Dobesilate Repurposing for AMD Retinal Architecture Normalization

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Solution Overview

Problem

Current treatments for age-related macular degeneration, particularly wet AMD, are associated with side effects like inflammation and fibrosis, and are expensive, while dry AMD lacks effective treatments, necessitating a safer, less expensive, and more efficient therapeutic option.

Innovation Solution

The use of dobesilate and its pharmaceutically acceptable salts, such as diethylamine 2,5-dihydroxybenzenesulfonate, for treating both wet and dry forms of age-related macular degeneration, which normalizes retinal architecture and improves visual acuity through intravitreal or topical administration.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Measurement precision

If current treatments for wet AMD are used, then visual acuity can be maintained or improved, but side effects such as inflammation and fibrosis occur and treatment cost increases

Engineering Contradiction:
Improvevisual acuityVSAvoidinflammation and fibrosis
Core Design Contradiction:
Measurement precisionVSObject-affected harmful factors

Solution Approach 1:

The patent employs dobesilate, a short-acting vasoprotective agent with a brief half-life, administered repeatedly at intervals. This approach replaces chronic, expensive anti-VEGF therapies with a cost-effective, short-acting alternative that achieves therapeutic goals without the severe side effects of current treatments.

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

Solution Approach 2:

The invention changes the therapeutic parameter from anti-VEGF mechanism to vasoprotective mechanism using dobesilate. This parameter change shifts the treatment approach from blocking vascular growth to protecting existing vessels, thereby improving visual acuity while avoiding inflammation and fibrosis associated with current therapies.

Inventive Principle:
Principle #35Parameter changes

2Measurement precision

If current treatments for wet AMD are used, then visual acuity can be maintained or improved, but treatment cost increases significantly

Engineering Contradiction:
Improvevisual acuityVSAvoidtreatment cost
Core Design Contradiction:
Measurement precisionVSQuantity of substance

Solution Approach 1:

The patent employs dobesilate, a short-acting vasoprotective agent with a brief half-life, administered repeatedly at intervals. This approach replaces chronic, expensive anti-VEGF therapies with a cost-effective, short-acting alternative that achieves therapeutic goals without the severe side effects of current treatments.

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

Solution Approach 2:

The invention uses dobesilate, a well-established, inexpensive drug originally developed for other indications, and repurposes it for AMD treatment. This copying approach leverages an existing safe and cheap medication to address a costly medical problem, avoiding the need for expensive new drug development.

Inventive Principle:
Principle #26Copying

3Object-affected harmful factors

If no treatment is used for dry AMD, then no side effects occur, but visual acuity deteriorates due to geographic atrophy

Engineering Contradiction:
Improveside effectsVSAvoidvisual acuity
Core Design Contradiction:
Object-affected harmful factorsVSMeasurement precision

Solution Approach 1:

The patent applies dobesilate to enhance the eye's own protective mechanisms against geographic atrophy. The drug stimulates endogenous vasoprotective pathways and promotes survival of retinal vessels and surrounding tissue, enabling the ocular system to fight atrophy through its own reinforced defenses rather than external intervention.

Inventive Principle:
Principle #25Self-service

Solution Approach 2:

The invention administers dobesilate prophylactically to prevent geographic atrophy progression before significant vision loss occurs. By treating early-stage dry AMD with vasoprotective therapy, the drug preserves retinal architecture and visual acuity before irreversible damage sets in, acting as a preventive measure rather than a corrective one.

Inventive Principle:
Principle #10Preliminary action

Data Source

PatentEP2777699B1Diethylamine-2,5-dihydroxybenzenesulfonate for the treatment of age-related macular degeneration
Publication Date: 2017.03.29 INVESFOVEA SL
  • EP2777699B1 patent drawing
  • EP2777699B1 patent drawing
  • EP2777699B1 patent drawing

AI summary

The invention relates to the safety and efficacy of Dobesilate, a very well known pharmaceutical composition, used as intravitreal injection in patients with age-related macular degeneration.