C2b-Targeting Binding Molecule for Selective Complement Inhibition

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Solution Overview

Problem

Current therapies for inhibiting complement activation in inflammatory diseases often come with the risk of increased susceptibility to infections, as they can impair the body's ability to defend against microorganisms, and existing antibodies targeting C2 have not been effective in blocking its activation.

Innovation Solution

Development of a binding molecule comprising specific immunoglobulin heavy and light chain variable regions that selectively target the C2b domain of human complement factor C2, inhibiting complement activation while preserving the alternative pathway's functionality to maintain immune defense.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Object-affected harmful factors

If complement activation is inhibited to treat inflammatory diseases, then complement-mediated tissue damage is reduced, but susceptibility to infections increases

Engineering Contradiction:
Improvecomplement-mediated tissue damageVSAvoidsusceptibility to infections
Core Design Contradiction:
Object-affected harmful factorsVSReliability

Solution Approach 1:

The binding molecule specifically targets the C2b domain of complement factor C2, creating a localized inhibition effect on the classical and lectin pathways while leaving the alternative pathway intact. This selective local action reduces complement-mediated tissue damage in inflammatory diseases without completely suppressing the complement system, thereby maintaining immune defense against infections

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The invention segments the complement system inhibition by targeting only a specific component (C2b domain) rather than inhibiting the entire complement cascade. This segmentation allows differential control of complement pathways, enabling therapeutic inhibition of harmful pathways while preserving protective functions

Inventive Principle:
Principle #1Segmentation

2Object-affected harmful factors

If existing antibodies targeting C2 are used to inhibit complement activation, then complement-mediated damage is reduced, but they fail to effectively block C2 activation

Engineering Contradiction:
Improvecomplement-mediated damageVSAvoidblocking effectiveness on C2 activation
Core Design Contradiction:
Object-affected harmful factorsVSManufacturing precision

Solution Approach 1:

The invention replaces existing antibody-based approaches with a novel binding molecule that has proven effectiveness in blocking C2 activation. The binding molecule comprises specifically engineered immunoglobulin heavy and light chain variable regions that target the C2b domain, providing superior blocking effectiveness compared to previously tested antibodies against C2

Inventive Principle:
Principle #28Mechanics substitution (Replace mechanical system)

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 binding molecule effectively treats conditions like myasthenia gravis, haemolytic anaemia, and ischemia-reperfusion injuries by limiting complement-mediated damage without significantly increasing the risk of infections, by inhibiting the classical and lectin pathways while sparing the alternative pathway.

Implementation Method 1

a binding molecule that binds to human complement factor C2... wherein the binding molecule comprises an immunoglobulin heavy chain variable region and an immunoglobulin light chain variable region

Methodology Applied
Scientific EffectAntibody-antigen binding:

Data Source

PatentEP3725803B1Binding molecules that bind human complement factor c2b and uses thereof
Publication Date: 2021.12.15 BROTEIO PHARMA
  • EP3725803B1 patent drawingFigure 1
  • EP3725803B1 patent drawingFigure 2
  • EP3725803B1 patent drawingFigure 3A

AI summary

The invention relates to means and methods that relate to binding molecules that bind human complement factor C2. Specific binding molecules are described with specific C2 activity inhibiting properties. Such binding molecules are useful in the treatment of symptoms of various human disease among which there is inflammatory disease, neuro-inflammatory disease or ischemia-reperfusion (I/R) injury.