Bispecific Antibodies Modulating IL-2 Receptor Binding Specificity

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Solution Overview

Problem

High doses of IL-2 therapy for treating certain diseases are toxic due to adverse effects like vascular leak syndrome, and there is no effective treatment for this condition, which is caused by the release of proinflammatory cytokines from IL-2-activated NK cells and direct binding of IL-2 to lung endothelial cells.

Innovation Solution

Development of bispecific antibodies or antigen binding fragments that specifically bind to CD122 and common γ chain (γc), acting as IL-2 receptor agonists to stimulate immune cells without activating high-affinity IL-2R α-β-γc receptors, thereby reducing toxicity and promoting immune stimulation.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Productivity

If high doses of IL-2 are administered for effective treatment, then immune stimulation is improved, but vascular leak syndrome and pulmonary edema occur due to direct binding to lung endothelial cells

Engineering Contradiction:
Improveimmune stimulationVSAvoidvascular leak syndrome
Core Design Contradiction:
ProductivityVSObject-affected harmful factors

Solution Approach 1:

The patent employs blocking antibodies against IL-2Rα as intermediaries to prevent direct binding of IL-2 to lung endothelial cells. The antibody complex acts as a mediator that allows IL-2 to stimulate immune cells through intermediate-affinity receptors while blocking the harmful high-affinity interaction with endothelial cells, thereby resolving the contradiction between effective immune stimulation and avoidance of vascular leak syndrome

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The invention applies local quality by creating differential receptor interactions: the antibody complex selectively allows binding to intermediate-affinity IL-2Rβ-γc receptors on immune cells while blocking high-affinity IL-2Rα-β-γc receptors on endothelial cells. This spatially selective binding pattern enables immune stimulation in specific tissues while preventing harmful effects in others

Inventive Principle:
Principle #3Local quality

2Productivity

If high doses of IL-2 are administered, then immune cell activation is improved, but proinflammatory cytokine release from NK cells causes toxicity

Engineering Contradiction:
Improveimmune cell activationVSAvoidproinflammatory cytokine release
Core Design Contradiction:
ProductivityVSObject-generated harmful factors

Solution Approach 1:

The patent applies partial action by using submaximal doses of IL-2 in combination with blocking antibodies, which provides sufficient immune cell activation through intermediate-affinity receptors while avoiding the excessive activation that triggers harmful proinflammatory cytokine release. The blocking antibody modulates the response to achieve optimal activation without overstimulation

Inventive Principle:
Principle #16Partial or excessive action

Solution Approach 2:

The blocking antibody serves as an intermediary that modulates IL-2 signaling to achieve controlled immune cell activation. It allows beneficial activation through intermediate-affinity receptors while preventing the excessive signaling that would trigger harmful cytokine release from NK cells

Inventive Principle:
Principle #24Intermediary (Mediator)

3Object-affected harmful factors

If IL-2Rα is blocked to prevent VLS, then pulmonary edema is reduced, but immune stimulation may be compromised

Engineering Contradiction:
Improvepulmonary edemaVSAvoidimmune stimulation
Core Design Contradiction:
Object-affected harmful factorsVSProductivity

Solution Approach 1:

The invention achieves multi-functionality by using a single IL-2/antibody complex that simultaneously blocks harmful high-affinity interactions with endothelial cells while preserving beneficial intermediate-affinity interactions with immune cells. This universal approach addresses both protection from VLS and maintenance of immune stimulation through one therapeutic agent

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

Data Source

PatentEP3428193B1Il2rbeta/common gamma chain antibodies
Publication Date: 2020.09.30 AGENCY FOR SCI TECH & RES
  • EP3428193B1 patent drawingFigure 1
  • EP3428193B1 patent drawingFigure 1
  • EP3428193B1 patent drawingFigure 1

AI summary

Anti-CD122 and/or yc antibodies and fragments thereof are disclosed. Also disclosed are compositions comprising such antibodies and fragments, and uses and methods using the same.