FENM and Acetylcholinesterase Inhibitor Combination at Lower Doses

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Solution Overview

Problem

Current treatments for neurodegenerative diseases, particularly Alzheimer's disease, lack efficacy in early stages and are associated with significant adverse effects, limiting their long-term use, and there is a need for more effective therapies that can slow disease progression.

Innovation Solution

A synergistic combination of 3-(2-fluoroethyl)adamantan-1-amine (FENM) with at least one acetylcholinesterase inhibitor, such as donepezil, galantamine, or rivastigmine, administered at reduced doses to enhance cognitive preservation and reduce side effects.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If a single agent is used to treat Alzheimer's disease, then the treatment is simple, but the efficacy is insufficient

Engineering Contradiction:
Improvetreatment efficacyVSAvoidtreatment complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent combines fenobam (a metabotropic glutamate receptor modulator) with an acetylcholinesterase inhibitor into a single pharmaceutical composition, merging two different mechanisms of action into one treatment regimen to achieve synergistic cognitive enhancement while simplifying administration compared to separate therapies

Inventive Principle:
Principle #5Merging (Combining)

2Reliability

If multiple agents are combined to improve treatment efficacy, then the cognitive enhancement is synergistic, but the side effects increase

Engineering Contradiction:
Improvecognitive enhancementVSAvoidside effects
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent optimizes the dosage parameters of fenobam (0.5-5 mg/kg/day) and acetylcholinesterase inhibitor (0.1-10 mg/kg/day) to achieve synergistic cognitive enhancement while minimizing side effects, demonstrating that proper parameter selection can resolve the contradiction between efficacy and safety

Inventive Principle:
Principle #35Parameter changes

3Reliability

If high doses of a single agent are used to achieve therapeutic effect, then the cognitive improvement is sufficient, but the adverse reactions increase

Engineering Contradiction:
Improvetherapeutic effectVSAvoidadverse reactions
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent distributes the therapeutic effect across two agents at lower individual doses, where fenobam and acetylcholinesterase inhibitor work synergistically to achieve the desired cognitive improvement without the adverse reactions associated with high-dose monotherapy

Inventive Principle:
Principle #5Merging (Combining)

Data Source

PatentEP4429648B1Novel synergistic combinations based on fluoroethylnoremmantine (FENM) and an acetylcholinesterase inhibitor for use in the treatment of neurodegeative diseases
Publication Date: 2026.05.13 REST THERAPEUTICS
  • EP4429648B1 patent drawingFigure 1A~1B
  • EP4429648B1 patent drawingFigure 2A~2B
  • EP4429648B1 patent drawing

AI summary

The invention relates to a composition comprising a synergistic combination of fluoroethylnormemantine (FENM) and of at least one acetylcholinesterase inhibitor. More particularly, the invention relates to said composition for use thereof as a medicament, even more particularly for use thereof in the treatment of a pathological condition selected from tauopathies, synucleinopathies, amyloidopathies, Alzheimer's disease, Parkinson's disease, multiple system atrophy, Huntington's disease, posterior cortical atrophy, Pick's disease, epilepsy, vascular dementia, frontotemporal dementia, Lewy body dementia and amyotrophic lateral sclerosis.