Omidenepag EP2 Agonist Retinal Vasodilation Nerve Protection

Solution Overview

Problem

Current treatments for retinal nerve cell disorders and blood flow issues related to the retina lack effective agents that can significantly dilate retinal blood vessels and improve blood flow, which are crucial for protecting retinal nerve cells and treating conditions like glaucoma and diabetic retinopathy.

Innovation Solution

Omidenepag, its esters, or salts are used as active ingredients in a medicament to provide retinal vasodilatory action, nerve cell protection, and blood flow improvement, offering a novel pharmaceutical use by significantly dilating retinal blood vessels and increasing blood flow rates.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional medicaments (calcium channel blockers, beta-blockers, alpha1-receptor blockers) are used to treat retinal nerve cell disorders, then some protective effect may be achieved, but they cannot significantly dilate retinal blood vessels and improve blood flow

Engineering Contradiction:

Improveretinal nerve cell protectionVSAvoidblood flow improvement

Core Design Contradiction:

ReliabilityVSSpeed

Solution Approach 1:

The patent applies parameter changes by using omidenepag, an EP2 receptor agonist, which activates a different pharmacological pathway compared to conventional medications. This activates prostacyclin signaling and increases cAMP levels in vascular smooth muscle cells, leading to significant vasodilation and improved blood flow while simultaneously protecting retinal nerve cells through anti-apoptotic effects

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent demonstrates multi-functionality by showing that omidenepag simultaneously achieves multiple therapeutic effects: it dilates retinal blood vessels, improves blood flow, and protects retinal nerve cells from apoptosis. This single agent addresses both the vascular and neuroprotective aspects of retinal diseases, eliminating the need for combination therapy with conventional medications

Inventive Principle:

Principle #6Universality (Multi-functionality)

2Speed

If medications aimed at improving retinal blood flow are applied, then blood flow may be enhanced, but they lack the ability to directly protect retinal nerve cells from functional breakdown

Engineering Contradiction:

Improveblood flowVSAvoidretinal nerve cell protection

Core Design Contradiction:

SpeedVSReliability

Solution Approach 1:

The patent demonstrates multi-functionality by showing that omidenepag simultaneously achieves multiple therapeutic effects: it dilates retinal blood vessels, improves blood flow, and protects retinal nerve cells from apoptosis. This single agent addresses both the vascular and neuroprotective aspects of retinal diseases, eliminating the need for combination therapy with conventional medications

Inventive Principle:

Principle #6Universality (Multi-functionality)

3Stress or pressure

If existing glaucoma therapeutic agents are used, then intraocular pressure may be lowered, but they do not provide significant retinal vasodilatory action

Engineering Contradiction:

Improveintraocular pressureVSAvoidretinal blood vessel dilation

Core Design Contradiction:

Stress or pressureVSSpeed

Solution Approach 1:

The patent applies parameter changes by using omidenepag, an EP2 receptor agonist, which activates a different pharmacological pathway compared to conventional medications. This activates prostacyclin signaling and increases cAMP levels in vascular smooth muscle cells, leading to significant vasodilation and improved blood flow while simultaneously protecting retinal nerve cells through anti-apoptotic effects

Inventive Principle:

Principle #35Parameter changes

Applied Scientific Principles

This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.

Function Achieved in This Case

Omidenepag-based medicaments effectively dilate retinal blood vessels, enhance blood flow, and protect retinal nerve cells, providing a therapeutic benefit for retinal disorders by suppressing nerve cell death and improving visual function.

Implementation Method 1

ONO-AE1-259-01, which is an EP2 receptor agonist, dilates retinal blood vessels and has a retinal neuroprotective action

Methodology Applied

Scientific EffectEP2 receptor agonism:

Implementation Method 2

omidenepag, an ester thereof, or a salt thereof can significantly dilate retinal blood vessels as compared with other EP2 agonists, and thereby significantly increase blood flow

Methodology Applied

Scientific EffectVasodilation:

Implementation Method 3

omidenepag, an ester thereof, or a salt thereof can significantly dilate retinal blood vessels as compared with other EP2 agonists, and thereby significantly increase blood flow. This finding has led to the completion of the present invention. Specifically, the present invention provides the following: A medicament for retinal vasodilatory action, retinal nerve cell protection, and/or retinal blood flow improvement

Methodology Applied

Scientific EffectNeuroprotection:

Data Source

PatentUS10940144B2Drug containing pyridylaminoacetic acid compound

Publication Date: 2021.03.09 SANTEN PHARMACEUTICAL CO LTD

AI summary

The present invention aims to find a novel pharmaceutical use of omidenepag, esters thereof, or salts thereof. The present inventors have made intensive studies to find a novel pharmaceutical use of omidenepag, an ester thereof, or a salt thereof, and have found as a result that omidenepag, an ester thereof, or a salt thereof significantly dilates retinal blood vessels, and significantly increases blood flow. Therefore, omidenepag, an ester thereof, or a salt thereof is expected to protect retinal nerve cells and be useful for prevention and/or treatment of ophthalmic diseases involving retinal nerve cell disorder.