Indole Derivative Compositions for Drug-Resistant Liver Flukes

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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 improved efficacy.

Innovation Solution

The use of indole derivatives in oral, topical, or injectable veterinary compositions that demonstrate anthelmintic effectiveness against trematode infections, including Fasciola hepatica, offering superior efficacy and a quick onset of action with a long duration of activity.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If triclabendazole is used to treat liver fluke infections, then high efficacy is achieved, but parasite resistance increases

Engineering Contradiction:

ImproveefficacyVSAvoidresistance

Core Design Contradiction:

ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent changes the chemical structure parameter from benzimidazole (triclabendazole) to indole derivatives, creating a new chemical class that bypasses resistance mechanisms developed against triclabendazole while maintaining anthelmintic efficacy against Fasciola hepatica

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent combines indole derivatives with macrocyclic lactones to create a composite anthelmintic composition that targets different physiological pathways in the parasite, thereby overcoming resistance to either agent alone

Inventive Principle:

Principle #40Composite materials

2Reliability

If existing anthelmintics are used, then treatment effectiveness is maintained, but side effects increase

Engineering Contradiction:

Improvetreatment effectivenessVSAvoidside effects

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent changes the chemical structure to indole derivatives with modified pharmacological properties that maintain anthelmintic effectiveness while reducing toxic side effects compared to traditional benzimidazoles and halogenated compounds

Inventive Principle:

Principle #35Parameter changes

3Speed

If faster acting treatments are used, then speed of onset is improved, but duration of activity may be reduced

Engineering Contradiction:

Improvespeed of onsetVSAvoidduration of activity

Core Design Contradiction:

SpeedVSDuration of action of moving object

Solution Approach 1:

The patent designs indole derivative compositions that provide continuous anthelmintic action through sustained release mechanisms and combination with macrocyclic lactones, ensuring both rapid initial effect and prolonged duration of activity

Inventive Principle:

Principle #20Continuity of useful action

Data Source

PatentUS9776986B2Parasiticidal compositions comprising indole derivatives, methods and uses thereof

Publication Date: 2017.10.03 MERIAL LTD

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.