Dual-Function Antigen-Binding Molecules for Cancer-Cell Peptide Delivery

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Solution Overview

Problem

Existing anti-cancer therapies lack effective methods to deliver immunogenic peptides specifically to cancer cells, thereby limiting immune surveillance and cancer cell killing.

Innovation Solution

Development of antibodies or antigen binding fragments with inserted immunogenic peptides and cell penetration sequences, allowing targeted delivery of these peptides to cancer cells, enhancing immune response through endosomal escape or receptor-mediated transcytosis, and presentation on HLA molecules for immune cell recognition.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If immunogenic peptides are delivered to cancer cells using existing anti-cancer therapies, then immune surveillance and cancer cell killing are enhanced, but effective delivery methods are lacking

Engineering Contradiction:

Improveimmune surveillance effectivenessVSAvoiddelivery method availability

Core Design Contradiction:

ReliabilityVSEase of manufacture

Solution Approach 1:

The patent combines an immunogenic peptide with an antibody molecule to create a dual-function antigen binding molecule. The antibody component provides targeted delivery to cancer cells expressing specific antigens, while the immunogenic peptide component stimulates immune response. This merging resolves the contradiction by integrating delivery capability (from antibody) with immune surveillance enhancement (from immunogenic peptide) into a single molecule.

Inventive Principle:

Principle #5Merging (Combining)

Solution Approach 2:

The antibody serves as an intermediary that mediates the delivery of the immunogenic peptide to cancer cells. The antibody's antigen-binding capability allows it to specifically target cancer cells, while its structure enables it to carry and deliver the immunogenic peptide to the target cell surface or interior, thereby solving the delivery method availability problem.

Inventive Principle:

Principle #24Intermediary (Mediator)

2Ease of operation

If immunogenic peptides are inserted into antibody variable regions, then targeted delivery to cancer cells is achieved, but CDR sequence is removed

Engineering Contradiction:

Improvetargeted delivery capabilityVSAvoidantibody structure modification

Core Design Contradiction:

Ease of operationVSDevice complexity

Solution Approach 1:

The patent applies local quality by making modifications only to specific regions of the antibody (variable regions and CDRs) rather than the entire molecule. The immunogenic peptide is inserted into the variable region, and CDR sequences are selectively removed or modified only where necessary, preserving the overall antibody structure and function while achieving targeted delivery capability.

Inventive Principle:

Principle #3Local quality

Solution Approach 2:

The antibody structure is segmented into functional regions (variable regions, CDRs, constant regions), with modifications applied selectively to the variable regions where the immunogenic peptide is inserted. This segmentation allows the invention to achieve targeted delivery without compromising the essential antigen-binding function provided by the CDRs, as only non-essential CDR sequences are removed.

Inventive Principle:

Principle #1Segmentation

3Adaptability or versatility

If CDR sequences are removed for peptide insertion, then peptide delivery is enabled, but antigen binding function may be affected

Engineering Contradiction:

Improvepeptide delivery functionVSAvoidantigen binding affinity

Core Design Contradiction:

Adaptability or versatilityVSReliability

Solution Approach 1:

Inventive Principle:

Principle #3Local quality

Solution Approach 2:

The patent applies partial action by removing only specific CDR sequences that are less critical for antigen binding, rather than removing all CDRs. This selective removal enables peptide insertion while maintaining sufficient antigen binding function. The invention also applies excessive action by testing multiple CDR removal combinations to ensure optimal balance between peptide delivery and antigen binding.

Inventive Principle:

Principle #16Partial or excessive action

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

Enhances immune surveillance and killing of cancer cells by delivering immunogenic peptides to the cytoplasm or dendritic cells, increasing immune recognition and response against cancer.

Implementation Method 1

the antibody or antigen binding fragment thereof further comprises a cell penetration sequence that targets the antibody or antigen binding fragment thereof to a cytoplasm of a cell binding the antibody or antigen binding fragment thereof

Methodology Applied

Scientific EffectEndosomal escape:

Implementation Method 2

The antibody devoid of the immunogenic peptide is endocytosed into an endosomal pathway and is delivered to the cytoplasm

Methodology Applied

Scientific EffectEndocytosis:

Implementation Method 3

presentation on HLA molecules for immune cell recognition

Methodology Applied

Scientific EffectAntigen presentation:

Data Source

PatentUS20250255955A1Dual function antigen binding molecules

Publication Date: 2025.08.14 TROJAN BIO LTD

AI summary

Antibodies or antigen binding fragments thereof comprising at least one immunogenic peptide inserted into a variable region of the antibody or antigen binding fragment thereof, wherein the insertion comprises removal of antibody or antigen binding fragment sequence are provided. Dual-function antigen binding molecules comprising an antibody or antigen binding fragment of the invention and a second antibody or antigen binding fragment thereof capable of binding an antigen overexpressed on a target cell are provided. Nucleic acid molecules encoding same, pharmaceutical compositions comprising same and methods of treating cancer by administrating same are also provided. Methods of producing antibodies or antigen binding fragments are also provided.