Indole Anthelmintic Compositions for Resistant Liver Fluke Control

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Solution Overview

Problem

Current treatments for liver fluke infections, particularly those caused by Fasciola hepatica, face challenges due to increasing resistance to existing anthelmintics like triclabendazole, necessitating the development of alternative compounds with low side effects and effective against both mature and immature flukes without contaminating food sources.

Innovation Solution

Development of indole derivatives in oral, topical, or injectable veterinary compositions that demonstrate superior efficacy against F. hepatica, offering quick onset and long duration of activity while being safe for both animals and humans.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If existing anthelmintics like triclabendazole are used to treat liver fluke infections, then treatment efficacy is achieved, but parasite resistance increases

Engineering Contradiction:

Improvetreatment efficacyVSAvoidparasite resistance

Core Design Contradiction:

ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent applies parameter changes by developing new chemical compounds with different molecular structures (indole derivatives) compared to existing anthelmintics. This structural parameter change enables the new compounds to act through different mechanisms of action, thereby overcoming parasite resistance that has developed against traditional drugs like triclabendazole.

Inventive Principle:

Principle #35Parameter changes

2Reliability

If higher concentrations of anthelmintics are used to overcome resistance, then treatment efficacy improves, but toxic side effects increase

Engineering Contradiction:

Improvetreatment efficacyVSAvoidtoxic side effects

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent creates new chemical copies (indole derivative compounds) that mimic the desired therapeutic effect of existing anthelmintics but with modified structures. These copied compounds maintain efficacy against resistant parasites while exhibiting reduced toxicity, as demonstrated by their selective action on parasite tubulin without significant harm to host animals.

Inventive Principle:

Principle #26Copying

3Adaptability or versatility

If benzimidazole compounds are used for broad anthelmintic spectrum, then efficacy against nematodes and mature F. hepatica is achieved, but resistance to triclabendazole develops

Engineering Contradiction:

Improveanthelmintic spectrumVSAvoidsusceptibility to resistance

Core Design Contradiction:

Adaptability or versatilityVSReliability

Solution Approach 1:

The patent segments the broad anthelmintic approach into more specific compound classes (indole derivatives). Rather than relying on a single broad-spectrum class like benzimidazoles, the invention divides the therapeutic strategy into multiple distinct chemical classes with different mechanisms of action, thereby preventing the development of widespread resistance while maintaining versatility.

Inventive Principle:

Principle #1Segmentation

Data Source

PatentEP3517524B1Parasiticidal compositions comprising indole derivatives, methods and uses thereof

Publication Date: 2021.05.26 BOEHRINGER INGELHEIM ANIMAL HEALTH USA INC

Figure 1A~1F

AI summary

The invention relates to oral, topical or injectable compositions for combating liver fluke parasites in mammals, comprising at least one indole derivative active agent. The invention also provides for an improved method for eradicating and controlling liver fluke parasite infections and infestations in a mammal comprising administering the compositions of the invention to the mammal in need thereof.