Nor-UDCA for Reducing Atherosclerotic Plaque Size

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Solution Overview

Problem

Current treatments for arteriosclerosis, particularly atherosclerosis, are inadequate in reducing atherosclerotic lesions and plaques, and often come with significant side effects, while also failing to address associated risk factors like non-alcoholic fatty liver disease (NAFLD).

Innovation Solution

Nor-ursodeoxycholic acid (nor-UDCA) and its pharmaceutically acceptable salts or esters are used to treat and prevent arteriosclerosis, including atherosclerosis, by reducing plaque size, hepatic triglyceride levels, and inflammatory signals, thereby addressing both the disease and its risk factors.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Quantity of substance

If current medications are used for treatment of atherosclerosis, then cholesterol levels may be reduced, but considerable side effects occur and atherosclerotic lesions are not effectively reduced

Engineering Contradiction:
Improvecholesterol levelsVSAvoidside effects
Core Design Contradiction:
Quantity of substanceVSObject-affected harmful factors

Solution Approach 1:

The patent uses nor-UDCA, a modified bile acid derivative, to change the biochemical parameters of lipid metabolism. This compound specifically targets atherosclerotic plaque composition by altering cholesterol esterification and mobilization processes, reducing plaque burden while avoiding the side effects of conventional statin medications through a different mechanism of action

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

Nor-UDCA acts as an intermediary substance that mediates between the liver and atherosclerotic plaques. It facilitates cholesterol extraction from plaques and promotes its excretion, serving as a bridge that transports cholesterol from the arterial wall to the bile for elimination, thereby reducing plaque volume without directly interfering with systemic cholesterol synthesis

Inventive Principle:
Principle #24Intermediary (Mediator)

2Reliability

If statins are used to reduce high cholesterol blood levels, then prophylactic effect is achieved, but they are not suitable to reduce existing atherosclerotic lesions and plaques

Engineering Contradiction:
Improveprophylactic effectVSAvoidatherosclerotic lesions
Core Design Contradiction:
ReliabilityVSQuantity of substance

Solution Approach 1:

Nor-UDCA performs preliminary action by stabilizing and reducing existing atherosclerotic plaques before they can cause acute events. The compound works on established lesions by promoting cholesterol efflux from macrophages within plaques and reducing inflammatory activity, thereby preventing plaque rupture and subsequent cardiovascular events

Inventive Principle:
Principle #10Preliminary action

Solution Approach 2:

The patent employs nor-UDCA to change the physical and chemical parameters of atherosclerotic plaques. It alters plaque composition by reducing cholesterol ester content, decreasing inflammatory cell infiltration, and modifying the fibrous cap structure, thereby transforming vulnerable plaques into more stable configurations that are less prone to rupture

Inventive Principle:
Principle #35Parameter changes

3Quantity of substance

If conventional treatments are used for atherosclerosis, then cholesterol management is addressed, but associated risk factors like NAFLD are not treated

Engineering Contradiction:
Improvecholesterol blood levelsVSAvoidcoverage of risk factors
Core Design Contradiction:
Quantity of substanceVSAdaptability or versatility

Solution Approach 1:

Nor-UDCA exhibits multi-functionality by simultaneously addressing multiple risk factors associated with atherosclerosis. It acts on both lipid metabolism in the liver (reducing hepatic triglycerides and treating NAFLD) and vascular pathology (reducing atherosclerotic plaque burden), providing a unified therapeutic approach that covers both cardiovascular and metabolic aspects of the disease syndrome

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

Data Source

PatentEP2182954B1Use of nor-bile acids in the treatment of arteriosclerosis
Publication Date: 2018.11.28 MEDIZINISCHE UNIV GRAZ
  • EP2182954B1 patent drawingFigure 1
  • EP2182954B1 patent drawingFigure 2A~2B
  • EP2182954B1 patent drawingFigure 3

AI summary

The present invention relates to the use of nor-bile acids and their pharmaceutically acceptable salts, esters and/or derivatives in the treatment arteriosclerosis.