Aspirin-Fumaric Acid Combination for MS Treatment

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Solution Overview

Problem

Current treatments for multiple sclerosis (MS) using dimethyl fumarate (DMF) and its metabolite, monomethyl fumarate (MMF), are limited by side effects such as cutaneous flush, which can lead to non-compliance due to intolerance.

Innovation Solution

The administration of aspirin in conjunction with fumaric acid or its esters/salts, such as DMF and MMF, enhances the bioavailability of fumaric acid, allowing for a lower effective dose without compromising treatment outcomes, and enables patients to tolerate higher doses with reduced side effects.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If dimethyl fumarate (DMF) and monomethyl fumarate (MMF) are used to treat multiple sclerosis, then treatment efficacy is improved, but cutaneous flush side effects increase

Engineering Contradiction:
Improvetreatment efficacyVSAvoidcutaneous flush
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

Aspirin is introduced as an intermediary substance that modifies the interaction between fumaric acid esters and the patient's body. The aspirin-fumaric acid combination enhances bioavailability and reduces cutaneous flush, acting as a mediator that improves the risk-benefit ratio of the treatment

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent changes the dosing parameters by allowing lower doses of fumaric acid (360-480 mg/day) when combined with aspirin, compared to conventional higher doses. This parameter change maintains efficacy while reducing harmful side effects through the synergistic interaction with aspirin

Inventive Principle:
Principle #35Parameter changes

2Reliability

If higher doses of fumaric acid or its esters are administered, then treatment outcome is improved, but patient tolerance decreases due to side effects

Engineering Contradiction:
Improvetreatment outcomeVSAvoidpatient tolerance
Core Design Contradiction:
ReliabilityVSEase of operation

Solution Approach 1:

Aspirin serves as a protective intermediary that reduces the toxic effects of higher fumaric acid doses. This allows patients to tolerate higher effective doses without experiencing excessive side effects, improving both treatment outcome and patient comfort

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

Aspirin is administered concurrently with fumaric acid to pre-establish protective effects against cutaneous flush and other side effects. This preliminary protective action enables patients to tolerate higher doses of fumaric acid without compromising safety or comfort

Inventive Principle:
Principle #10Preliminary action

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

The combination of aspirin and fumaric acid or its esters/salts increases bioavailability, allowing for a lower daily dose of fumaric acid (e.g., 360 mg) to achieve the same efficacy as a conventional 480 mg dose, while also reducing side effects and improving patient tolerance.

Implementation Method 1

The administration of aspirin in conjunction with fumaric acid or its esters/salts, such as DMF and MMF, enhances the bioavailability of fumaric acid

Methodology Applied
Scientific EffectBioavailability enhancement: Absorption (physical)

Data Source

PatentUS20250144121A1Compositions and methods for treating multiple sclerosis
Publication Date: 2025.05.08 VITALIS LLC
  • US20250144121A1 patent drawing

AI summary

Provided are compositions and methods for treating multiple sclerosis (MS). One embodiment of the disclosed method entails orally administering to a MS patient a first amount of aspirin and a second amount of fumaric acid or an ester or a salt thereof. In some embodiments, the aspirin is administered at from about 80 mg to about 500 mg per day and the fumaric acid or ester or salt thereof is administered at about 360 mg per day.