Neramexane Dual-Receptor Therapy for Cochlear Tinnitus

Resolve Bottlenecks,
Find Innovative Solutions
Generate Solutions

Solution Overview

Problem

Current treatments for tinnitus associated with hearing loss or mild hearing loss are ineffective in providing replicable reduction of tinnitus and associated annoyance, with existing pharmaceutical approaches showing limited success due to targeting mainly the afferent part of the auditory system while neglecting efferent neurotransmission.

Innovation Solution

The use of 1-amino-alkylcyclohexane derivatives, such as neramexane or its pharmaceutically acceptable salts, which act as NMDA receptor antagonists and α9/α10 nicotinic receptor antagonists, to treat cochlear tinnitus by addressing both afferent and efferent neurotransmission pathways.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Device complexity

If existing pharmaceutical approaches targeting mainly the afferent part of the auditory system are used, then the treatment mechanism is simplified, but the treatment effectiveness is limited

Engineering Contradiction:
Improvetreatment mechanism complexityVSAvoidtreatment effectiveness
Core Design Contradiction:
Device complexityVSReliability

Solution Approach 1:

The treatment approach is segmented into two distinct pathways: afferent neurotransmission (NMDA receptors) and efferent neurotransmission (nicotinic receptors). This segmentation allows each pathway to be targeted with specific receptor antagonists, addressing the limitation of previous single-pathway approaches while maintaining clear mechanistic understanding.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent combines two different receptor antagonistic mechanisms (NMDA and nicotinic) into a single treatment strategy. This merging of multiple therapeutic actions addresses the technical contradiction by integrating complexity into the treatment mechanism to achieve improved reliability and effectiveness in tinnitus management.

Inventive Principle:
Principle #5Merging (Combining)

2Adaptability or versatility

If treatment is delayed beyond three to twelve months of onset, then more patients can be reached, but treatment effectiveness decreases

Engineering Contradiction:
Improvetreatment accessibilityVSAvoidtreatment effectiveness
Core Design Contradiction:
Adaptability or versatilityVSReliability

Solution Approach 1:

The patent emphasizes preliminary treatment action within the optimal window of three to twelve months after tinnitus onset. By establishing treatment protocols that prioritize early intervention, the approach maximizes effectiveness while the defined time window provides clear guidance for clinical decision-making.

Inventive Principle:
Principle #10Preliminary action

3Ease of operation

If NMDA receptor-blocking substances are used alone, then the afferent pathway is addressed, but efferent neurotransmission remains uninfluenced

Engineering Contradiction:
Improvetreatment simplicityVSAvoidneurotransmission coverage
Core Design Contradiction:
Ease of operationVSReliability

Solution Approach 1:

The treatment is segmented to specifically address afferent (NMDA) and efferent (nicotinic) pathways separately, allowing each to be optimized independently while understanding their distinct roles in tinnitus pathophysiology.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The combined treatment approach creates a multi-functional therapy that simultaneously addresses both afferent and efferent neurotransmission. This universal approach covers the full spectrum of auditory neurotransmission involved in tinnitus, enhancing overall treatment reliability.

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

Data Source

PatentEP2386299B11-Amino-Alkylcyclohexane derivatives for use in the treatment of tinnitus associated with hearing loss
Publication Date: 2016.07.13 MERZ PHARMA GMBH & CO KGAA
  • EP2386299B1 patent drawingFigure 1
  • EP2386299B1 patent drawing

AI summary

The present invention relates to the treatment of an individual afflicted with cochlear tinnitus comprising administering to the individual an effective amount of a 1-amino-alkylcyclohexane derivative.