ERRγ Inhibitors to Prevent Pancreatic Enzyme Autodigestion

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Solution Overview

Problem

Current treatments for pancreatitis, particularly acute pancreatitis, are inadequate, with high morbidity and mortality rates due to the lack of approved drugs, and existing models fail to effectively target the underlying pathophysiology of the disease.

Innovation Solution

The use of aryl ethene compounds, specifically ERRγ inhibitors such as DMRC200434, DMRC2001000, DMRC200699, and DMRC200996, to prevent the premature activation of pancreatic digestive enzymes by inhibiting ERRγ, thereby reducing pancreatic autodigestion and inflammation.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current treatments for pancreatitis are used, then existing therapy options are available, but morbidity and mortality rates remain high due to lack of approved drugs

Engineering Contradiction:
Improvetreatment effectivenessVSAvoidavailability of approved drugs
Core Design Contradiction:
ReliabilityVSEase of manufacture

Solution Approach 1:

The patent segments the complex pathophysiological process of pancreatitis into specific molecular targets (ERRγ, mitochondrial dysfunction, autophagic dysfunction) and addresses each separately with targeted compounds, moving away from non-specific current treatments

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent introduces ERRγ inhibitors as intermediary compounds that mediate between the trigger of pancreatitis and the downstream harmful effects (enzyme activation, tissue damage), blocking the pathological cascade at a specific molecular level

Inventive Principle:
Principle #24Intermediary (Mediator)

2Adaptability or versatility

If existing treatments are applied, then some therapeutic intervention is provided, but they fail to effectively target the underlying pathophysiology of the disease

Engineering Contradiction:
Improvepathophysiology targeting capabilityVSAvoiddisease outcome improvement
Core Design Contradiction:
Adaptability or versatilityVSReliability

Solution Approach 1:

The patent applies local quality by targeting specific cellular compartments and molecular pathways (mitochondria, autophagy, ERRγ receptor) within the pancreatic acinar cells, rather than applying general anti-inflammatory treatments throughout the system

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The patent changes the therapeutic parameter from general symptom management to specific molecular pathway modulation by inhibiting ERRγ and its downstream effects on mitochondrial and autophagic function, thereby addressing the root pathophysiology

Inventive Principle:
Principle #35Parameter changes

3Productivity

If pancreatic digestive enzymes are activated prematurely, then digestive function is initiated, but pancreatic autodigestion and inflammation occur leading to tissue damage

Engineering Contradiction:
Improveenzyme activation timingVSAvoidpancreatic tissue damage
Core Design Contradiction:
ProductivityVSObject-affected harmful factors

Solution Approach 1:

The patent applies preliminary action by preventing the premature activation of pancreatic enzymes through ERRγ inhibition before autodigestion can occur, addressing the problem at an upstream regulatory level

Inventive Principle:
Principle #10Preliminary action

Solution Approach 2:

The patent applies preliminary anti-action by introducing ERRγ inhibitors that counteract the premature enzyme activation process before it causes significant tissue damage, neutralizing the harmful effect in advance

Inventive Principle:
Principle #9Preliminary anti-action

Data Source

PatentEP4168013B1Estrogen-related receptor gamma (ERRG) inhibitors for use in treating pancreatitis
Publication Date: 2025.10.22 NOVMETAPHARMA CO LTD
  • EP4168013B1 patent drawingFigure 1A~1B
  • EP4168013B1 patent drawingFigure 2A~2B
  • EP4168013B1 patent drawingFigure 3

AI summary

A composition for preventing and/or treating pancreatitis and a method of prevention and/or treatment of pancreatitis are disclosed. The composition include an aryl ethene compound, a pharmaceutically acceptable salt thereof, or a solvate thereof, as an active ingredient. Also disclosed is a use of the aryl ethene compound, a pharmaceutically acceptable salt thereof, or a solvate thereof, in manufacturing a medicament for preventing and/or treating pancreatitis or for treating one or more symptoms of pancreatitis in a patient. The method includes administering the aryl ethene compound, an isomer, a pharmaceutically acceptable salt thereof, or a solvate thereof, in an effective amount to a subject in need thereof.