SWAP-70 Inhibitor Screening for Causal IgE Allergy Therapy

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Solution Overview

Problem

Current allergy treatments are largely symptomatic and do not address the root cause of IgE production, leading to inefficiencies and side effects, with existing inhibitors like omalizumab intercepting rather than stopping IgE production and potentially triggering allergic reactions.

Innovation Solution

A method to screen for active ingredients that inhibit SWAP-70, which positively regulates IgE production by modulating the interaction between STAT-6 and BCL-6, allowing for the development of causal therapies for allergies and autoimmune diseases by specifically targeting IgE production.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If omalizumab is used to treat allergies, then IgE-mediated allergic reactions are reduced, but IgE production is not stopped and new allergic reactions may be triggered

Engineering Contradiction:
Improveeffectiveness of allergy treatmentVSAvoidpotential allergic reactions to antibody therapy
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent applies preliminary action by developing compounds that prevent IgE production before it occurs, rather than intercepting IgE after production. The screenable compounds inhibit the IgE production pathway upstream, blocking the formation of IgE antibodies in the first place, which eliminates the risk of reactions to therapeutic antibodies while maintaining treatment effectiveness

Inventive Principle:
Principle #10Preliminary action

Solution Approach 2:

The patent uses small molecule compounds as intermediaries that target the IgE production pathway. These small molecules act as mediators between the therapeutic goal and the biological system, inhibiting key enzymes or proteins involved in IgE synthesis without requiring large protein therapeutics, thus avoiding immunogenicity issues

Inventive Principle:
Principle #24Intermediary (Mediator)

2Object-affected harmful factors

If current symptomatic treatments are used, then allergic symptoms are alleviated, but the root cause of IgE production is not addressed

Engineering Contradiction:
Improveallergic symptomsVSAvoidcausal therapy effectiveness
Core Design Contradiction:
Object-affected harmful factorsVSReliability

Solution Approach 1:

The patent extracts and targets the specific molecular mechanism responsible for IgE production. By identifying and inhibiting key proteins or enzymes in the IgE production pathway using screenable compounds, the treatment addresses the root cause rather than just symptoms, while the compounds can be optimized for specificity and efficacy

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The patent employs screenable compounds that modify parameters in the IgE production pathway, such as inhibiting enzyme activity or blocking protein-protein interactions. This changes the biological parameters controlling IgE synthesis, shifting the system from a symptomatic treatment approach to a causal therapy that fundamentally alters the disease mechanism

Inventive Principle:
Principle #35Parameter changes

3Reliability

If antibody therapies are used to inhibit IgE, then allergic reactions are reduced, but the therapy is pharmacologically complex to produce and may trigger immune reactions

Engineering Contradiction:
Improveallergy treatment effectivenessVSAvoidpharmaceutical production complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent replaces complex, expensive monoclonal antibody therapies with small molecule compounds that are simpler to produce and administer. These small molecules can be synthesized through established pharmaceutical processes, reducing manufacturing complexity and cost while maintaining therapeutic effectiveness through targeted inhibition of IgE production

Inventive Principle:
Principle #27Cheap short-living objects (Disposable)

Solution Approach 2:

The patent substitutes the mechanical/structural complexity of large protein therapeutics with simpler small molecule compounds. By using screenable small molecules that target specific molecular interactions in the IgE pathway, the therapy replaces the need for complex antibody production and administration with simpler chemical entities that can be orally administered or given via standard routes

Inventive Principle:
Principle #28Mechanics substitution (Replace mechanical system)

Data Source

PatentEP2558861B1Method and means of identification of substances, which inhibit ige production
Publication Date: 2016.08.10 THORNE
  • EP2558861B1 patent drawingFigure 1A~1C
  • EP2558861B1 patent drawingFigure 2A~2C
  • EP2558861B1 patent drawingFigure 3

AI summary

The invention relates to the field of biomedical and pharmacological research, in particular to the area of immunology, allergies and autoimmune diseases. The inventors have shown that SWAP-70 is a higher-level regulator for STAT-6 and BCL-6, the regulator being specific for IgE production in B-cells by amplifying the effect of STAT-6 and antagonizing the effect of BCL-6. The inventors have observed no influence of SWAP-70 on the expression of other genes that are likewise regulated by STAT-6 and/or BCL-6. In summary, it can be concluded that SWAP-70 positively regulates IgE production by shifting the interaction of the two antagonists STAT-6 and BCL-6 with regulatory elements of the IgE gene in favor of the activator STAT-6. Based on said findings, the invention provides a screening method which allows for identifying novel active agents that specifically inhibit IgE production. The substances identified by the method according to the invention are particularly suited for treating IgE-induced allergies and IgE-dependent autoimmune diseases.