ST2L Antagonists Block IL-33 Interaction to Reduce Inflammation

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Solution Overview

Problem

There is a need for effective ST2L antagonists to treat immune-mediated diseases such as asthma, rheumatoid arthritis, inflammatory bowel disease, and other conditions characterized by excessive type 2 cytokine responses and airway hyper-reactivity, as existing treatments are inadequate in managing these dysregulated immune responses.

Innovation Solution

Development of isolated antibodies or fragments that specifically bind to Domain I of human ST2L, comprising specific heavy and light chain variable regions, which inhibit IL-33/ST2L interaction and subsequent mast cell responses, thereby modulating immune system activity and reducing cytokine release.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If ST2L is activated by IL-33, then type 2 cytokine release is induced, but excessive cytokine responses and airway hyper-reactivity occur

Engineering Contradiction:
Improveimmune response regulationVSAvoidexcessive type 2 cytokine responses
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent applies preliminary anti-action by developing ST2L antagonists that pre-block the ST2L receptor before IL-33 can bind and activate it. The antagonists are designed to occupy the binding site on ST2L, preventing the formation of the ST2L/IL-33 complex and thereby preventing downstream type 2 cytokine release and airway hyper-reactivity before they can occur.

Inventive Principle:
Principle #9Preliminary anti-action

Solution Approach 2:

The patent uses ST2L antagonists as intermediary molecules that mediate between IL-33 and the ST2L receptor. These antagonists act as blocking agents that interfere with the natural interaction between IL-33 and ST2L, thereby modulating the immune response and preventing excessive cytokine production without completely eliminating the signaling pathway.

Inventive Principle:
Principle #24Intermediary (Mediator)

2Object-generated harmful factors

If anti-ST2 antibody is administered to treat immune-mediated diseases, then cytokine production is inhibited, but treatment efficacy is limited

Engineering Contradiction:
Improvecytokine productionVSAvoidtreatment efficacy
Core Design Contradiction:
Object-generated harmful factorsVSReliability

Solution Approach 1:

The patent applies parameter changes by developing new ST2L antagonists with optimized binding affinity and specificity parameters. The antagonists are engineered to have improved pharmacological properties including higher affinity for ST2L, better tissue penetration, and enhanced stability, thereby improving treatment efficacy compared to existing anti-ST2 antibodies.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent employs disposable single-use antibody formulations that are administered at optimized doses to achieve therapeutic effect. The antagonists are designed as ready-to-use therapeutic agents that can be administered in controlled doses, replacing the need for long-term continuous treatment with less effective antibodies.

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

3Ease of operation

If existing treatments are used for ST2L-mediated diseases, then some symptom relief is achieved, but inadequate disease management occurs

Engineering Contradiction:
Improvesymptom reliefVSAvoiddisease management
Core Design Contradiction:
Ease of operationVSReliability

Solution Approach 1:

The patent applies universality by developing ST2L antagonists that can treat multiple ST2L-mediated diseases through a single mechanism of action. The antagonists are designed to block the ST2L/IL-33 pathway universally, making them effective for asthma, rheumatoid arthritis, inflammatory bowel disease, and other conditions mediated by this pathway, thereby providing comprehensive disease management.

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

Data Source

PatentEP2844292B1St2l antagonists and methods of use
Publication Date: 2019.08.21 JANSSEN BIOTECH INC
  • EP2844292B1 patent drawingFigure 1
  • EP2844292B1 patent drawingFigure 2
  • EP2844292B1 patent drawingFigure 3

AI summary

The present invention relates to ST2L antagonists, polynucleotides encoding the antagonists or fragments thereof, and methods of making and using the foregoing.