Mucin-Binding Antibody Conjugates for Respiratory Mucosal Retention

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Solution Overview

Problem

Existing biopharmaceuticals, such as antipathogenic antibodies, face low efficacy in clinical trials due to high dilution effects from muco-ciliary clearance in the respiratory system, necessitating improved methods to enhance their inherent virus-, bacterium-, allergen-, or sperm-cell binding efficacy.

Innovation Solution

A conjugation product comprising an antigen binding moiety covalently bound to a mucin binding moiety, which can be directly bound or linked via a linker, excluding certain specific antigen binding moieties and virus binding moieties, enhances the efficacy of biopharmaceuticals by increasing their interaction with mucosal tissues.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of operation

If biopharmaceuticals are administered via aerosol deposition in the respiratory system, then the route of administration is simple and dosing is easy, but high dilution effects occur due to muco-ciliary clearance leading to low efficacy

Engineering Contradiction:
Improveroute of administration and dosing simplicityVSAvoidbiopharmaceutical efficacy
Core Design Contradiction:
Ease of operationVSReliability

Solution Approach 1:

The patent combines an antigen binding moiety (such as an antibody or viral vector) with a mucin binding moiety to form a conjugation product. This merging allows the biopharmaceutical to bind to mucin proteins in the respiratory tract, preventing dilution by muco-ciliary clearance and thereby maintaining efficacy while preserving the simplicity of aerosol administration

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The mucin binding moiety acts as an intermediary that facilitates retention of the antigen binding moiety in the respiratory tract. By binding to mucin proteins, the conjugation product serves as a mediator that prevents rapid clearance and enhances local efficacy without complicating the administration process

Inventive Principle:
Principle #24Intermediary (Mediator)

2Reliability

If a conjugation product comprises an antigen binding moiety covalently bound to a mucin binding moiety, then the inherent binding efficacy is enhanced, but the structural complexity increases

Engineering Contradiction:
Improveinherent binding efficacyVSAvoidconjugation product structure
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The conjugation product is segmented into distinct functional moieties: an antigen binding moiety responsible for pathogen recognition and a mucin binding moiety responsible for mucosal retention. This segmentation allows each component to perform its specific function efficiently while maintaining overall structural organization and manageable complexity

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The invention creates a composite molecular structure by covalently combining different protein moieties (antigen binding and mucin binding). This composite approach integrates multiple functions into a single conjugation product, enhancing binding efficacy while the modular nature keeps the structural complexity manageable through standardized conjugation methodologies

Inventive Principle:
Principle #40Composite materials

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 conjugation product increases the efficacy of therapeutic cytokines, protein vaccines, and other bioactive substances by trapping pathogens and reducing viral shedding, while minimizing impact on treated individuals, and can be used therapeutically in infected patients.

Implementation Method 1

a conjugation product comprising an antigen binding moiety and a mucin binding moiety which is covalently bound to the antigen binding moiety

Methodology Applied
Scientific EffectBinding:

Implementation Method 2

The binding between the antigen binding moiety and the mucin binding moiety can be a direct covalent binding or a binding via a linker

Methodology Applied
Scientific EffectCovalent binding: Chemical Bonding

Data Source

PatentEP4684804A1Conjugation product comprising an antigen binding moiety and a mucin binding moiety
Publication Date: 2026.01.28 FORSCHUNGSVERBUND BERLIN EV
  • EP4684804A1 patent drawingFigure 1
  • EP4684804A1 patent drawingFigure 2
  • EP4684804A1 patent drawingFigure 3

AI summary

The present invention relates to a conjugation product comprising an antigen binding moiety and a mucin binding moiety covalently bound to the antigen binding moiety. Due to the mucin binding moiety, the antigen binding efficacy of the antigen binding moiety is significantly increased.