Neramexane NMDA Antagonist for Mast Cell Diseases
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Solution Overview
Problem
Current treatments for mast cell-mediated diseases such as urticaria, atopic dermatitis, psoriasis, pruritus, asthma, rhinitis, mastocytosis, conjunctivitis, and keratoconjunctivitis are inadequate, particularly for severe and chronic forms, with low efficacy and significant impact on quality of life.
Innovation Solution
Administration of neramexane, a 1-amino-alkylcyclohexane derivative, either alone or in combination with other pharmaceutical agents like anticholinergic substances, antihistamines, and corticosteroids, in various formulations including immediate release, modified release, topical, and oral forms, to effectively manage mast cell-mediated diseases.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If current treatments (antihistamines, mast cell membrane stabilizers) are used for mast cell-mediated diseases, then some symptom relief is achieved, but treatment efficacy is insufficient particularly for severe and chronic forms
Solution Approach 1:
The patent applies parameter changes by introducing neramexane, a compound with a different mechanism of action (NMDA receptor antagonism) compared to conventional treatments. This changes the therapeutic parameter from histamine receptor blockade to glutamate receptor modulation, thereby improving efficacy in severe and chronic mast cell-mediated diseases where conventional treatments fail
Solution Approach 2:
The patent employs composite materials by combining neramexane with existing pharmaceutical agents (antihistamines, mast cell membrane stabilizers, corticosteroids). This composite approach leverages multiple mechanisms of action simultaneously, enhancing overall treatment efficacy while maintaining the benefits of established therapies
2Reliability
If mast cells release mediators during degranulation, then inflammatory response is triggered, but this causes harmful effects in surrounding tissue
Solution Approach 1:
The patent converts the harmful effect of mast cell degranulation into a beneficial outcome by using neramexane to block NMDA receptors. This prevents the cascade of inflammatory events triggered by mediator release, transforming the pathological process into a controlled therapeutic response that maintains immune function while preventing tissue damage
Solution Approach 2:
The patent introduces neramexane as an intermediary substance that interferes with the signaling pathway between mast cell degranulation and tissue damage. By antagonizing NMDA receptors, neramexane acts as a mediator that blocks the harmful transmission of inflammatory signals while allowing the initial immune response to proceed
Data Source
Figure 1
AI summary
The present invention relates to the treatment of an individual afflicted with mast cell mediated diseases comprising administering to the individual an effective amount of a 1-amino-alkylcyclohexane derivative.