Antibody-Drug Conjugates Targeting Lipopolysaccharides for Bacterial Infections

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Solution Overview

Problem

The emergence of antibiotic-resistant bacterial strains complicates the treatment of infections, leading to increased disability and death, and existing antibiotic use contributes to resistance, necessitating new approaches for treating, preventing, and diagnosing bacterial infections.

Innovation Solution

Development of antibody molecule-drug conjugates (ADCs) that bind to Gram-negative bacteria by targeting lipopolysaccharides, comprising antimicrobial peptides covalently coupled to anti-LPS antibodies, improving binding affinity and inhibitory properties.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If antibiotics are used to treat bacterial infections, then infections can be treated, but antibiotic-resistant bacterial strains emerge

Engineering Contradiction:
Improveinfection treatment effectivenessVSAvoidbacterial resistance
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent creates an antibody-drug conjugate by covalently coupling antimicrobial peptides to anti-LPS antibodies. This composite structure combines the specific binding capability of antibodies with the antimicrobial activity of peptides, creating a targeted therapy that delivers the antimicrobial agent directly to Gram-negative bacteria while reducing systemic exposure and resistance development

Inventive Principle:
Principle #40Composite materials

Solution Approach 2:

The anti-LPS antibody serves as an intermediary that specifically recognizes and binds to lipopolysaccharides on the surface of Gram-negative bacteria. This intermediary function enables selective delivery of the antimicrobial peptide to the target bacteria, improving treatment effectiveness while minimizing off-target effects that contribute to resistance

Inventive Principle:
Principle #24Intermediary (Mediator)

2Reliability

If antimicrobial peptides are used alone, then they can inhibit bacteria, but they have limited stability and binding affinity

Engineering Contradiction:
Improveantimicrobial activityVSAvoidpeptide stability
Core Design Contradiction:
ReliabilityVSStability of the object's composition

Solution Approach 1:

The patent merges the antimicrobial peptide with the anti-LPS antibody through covalent coupling to form an antibody-drug conjugate. This combination preserves the antimicrobial activity of the peptide while the antibody portion provides enhanced stability, prolonged circulation time, and targeted delivery to bacteria

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

By conjugating the peptide to the antibody, the patent fundamentally changes the pharmacokinetic parameters of the antimicrobial agent. The conjugate exhibits improved stability, altered distribution patterns, and enhanced binding affinity through the antibody's high-affinity interaction with LPS, while maintaining the peptide's bactericidal activity

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 ADCs demonstrate enhanced ability to inhibit and reduce the viability of Gram-negative bacteria, potentially offering a more effective treatment option with reduced resistance probability and improved stability compared to standalone antimicrobial peptides.

Implementation Method 1

antibody molecule-drug conjugates (ADC) that bind to Gram-negative bacteria, e.g., lipopolysaccharides (LPS) on the outer membrane of Gram-negative bacteria

Methodology Applied
Scientific EffectAntigen-antibody binding:

Implementation Method 2

comprise an antimicrobial peptide site-specifically coupled (e.g., conjugated) to an anti-LPS antibody molecule

Methodology Applied
Scientific EffectCovalent bonding: Chemical Bonding

Data Source

PatentEP3571223B1Antibody molecule-drug conjugates and uses thereof
Publication Date: 2024.09.18 VISTERRA INC
  • EP3571223B1 patent drawingFigure 1
  • EP3571223B1 patent drawingFigure 2~3
  • EP3571223B1 patent drawingFigure 4

AI summary

Antibody molecule-drug conjugates (ADCs) that specifically bind to lipopolysaccharides (LPS) are disclosed. The antibody molecule-drug conjugates can be used to treat, prevent, and/or diagnose bacterial infections and related disorders.