Methyl Cyclodextrins Reduce Hepatic Lipid Accumulation

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Solution Overview

Problem

Current treatments for non-alcoholic fatty liver disease (NAFLD) and its aggressive form, non-alcoholic steatohepatitis (NASH), are insufficient as they primarily act downstream of the pathological process and lack medications that effectively limit lipid accumulation in the liver, leading to progressive fibrosis and cirrhosis.

Innovation Solution

Pharmaceutical compositions based on methyl cyclodextrins, specifically those with a molar substitution value between 0.05 and 1.5, are used to reduce lipid storage in the liver, effectively treating and preventing hepatic steatosis and associated conditions by promoting lipid removal and cholesterol increase.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Object-affected harmful factors

If current treatments (caspase or ASK1 inhibitors) are used to act on cell death process, then inflammation is reduced, but lipid accumulation in the liver continues to progress

Engineering Contradiction:
ImproveinflammationVSAvoidlipid accumulation
Core Design Contradiction:
Object-affected harmful factorsVSQuantity of substance

Solution Approach 1:

The patent applies preliminary action by using methyl cyclodextrins to prevent lipid accumulation in the liver before it progresses to inflammation and cell death. The active substance acts upstream in the pathological cascade, blocking lipid storage at its origin rather than treating downstream effects like inflammation or cell death, thereby preventing the development of NASH and fibrosis

Inventive Principle:
Principle #10Preliminary action

Solution Approach 2:

Methyl cyclodextrins serve as an intermediary substance that mediates between the metabolic disturbance causing lipid accumulation and the pathological consequences. The compound specifically targets and reduces hepatic lipid storage through its unique molecular structure, acting as a bridge to correct the metabolic imbalance without affecting other pathological processes

Inventive Principle:
Principle #24Intermediary (Mediator)

2Reliability

If no medication is available to act upstream on lipid accumulation, then the disease progresses to fibrosis and cirrhosis, but current drugs cannot prevent this progression

Engineering Contradiction:
Improvedisease progression controlVSAvoidmedication availability
Core Design Contradiction:
ReliabilityVSEase of manufacture

Solution Approach 1:

The patent applies parameter changes by modifying the chemical structure of cyclodextrins to create methyl cyclodextrins with specific properties (molar substitution value between 0.05 and 1.5). This chemical modification optimizes the compound's ability to reduce hepatic lipid accumulation while maintaining safety, providing a reliable treatment that was previously unavailable

Inventive Principle:
Principle #35Parameter changes

Applied Scientific Principles

This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.

Function Achieved in This Case

Methyl cyclodextrins demonstrate a superior ability to reduce liver lipid accumulation and enhance cholesterol removal, providing both preventive and curative effects on hepatic steatosis, outperforming other cyclodextrin derivatives in clinical models.

Implementation Method 1

pharmaceutical compositions based on methyl cyclodextrins make it possible to reduce the storage of lipids in the liver

Methodology Applied
Scientific EffectInclusion complex formation: Solvation

Data Source

PatentUS20240000827A1Compositions comprising methyl cyclodextrins for the treatment and/or prevention of hepatic steatosis
Publication Date: 2024.01.04 ROQUETTE FRERES SA
  • US20240000827A1 patent drawing
  • US20240000827A1 patent drawing
  • US20240000827A1 patent drawing

AI summary

The present invention relates to a novel use of a pharmaceutical composition comprising at least one methyl cyclodextrin in the treatment and/or prevention of hepatic steatosis and related diseases. The invention also relates to the use of methyl cyclodextrin to reduce lipid accumulation in the liver.