Pentaaza Macrocyclic Complex for Chemotherapy Ototoxicity Reduction

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Solution Overview

Problem

Platinum-based chemotherapeutic agents like cisplatin cause significant toxicities such as ototoxicity, nephrotoxicity, and myelotoxicity, limiting their use in cancer treatment.

Innovation Solution

Administer a therapeutically effective amount of a pentaaza macrocyclic ring complex, such as GC4419, prior to, concomitantly with, or after platinum-based chemotherapy to reduce toxic effects.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If platinum-based chemotherapeutic agents are administered to treat cancer, then cancer treatment effectiveness is improved, but toxic effects such as ototoxicity, nephrotoxicity, and myelotoxicity increase

Engineering Contradiction:

Improvecancer treatment effectivenessVSAvoidtoxic effects

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent introduces a pentaaza macrocyclic ring complex as an intermediary substance that selectively protects normal cells from platinum-based chemotherapeutic agents. This mediator compound binds to the chemotherapeutic agent or interacts with cellular targets to prevent direct toxic damage to healthy tissues while allowing the chemotherapeutic agent to maintain its anticancer activity. The macrocyclic complex acts as a protective intermediary that modulates the interaction between the chemotherapeutic agent and cellular components, thereby reducing ototoxicity, nephrotoxicity, and myelotoxicity without compromising cancer treatment effectiveness.

Inventive Principle:

Principle #24Intermediary (Mediator)

2Productivity

If the dose of platinum-based chemotherapeutic agents is increased to enhance cancer killing, then therapeutic effect is improved, but toxicity to normal tissues increases

Engineering Contradiction:

Improvecancer cell killing efficiencyVSAvoidtissue toxicity

Core Design Contradiction:

ProductivityVSObject-affected harmful factors

Solution Approach 1:

The patent applies local quality by creating differential protection: the pentaaza macrocyclic ring complex provides selective protection to normal tissues while leaving cancer cells vulnerable to the chemotherapeutic agent. This localized differential effect allows high doses of platinum-based agents to be administered safely, as the macrocyclic complex concentrates its protective effect in healthy tissues (kidneys, ears, bone marrow) rather than uniformly distributing throughout all cells. This enables enhanced cancer cell killing while maintaining normal tissue tolerance.

Inventive Principle:

Principle #3Local quality

3Reliability

If platinum-based chemotherapeutic agents are used to treat cancer, then tumor response is improved, but quality of life due to side effects deteriorates

Engineering Contradiction:

Improvetumor responseVSAvoidquality of life

Core Design Contradiction:

ReliabilityVSEase of operation

Solution Approach 1:

The patent converts the harmful toxic effects of platinum-based chemotherapeutic agents into a beneficial protective mechanism. The pentaaza macrocyclic ring complex, when administered with the chemotherapeutic agent, transforms what would be damaging interactions into a protective effect. The macrocyclic complex binds to or interacts with the chemotherapeutic agent in a way that neutralizes its toxic effects on normal tissues while preserving its anticancer activity. This converts the harmful toxicity into a beneficial protective interaction, thereby improving quality of life without compromising tumor response.

Inventive Principle:

Principle #22Blessing in disguise (Convert harm into benefit)

Data Source

PatentUS20250387406A1Therapy for reduced ototoxicity from chemotherapeutic agent with pentaaza macrocyclic ring complex

Publication Date: 2025.12.25 BIOSSIL INC

AI summary

A method of treating and/or reducing ototoxicity caused by a chemotherapeutic agent in a mammalian subject, comprising administering to the subject a therapeutically effective amount of a chemotherapeutic agent, and administering to the subject a therapeutically effective amount of a pentaaza macrocyclic ring complex corresponding to the Formula (I) below, prior to, concomitantly with, or after administration of the chemotherapeutic agent, whereby ototoxicity of the chemotherapeutic agent is decreased: