AAV Ocular Gene Therapy for Sustained Anti-VEGF Treatment

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Solution Overview

Problem

Current treatments for ocular angiogenic diseases such as wet age-related macular degeneration and diabetic retinopathy require frequent intravitreal injections, posing a burden on patients and caregivers, and real-world efficacy is often inferior to clinical trial results.

Innovation Solution

Compositions comprising nucleic acids encoding anti-angiogenic polypeptides like aflibercept and interfering RNA molecules targeting pro-angiogenic genes, delivered via adeno-associated virus vectors, to inhibit vascular endothelial growth factor (VEGF) signaling.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If repeated intravitreal injections of anti-VEGF protein therapies are administered to maintain vision, then therapeutic efficacy is improved, but treatment burden on patients and caregivers increases substantially

Engineering Contradiction:
Improvetherapeutic efficacyVSAvoidtreatment burden
Core Design Contradiction:
ReliabilityVSEase of operation

Solution Approach 1:

The patent employs self-complementary AAV vectors that can transduce and express therapeutic genes autonomously in retinal cells, enabling the tissue to produce its own anti-angiogenic factors continuously without requiring repeated external injections. This self-sustaining expression mechanism directly reduces treatment burden while maintaining therapeutic efficacy.

Inventive Principle:
Principle #25Self-service

Solution Approach 2:

The patent uses AAV-mediated gene delivery to establish permanent or long-lasting expression of anti-VEGF proteins and interfering RNAs in retinal cells before disease progression occurs or as a single upfront intervention. This preliminary genetic modification eliminates the need for subsequent repeated injections, addressing both the efficacy and treatment burden contradiction.

Inventive Principle:
Principle #10Preliminary action

2Duration of action of moving object

If frequent intravitreal injections are required to maintain visual acuity benefit, then sustained anti-angiogenic activity is achieved, but patient compliance and real-world efficacy decrease

Engineering Contradiction:
Improveduration of anti-angiogenic activityVSAvoidreal-world efficacy
Core Design Contradiction:
Duration of action of moving objectVSReliability

Solution Approach 1:

By enabling retinal cells to autonomously produce anti-angiogenic therapeutics through integrated gene therapy, the system ensures continuous drug production regardless of patient compliance issues. This self-sustaining mechanism extends the duration of action from weeks to potentially years, directly improving real-world efficacy by eliminating adherence barriers.

Inventive Principle:
Principle #25Self-service

Solution Approach 2:

The patent achieves continuous anti-angiogenic activity through permanent or long-term expression of therapeutic genes in retinal cells. The AAV vectors integrate into the genome or maintain stable episomal expression, ensuring uninterrupted production of anti-VEGF proteins and interfering RNAs, thereby maintaining therapeutic effect without the gaps that occur with intermittent injections.

Inventive Principle:
Principle #20Continuity of useful action

3Ease of operation

If single nucleic acid therapies are used to reduce injection frequency, then treatment burden is reduced, but sustained therapeutic effect may be insufficient compared to combination therapies

Engineering Contradiction:
Improvetreatment burdenVSAvoidduration of therapeutic effect
Core Design Contradiction:
Ease of operationVSDuration of action of moving object

Solution Approach 1:

The patent combines multiple therapeutic mechanisms into a single AAV vector construct: overexpression of anti-VEGF proteins (such as aflibercept), expression of interfering RNAs to suppress VEGF mRNA, and use of self-complementary AAV for enhanced transduction efficiency. This merged combination therapy is delivered as a single injection, reducing treatment burden while achieving sustained therapeutic effects through multiple concurrent mechanisms.

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The patent creates a composite therapeutic system within a single AAV vector that integrates multiple functional elements: promoter regions for constitutive expression, coding sequences for anti-VEGF proteins, interfering RNA sequences, and regulatory elements. This composite genetic construct enables simultaneous multiple mechanisms of action from a single administration, addressing both reduced injection frequency and sustained efficacy.

Inventive Principle:
Principle #40Composite materials

Data Source

PatentEP4330411B1Compositions and methods for treatment of ocular disease associated with angiogenesis
Publication Date: 2026.03.18 4D MOLECULAR THERAPEUTICS INC
  • EP4330411B1 patent drawingFigure 1A~1B
  • EP4330411B1 patent drawingFigure 2
  • EP4330411B1 patent drawingFigure 3A~3B

AI summary

The present disclosure provides compositions and methods for the treatment of ocular diseases associated with angiogenesis, particularly wet age-related macular degeneration.