LAG-3 Binding Members in CH3 Domain for Cancer Therapy

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Solution Overview

Problem

Current anti-LAG-3 therapies for cancer treatment are limited, with few options in clinical testing and none approved for therapy, highlighting a need for additional molecules that can effectively target LAG-3 in cancer therapy.

Innovation Solution

Development of specific binding members, such as antibody molecules or fragments, with high affinity for LAG-3, specifically designed to bind to the CH3 domain, which include antigen-binding sites in structural loops, to inhibit LAG-3 activity and enhance T cell activation.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Adaptability or versatility

If conventional anti-LAG-3 therapies are used, then immune suppression is targeted, but the number of available therapeutic options is limited

Engineering Contradiction:
Improvenumber of therapeutic optionsVSAvoidefficacy of LAG-3 targeting
Core Design Contradiction:
Adaptability or versatilityVSReliability

Solution Approach 1:

The patent segments the antibody molecule into distinct functional domains, specifically placing the LAG-3 antigen-binding site within the CH3 domain rather than the conventional variable region. This segmentation creates novel binding members with unique structural characteristics that expand the repertoire of available LAG-3 targeted therapies

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The invention moves the antigen-binding site from the traditional N-terminal variable region to the C-terminal CH3 domain, representing a dimensional shift in antibody architecture. This repositioning creates new therapeutic modalities with potentially different pharmacokinetic and pharmacodynamic properties, thereby increasing adaptability of treatment options

Inventive Principle:
Principle #17Another dimension (Dimensionality change)

2Reliability

If LAG-3 binding members are designed with antigen-binding sites in CH3 domain structural loops, then high affinity binding is achieved, but structural complexity increases

Engineering Contradiction:
Improvebinding affinityVSAvoidantibody structure
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent applies local quality by concentrating the antigen-binding functionality specifically within the structural loops of the CH3 domain, while the rest of the antibody structure maintains conventional configuration. This localized functional assignment achieves high binding affinity through optimized local interactions without requiring global structural complexity

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The CH3 domain, traditionally serving as a constant region involved in effector functions, is赋予 dual functionality by incorporating LAG-3 binding capability. This multi-functionality reduces the need for separate variable region elements, potentially simplifying overall molecular design while achieving high affinity binding

Inventive Principle:
Principle #6Universality (Multi-functionality)

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

These specific binding members demonstrate high affinity and activity in T cell activation assays, showing potential for improved efficacy in reducing tumour growth by overcoming LAG-3-mediated immune suppression and reactivating anti-tumour responses.

Implementation Method 1

specific binding members which bind to lymphocyte-activation gene 3 (LAG-3)... comprise a LAG-3 antigen-binding site

Methodology Applied
Scientific EffectAntigen-antibody binding: Adsorption

Data Source

PatentEP3472206B1LAG-3 binding members
Publication Date: 2025.01.15 INVOX PHARMA LTD
  • EP3472206B1 patent drawingFigure 1A
  • EP3472206B1 patent drawingFigure 1B
  • EP3472206B1 patent drawingFigure 2

AI summary

The present invention relates to specific binding members which bind to lymphocyte- activation gene 3 (LAG-3). The specific binding members preferably comprise a LAG-3 antigen-binding site which may be located in two or more structural loops of a CH3 domain of the specific binding member. The specific binding members of the invention find application, for example, in cancer therapy.