Bispecific Molecule Targeting TLR9 and CD32 for Allergy Treatment

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Solution Overview

Problem

Current treatments for allergies, such as immunotherapy, are only moderately effective and often come with side effects due to the low affinity of IgG antibodies for CD32 on immune cells, and there is a need for improved molecules that can induce Th1 responses to effectively treat allergic diseases.

Innovation Solution

Development of molecules with binding specificity to Toll-like Receptor 9 (TLR9) and CD32, incorporating T cell antigen epitopes, which activate allergen-specific Th1 cells without activating mast cells or B cells, promoting internalization and presentation of epitopes on MHC class II molecules to induce Th1 memory responses.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If classical immunotherapy using allergens is used, then IgG antibody production is increased, but the treatment effectiveness remains moderate due to low affinity of IgG for CD32 on immune cells

Engineering Contradiction:
Improvetreatment effectivenessVSAvoidlow affinity of IgG for CD32
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent creates a composite vaccine structure combining allergen peptides with TLR9-stimulating CpG motifs. This composite formulation enhances the immune response by simultaneously engaging both antigen-specific B cells and TLR9-expressing dendritic cells, overcoming the low affinity limitation through dual-mechanism activation that reliably induces Th1 responses and IgG production

Inventive Principle:
Principle #40Composite materials

Solution Approach 2:

The patent introduces TLR9-stimulating CpG motifs as an intermediary element that mediates enhanced immune activation. These CpG motifs act as a bridge between the allergen peptides and the immune system, stimulating dendritic cells to present antigens more effectively and induce stronger Th1 responses, thereby compensating for the low affinity of IgG for CD32

Inventive Principle:
Principle #24Intermediary (Mediator)

2Reliability

If rush immunotherapy with increasing amounts of allergen is used, then treatment effectiveness is slightly improved, but side effects increase

Engineering Contradiction:
Improvetreatment effectivenessVSAvoidside effects
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent changes the formulation parameters by incorporating TLR9-stimulating CpG motifs into the vaccine composition. This parameter change allows for effective immunotherapy at lower allergen doses by enhancing immune activation through the CpG component, thereby maintaining treatment effectiveness while reducing the allergen load and associated side effects

Inventive Principle:
Principle #35Parameter changes

3Ease of operation

If subcutaneous route is used for allergen administration, then immunotherapy is delivered, but results are not always consistent across different allergic diseases

Engineering Contradiction:
Improveadministration routeVSAvoidtreatment consistency
Core Design Contradiction:
Ease of operationVSReliability

Solution Approach 1:

The patent employs a composite vaccine formulation containing both allergen peptides and TLR9-stimulating CpG motifs. This composite structure creates a more robust and consistent immune response across different allergic conditions by engaging multiple immune pathways simultaneously, thereby improving treatment consistency regardless of the administration route used

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 molecules effectively induce allergen-specific Th1 memory cells, rebalancing the immune system from IgE to IgG antibody production, potentially providing a more effective and safer treatment for allergies by targeting specific immune cells and pathways.

Implementation Method 1

Molecules with binding specificity to both, Toll-like Receptor 9 (TLR9) and CD32 containing one or more T cell antigen epitopes

Methodology Applied
Scientific EffectToll-like receptor binding:

Implementation Method 2

The molecules effectively induce allergen-specific Th1 memory cells, rebalancing the immune system from IgE to IgG antibody production

Methodology Applied
Scientific EffectAntibody-antigen binding:

Data Source

PatentEP1996230B1Bispecific molecule binding TLR9 and CD32 and comprising a t cell epitope
Publication Date: 2014.04.30 S TARGET THERAPEUTICS
  • EP1996230B1 patent drawing
  • EP1996230B1 patent drawing
  • EP1996230B1 patent drawing

AI summary

A molecule or molecule complex capable of binding to TLR9 and to CD32 comprising at least one epitope of at least one antigen, its production and its use a medicament, especially for the treatment of allergies.