Antitumor Peptide Derived from Antibody CDR3 Region

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Solution Overview

Problem

Current cancer treatments face challenges with high recurrence rates and side effects, necessitating new therapeutic agents that can effectively inhibit neoplastic cell growth without severe adverse events, particularly for tumors that are resistant to existing therapies.

Innovation Solution

Development of antitumor peptides derived from the complementarity determining region of a humanized monoclonal antibody (RebMab200) that target specific cancer cells, inhibiting cell migration, invasion, and metastasis, and are designed for use in pharmaceutical compositions to treat cancer.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional cancer treatments are used, then tumor growth can be inhibited, but recurrence rates are high and severe side effects occur

Engineering Contradiction:
Improvetumor growth inhibitionVSAvoidside effects and recurrence
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent extracts the antigen-binding region (CDR3) from the complete monoclonal antibody structure to create a smaller peptide fragment. This extracted peptide retains the ability to bind to the NAPI2b transporter on tumor cells while eliminating the need for the full antibody structure, thereby reducing immunogenicity and side effects while maintaining antitumor activity

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The patent creates a simplified copy (peptide) that mimics the key functional element (antigen-binding region) of the original antibody. This peptide copy binds to the same tumor-associated antigen (NAPI2b) and elicits similar antitumor responses but with reduced immunogenicity and fewer side effects compared to the full antibody

Inventive Principle:
Principle #26Copying

2Measurement precision

If large monoclonal antibodies are used to target tumor cells, then specific binding can be achieved, but the molecules are too large for efficient penetration and distribution

Engineering Contradiction:
Improvebinding specificityVSAvoidmolecular size
Core Design Contradiction:
Measurement precisionVSLength of moving object

Solution Approach 1:

The patent extracts only the essential antigen-binding component (CDR3 region, approximately 10-20 amino acids) from the large monoclonal antibody structure. This extracted peptide maintains the ability to specifically bind to the NAPI2b transporter while being small enough (10-50 kDa) to efficiently penetrate tumor tissue and distribute throughout the body

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The patent segments the monoclonal antibody into smaller functional units, specifically isolating the CDR3 region as the active antitumor component. This segmentation creates a peptide fragment that can be synthesized and administered separately, providing both the specificity of the original antibody and the pharmacokinetic advantages of a smaller molecule

Inventive Principle:
Principle #1Segmentation

Data Source

PatentEP2654769B1Antitumor peptide derived from a complementarity determining region of a humanized monoclonal antibody to NAPI2b transporter
Publication Date: 2020.04.15 RECEPTA BIOPHARMA
  • EP2654769B1 patent drawingFigure 1A~1D
  • EP2654769B1 patent drawingFigure 2A~2D
  • EP2654769B1 patent drawingFigure 3A~3B

AI summary

Described herein is novel isolated or synthetic peptides derived from a complementarity determining region hypervariable domain amino acid sequence of a humanized monoclonal antibody to NaPi2B transporter, as well as derivatives thereof, and a pharmaceutical composition and a method for inhibiting tumor growth or treating a tumor or cancer treating using the antitumor peptides and derivatives thereof.