Segmented Polypeptide with Cathepsin Sites for Targeted Cancer Therapy

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Solution Overview

Problem

Current cancer treatment strategies, including chemotherapy and immunotherapy, often lack selectivity, leading to significant side effects and limited efficacy due to their impact on both healthy and cancerous cells, and cancer cells can develop resistance to these treatments, necessitating a more targeted approach.

Innovation Solution

Administering a polypeptide comprising two or more peptide fragments derived from tumour antigen proteins, with exogenous cathepsin cleavage sites, in combination with an immuno-oncology agent, such as a TNFR Superfamily agonist or checkpoint inhibitor, to enhance immune therapy efficacy while reducing toxic effects.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If chemotherapy agents are used to disrupt DNA repair processes, then cancer cell growth is inhibited, but healthy cells are also damaged causing side effects

Engineering Contradiction:
Improvecancer treatment efficacyVSAvoiddamage to healthy cells
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The invention segments the treatment approach by using multiple distinct peptide fragments (at least two) derived from different tumor antigen proteins, each targeting specific tumor antigens. This segmentation allows the immune system to recognize and attack tumor cells through multiple specific pathways, achieving effective cancer treatment while maintaining selectivity and reducing damage to healthy cells.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The invention introduces peptide fragments as intermediary substances that bridge the gap between the immune system and tumor cells. These peptides serve as mediators by presenting tumor-specific antigens to the immune system, thereby activating targeted immune responses against cancer cells without requiring direct toxic intervention that would harm healthy tissues.

Inventive Principle:
Principle #24Intermediary (Mediator)

2Object-affected harmful factors

If immunotherapy is used to target tumor-specific antigens, then selectivity is improved, but cancer cells can develop resistance through mutations

Engineering Contradiction:
Improveselectivity of treatmentVSAvoidlong-term treatment efficacy
Core Design Contradiction:
Object-affected harmful factorsVSReliability

Solution Approach 1:

The invention divides the immunotherapy approach into multiple segments by using peptide fragments from at least two different tumor antigen proteins. This multi-segmented strategy targets multiple distinct tumor antigens simultaneously, making it more difficult for cancer cells to develop resistance through single mutations, thereby maintaining long-term treatment efficacy while preserving selectivity.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The invention creates a composite therapeutic approach by combining peptide fragments from different tumor antigen proteins into a single polypeptide construct. This composite structure enables simultaneous targeting of multiple tumor antigens, enhancing both selectivity and durability of the immune response against cancer cells.

Inventive Principle:
Principle #40Composite materials

3Reliability

If high doses of immuno-oncology agents are administered, then treatment efficacy is maximized, but toxic side effects increase

Engineering Contradiction:
Improvetreatment efficacyVSAvoidtoxic side effects
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The invention segments the immune activation strategy by using multiple peptide fragments that target different tumor antigens. This segmented approach distributes the immune activation across multiple specific targets, achieving maximal treatment efficacy through comprehensive tumor antigen coverage while reducing the need for high doses of immuno-oncology agents, thereby minimizing toxic side effects.

Inventive Principle:
Principle #1Segmentation

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

This combination therapy improves treatment outcomes by increasing the effectiveness of immune therapy approaches, allowing for lower doses of immuno-oncology agents and reducing toxic side effects, thereby enhancing cancer treatment efficacy and patient safety.

Implementation Method 1

one or more exogenous cathepsin cleavage site sequences located between each of the two or more peptide fragments

Methodology Applied
Scientific EffectProteolytic cleavage: Enzyme

Data Source

PatentUS20240316170A1Polypeptides for cancer treatment
Publication Date: 2024.09.26 OXFORD VACMEDIX (UK) LTD
  • US20240316170A1 patent drawing
  • US20240316170A1 patent drawing
  • US20240316170A1 patent drawing

AI summary

The present invention relates to methods, polypeptides and compositions of said polypeptides and/or their encoding nucleic acids for the prophylactic vaccination and/or therapeutic treatment of cancer, and the use of polypeptides in treating and/or preventing cancer, and/or improving the therapeutic efficacy of agents for the treatment of cancer.