Pentaaza Macrocyclic Ring Complex for Checkpoint Inhibitor Response

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Solution Overview

Problem

There is a need for enhanced cancer treatment methods that improve the efficacy of cancer cell killing, particularly when combined with immune response checkpoint inhibitors, adoptive T-cell transfer therapies, or therapeutic vaccines.

Innovation Solution

Administering a transition metal pentaaza-macrocyclic ring complex prior to, concomitantly with, or after these therapies to enhance the response of tumors to the treatments.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional cancer therapies are used alone, then treatment simplicity is maintained, but cancer cell killing efficacy is insufficient

Engineering Contradiction:
Improvecancer cell killing efficacyVSAvoidtreatment complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent combines conventional cancer therapies (chemotherapy, radiation therapy, immunotherapy) with pentaaza macrocyclic ring complex treatment into a unified therapeutic regimen. The complex acts as a sensitizing agent that enhances the efficacy of multiple different treatment modalities simultaneously, achieving superior cancer cell killing compared to any single therapy alone.

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The treatment employs a composite therapeutic approach where the pentaaza macrocyclic ring complex serves as a molecular enhancer that works synergistically with conventional therapies. This composite treatment strategy leverages the properties of multiple therapeutic agents to achieve enhanced anticancer effects while managing treatment complexity.

Inventive Principle:
Principle #40Composite materials

2Reliability

If immune checkpoint inhibitors are used alone, then immune system activation is achieved, but tumor response is insufficient

Engineering Contradiction:
Improvetumor response to immunotherapyVSAvoidcombination therapy complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The pentaaza macrocyclic ring complex is administered prior to or concomitantly with immune checkpoint inhibitors to pre-condition the tumor microenvironment. This preliminary action sensitizes tumor cells and enhances their visibility to the immune system, thereby improving the subsequent efficacy of checkpoint inhibitor therapy.

Inventive Principle:
Principle #10Preliminary action

Solution Approach 2:

The pentaaza macrocyclic ring complex acts as an intermediary agent that bridges conventional therapies and immune checkpoint inhibitors. It modifies the tumor microenvironment and enhances immune cell infiltration, serving as a mediator that amplifies the interaction between the immune system and tumor cells.

Inventive Principle:
Principle #24Intermediary (Mediator)

3Reliability

If higher doses of checkpoint inhibitors are administered, then immune response is enhanced, but treatment cost and side effects increase

Engineering Contradiction:
Improveimmune response effectivenessVSAvoidtreatment side effects and cost
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent changes the therapeutic parameters by introducing the pentaaza macrocyclic ring complex, which alters the dose-response relationship of checkpoint inhibitors. The complex enables effective immune response at lower or standard doses of checkpoint inhibitors, thereby reducing treatment-related side effects and costs while maintaining or enhancing therapeutic effectiveness.

Inventive Principle:
Principle #35Parameter changes

Data Source

PatentUS12551581B2Combination cancer immunotherapy with pentaaza macrocyclic ring complex
Publication Date: 2026.02.17 BIOSSIL INC
  • US12551581B2 patent drawing
  • US12551581B2 patent drawing
  • US12551581B2 patent drawing

AI summary

A method of treating a cancer in a mammalian subject afflicted with the cancer, includes administering to the subject an immune checkpoint inhibitor, and administering to the subject a pentaaza macrocyclic ring complex corresponding to the formula (I) below, prior to, concomitantly with, or after administration of the immune checkpoint inhibitor, to increase the response of the cancer to the immune checkpoint inhibitor.