INT131 PPAR-gamma Agonist Neuroprotection Multiple Sclerosis

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Solution Overview

Problem

Current therapies for multiple sclerosis (MS) relapses are poorly tolerated due to adverse effects and do not provide overall neuroprotection, leaving a need for a safe and effective method to slow progression and alleviate symptoms.

Innovation Solution

Administration of INT131, a selective PPARγ agonist that activates anti-inflammatory and neuroprotective gene pathways, which has been shown to be effective in treating MS relapses by reducing inflammation and neurodegeneration.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current MS therapies are administered, then relapse frequency and severity are reduced, but adverse effects increase and neuroprotection is not provided

Engineering Contradiction:
Improveeffectiveness in reducing relapse frequency and severityVSAvoidadverse effects and lack of neuroprotection
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent changes the pharmacological parameter by using a PPAR-gamma agonist instead of conventional MS therapies. This parameter change results in both effectiveness in reducing relapse frequency and severity, and additional neuroprotective effects without the adverse effects associated with current treatments.

Inventive Principle:
Principle #35Parameter changes

2Object-generated harmful factors

If conventional MS treatments are used, then immune system activity is suppressed, but overall neuroprotection is not achieved

Engineering Contradiction:
Improveimmune-mediated inflammationVSAvoidneuroprotection
Core Design Contradiction:
Object-generated harmful factorsVSReliability

Solution Approach 1:

The PPAR-gamma agonist INT131 performs multiple functions simultaneously: it suppresses immune-mediated inflammation and provides neuroprotection. This multi-functionality resolves the contradiction by achieving both immune suppression and neuroprotection with a single therapeutic agent.

Inventive Principle:
Principle #6Universality (Multi-functionality)

Data Source

PatentEP2950798B1PPAR-gamma agonist for treatment of multiple sclerosis
Publication Date: 2021.05.12 INTEKRIN THERAPEUTICS INC
  • EP2950798B1 patent drawingFigure 1~2
  • EP2950798B1 patent drawingFigure 3
  • EP2950798B1 patent drawing

AI summary

Methods of treatment of multiple sclerosis (MS) with PPARγ agonists, and in particular with the compound of formula (I) known as INT131.