HDAC3 Inhibitor–Checkpoint Blockade Combination for MHC II Expression

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Solution Overview

Problem

Existing cancer treatments, particularly for immune-suppressive cancers, are ineffective, necessitating the development of combination therapies that harness the immune system to target cancer cells.

Innovation Solution

Combining a selective histone deacetylase 3 (HDAC3) inhibitor with an immunotherapy agent, such as monoclonal antibodies to PD-1, PD-L1, or CTLA-4, to increase MHC class II expression, enhancing the immune response against cancer cells.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional cancer treatments are used, then treatment simplicity is maintained, but treatment effectiveness is insufficient for immune-suppressive cancers

Engineering Contradiction:
Improvetreatment effectivenessVSAvoidtherapy complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent combines a selective HDAC3 inhibitor with an immune checkpoint inhibitor in a single treatment regimen. The HDAC3 inhibitor increases MHC class II expression on antigen-presenting cells, while the immune checkpoint inhibitor enhances T-cell activation. This combination therapy resolves the contradiction by merging two mechanisms that work synergistically to overcome immune suppression in cancer, achieving superior effectiveness compared to monotherapies while maintaining a manageable treatment complexity through coordinated administration of both agents.

Inventive Principle:
Principle #5Merging (Combining)

2Reliability

If selective HDAC3 inhibitor is used alone, then MHC class II expression is increased, but overall immune response against cancer is insufficient

Engineering Contradiction:
Improveimmune response effectivenessVSAvoidcombination therapy complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The HDAC3 inhibitor acts as an intermediary that prepares the immune system for enhanced response by upregulating MHC class II expression on antigen-presenting cells. This intermediary effect creates a more favorable immune microenvironment that amplifies the subsequent action of the immune checkpoint inhibitor. The combination resolves the contradiction by using the HDAC3 inhibitor as a facilitator that enables the immune checkpoint inhibitor to achieve stronger anti-tumor immunity, with both agents contributing to a coordinated immunotherapeutic effect.

Inventive Principle:
Principle #24Intermediary (Mediator)

Data Source

PatentEP3737362B1Combination of a selective histone deacetylase 3 (HDAC3) inhibitor and an immunotherapy agent for the treatment of cancer
Publication Date: 2025.10.15 KDAC THERAPEUTICS INC
  • EP3737362B1 patent drawingFigure 1A~1B
  • EP3737362B1 patent drawingFigure 2A~2B
  • EP3737362B1 patent drawingFigure 3A~3B

AI summary

Compositions and kits comprising a selective HDAC3 inhibitor in combination with an immunotherapy agent (e.g. an immune checkpoint inhibitor) for use in the treatment of cancer.