principle:
Principle #24Intermediary (Mediator)

Data Source

PatentUS12097247B2Pharmaceutical composition and kit for treating gout
Publication Date: 2024.09.24 IND ACADEMIC COOP FOUND YONSEI UNIV
  • US12097247B2 patent drawing
  • US12097247B2 patent drawing
  • US12097247B2 patent drawing

AI summary

The present invention relates to a pharmaceutical composition for treating gout and a gout treatment kit. According to an embodiment of the present invention, a pharmaceutical composition for treating gout comprising a probe containing at least one or more peptides specifically coupled to a monosodium urate (MSU) crystals and a first enzyme which is coupled to the probe and reacts with the target MSU crystal coupled to the probe or urea of surrounding joint fluid to remove the target MSU crystal is provided.