Endothelin Receptor Antagonists for Retinal Perfusion in Diabetic Retinopathy

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Solution Overview

Problem

Current treatments for ocular diseases such as glaucoma, diabetic retinopathy, retinal vein occlusion, non-arteritic anterior ischemic optic neuropathy, arteritic anterior ischemic optic neuropathy, and retinopathy of prematurity are inadequate, with no effective methods to improve blood flow and reduce inflammation, leading to potential vision loss.

Innovation Solution

Administration of endothelin receptor antagonists, specifically Edonentan and A-182086, to the eye using topical, intra-ocular, or implant delivery methods to improve tissue perfusion and reduce inflammation.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current treatments for ocular diseases are used, then existing therapy options are maintained, but blood flow improvement and inflammation reduction are insufficient leading to vision loss

Engineering Contradiction:
Improveeffectiveness of treatmentVSAvoidvision loss
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent introduces endothelin receptor antagonists (ERA) as a new pharmacological parameter/class of drugs to treat ocular diseases. This represents a fundamental change in treatment parameter from existing therapies to ERA mechanism, which blocks endothelin-1 binding to ETA and ETB receptors, thereby improving blood flow and reducing inflammation to prevent vision loss

Inventive Principle:
Principle #35Parameter changes

2Quantity of substance

If endothelin receptor antagonists are administered to improve tissue perfusion, then retinal and optic nerve perfusion is enhanced, but intraocular pressure must be controlled

Engineering Contradiction:
Improvetissue perfusionVSAvoidintraocular pressure
Core Design Contradiction:
Quantity of substanceVSStress or pressure

Solution Approach 1:

The patent utilizes parameter changes by administering ERA at controlled doses and frequencies to achieve optimal tissue perfusion while managing intraocular pressure. The treatment protocol is adjusted based on disease stage and patient response, representing a dynamic parameter adjustment approach

Inventive Principle:
Principle #35Parameter changes

Data Source

PatentUS20260076948A1Treatment of diabetic retinopathy using endothelin receptor antagonists
Publication Date: 2026.03.19 PERFUSE THERAPEUTICS INC
  • US20260076948A1 patent drawing
  • US20260076948A1 patent drawing
  • US20260076948A1 patent drawing

AI summary

The present disclosure relates to the discovery that certain diseases of the eye that profoundly affect the human visual system and, as a result, quality of life, may be treated using Edonentan or A-182086. Edonentan or A-182086 can be used alone or in combination with an intra-ocular pressure (IOP) reducing agent, a neuroprotective agent, an anti-VEGF agent, or all, for example. Using Edonentan or A-182086, alone or in combination with an additional agent, provides increased perfusion to the retina in certain diseases and reduces damage to retinal cells.