Anti-c-Met Antibody CDR Optimization for Binding Affinity and Immunogenicity

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Solution Overview

Problem

Current anti-cancer therapies targeting c-Met, a receptor tyrosine kinase involved in cancer development and resistance to other drugs, require additional effective anti-c-Met antibodies and compositions to overcome limitations in antigen binding affinity and immunogenicity.

Innovation Solution

Development of an anti-c-Met antibody or antigen-binding fragment with specific heavy and light chain complementarity determining regions (CDRs) sequences, including CDR-H1, CDR-H2, CDR-H3, CDR-L1, CDR-L2, and CDR-L3, which are optimized for humanization to enhance binding affinity and reduce immunogenicity, and a pharmaceutical composition for preventing or treating cancer.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If existing anti-c-Met antibodies are used, then c-Met binding is achieved, but binding affinity is insufficient and immunogenicity remains high

Engineering Contradiction:
Improvebinding affinityVSAvoidimmunogenicity
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies parameter changes by optimizing the amino acid sequences of CDR-H1, CDR-H2, CDR-H3, CDR-L1, CDR-L2, and CDR-L3 regions to achieve higher binding affinity while reducing immunogenicity. Specific amino acid substitutions and optimizations in these complementarity determining regions enable the antibody to bind more effectively to c-Met while being more suitable for human therapeutic use.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent creates a composite antibody structure by combining optimized heavy chain variable region (comprising CDR-H1, CDR-H2, CDR-H3) with light chain variable region (comprising CDR-L1, CDR-L2, CDR-L3) to form an antibody with enhanced properties. This composite approach integrates multiple optimized CDR sequences to achieve both high affinity and low immunogenicity simultaneously.

Inventive Principle:
Principle #40Composite materials

2Reliability

If additional anti-c-Met antibodies are developed, then therapeutic effectiveness improves, but development complexity increases

Engineering Contradiction:
Improvetherapeutic effectivenessVSAvoidantibody structure complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent segments the antibody structure into distinct complementarity determining regions (CDR-H1, CDR-H2, CDR-H3, CDR-L1, CDR-L2, CDR-L3) that can be independently optimized. This segmentation allows for systematic development of multiple antibody variants with different CDR combinations, enabling therapeutic effectiveness improvement while managing development complexity through modular design.

Inventive Principle:
Principle #1Segmentation

Data Source

PatentEP2764024B1Anti c-met antibody and uses thereof
Publication Date: 2019.08.28 SAMSUNG ELECTRONICS CO LTD
  • EP2764024B1 patent drawingFigure 1
  • EP2764024B1 patent drawingFigure 2
  • EP2764024B1 patent drawingFigure 3

AI summary

An anti c-Met antibody or antibody fragment and pharmaceutical composition comprising same, as well as a method for preventing and treating cancer by administering the antibody to a subject.