IL-36 Ocular Composition for Vascular Leakage Stabilization

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Solution Overview

Problem

Current anti-VEGF therapies for ocular disorders such as AMD, diabetic retinopathy, and macular oedema are less effective in stabilizing vascular leakage and proliferation, and long-term use can cause retinal degeneration, necessitating the development of alternative therapeutic approaches that target specific signal transduction cascades to reduce side effects.

Innovation Solution

The use of IL-36 and/or IL-18 compositions to treat or prophylaxis ocular disorders, optionally combined with anti-VEGF agents, to enhance endothelial cell barrier function and reduce vascular permeability, including administration routes like intraocular and intravitreal.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If anti-VEGF agents are used to treat ocular disorders, then vascular leakage and proliferation are stabilized, but long-term use causes retinal degeneration and reduces treatment effectiveness

Engineering Contradiction:
Improvestability of vascular leakage controlVSAvoidretinal degeneration
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent segments the VEGF signaling pathway targeting by using IL-36 and IL-18 to specifically modulate VEGFR2-mediated angiogenesis and vascular permeability, while preserving VEGFR1-mediated neuronal survival functions. This selective segmentation allows treatment of vascular pathology without harming retinal neurons.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent introduces IL-36 and IL-18 as intermediary cytokines that indirectly regulate VEGF signaling through modulation of endothelial cell function and VEGF expression, rather than directly blocking VEGF or its receptors. This intermediary approach provides more nuanced control over the VEGF pathway.

Inventive Principle:
Principle #24Intermediary (Mediator)

2Object-generated harmful factors

If anti-VEGF therapies are used to treat ocular disorders, then neovascularization is inhibited, but vascular permeability stabilization is reduced

Engineering Contradiction:
Improveneovascularization controlVSAvoidvascular permeability stabilization
Core Design Contradiction:
Object-generated harmful factorsVSReliability

Solution Approach 1:

The patent applies local quality by targeting specific functional aspects of the VEGF pathway through IL-36 and IL-18, which preferentially affect VEGFR2-mediated processes (angiogenesis and vascular permeability) while sparing VEGFR1-mediated functions. This creates differential effects on various pathological processes.

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The patent changes the therapeutic parameter from direct VEGF inhibition to cytokine-mediated modulation of VEGF signaling. IL-36 and IL-18 alter the biological parameters of endothelial cell function, VEGF expression, and receptor signaling dynamics, providing more comprehensive control over both neovascularization and vascular permeability.

Inventive Principle:
Principle #35Parameter changes

3Duration of action of stationary object

If regular monthly intraocular injections of anti-VEGF agents are administered, then choroidal neovascularization is stabilized, but treatment refractoriness develops over time

Engineering Contradiction:
Improveduration of disease stabilizationVSAvoidtreatment responsiveness
Core Design Contradiction:
Duration of action of stationary objectVSReliability

Solution Approach 1:

The patent inverts the conventional approach by instead of inhibiting VEGF signaling, using IL-36 and IL-18 to modulate and regulate VEGF pathway activity. This inverse approach of activation/modulation rather than inhibition provides alternative mechanisms of action that bypass resistance to anti-VEGF therapies.

Inventive Principle:
Principle #13The other way round (Inversion)

Solution Approach 2:

The patent fundamentally changes the therapeutic parameter from VEGF inhibition to cytokine-mediated VEGF pathway modulation. This parameter change introduces new biological mechanisms that are not subject to the same resistance patterns as anti-VEGF agents, potentially restoring treatment responsiveness.

Inventive Principle:
Principle #35Parameter changes

Data Source

PatentEP4706765A2A composition comprising il-36 and optionally il-18 for use in treating ocular disorders
Publication Date: 2026.03.11 THE PROVOST FELLOWS FOUNDATION SCHOLARS AND THE OTHER MEMBERS OF BOARD OF THE COLLEGE OF THE HOLY AND UNDIVIDED TRINITY OF QUEEN ELIZABETH NEAR DUBLIN
  • EP4706765A2 patent drawingFigure 1A~1B
  • EP4706765A2 patent drawingFigure 1C~1F
  • EP4706765A2 patent drawingFigure 2A~2C

AI summary

The present invention relates to a composition comprising IL-36 and/or IL-18 for use in treating ocular disorders such as age-related macular degeneration (AMD), macular oedema, retinopathy, diabetic retinopathy, and glaucoma. The present invention also relates to a method of identifying patients likely to respond to an anti-VEGF agent.