IP Receptor Antagonist Inhibits Choroidal Neovascularization

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Solution Overview

Problem

Current treatments are inadequate in effectively reducing neovascularization, particularly choroidal neovascularization associated with age-related macular degeneration, which leads to vision loss due to excessive vascular endothelial growth factor (VEGF) levels.

Innovation Solution

Administration of an effective amount of an IP receptor antagonist, such as Formula I or Formula II, to inhibit VEGF secretion and reduce neovascularization in subjects, including those with choroidal neovascularization.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Productivity

If VEGF levels are increased to stimulate neovascularization, then blood vessel formation is enhanced, but vision loss and retinal tissue destruction occur

Engineering Contradiction:
Improveneovascularization rateVSAvoidvision loss
Core Design Contradiction:
ProductivityVSObject-affected harmful factors

Solution Approach 1:

The patent identifies VEGF as a harmful factor causing vision loss through excessive neovascularization, yet recognizes its physiological role in wound healing and tissue repair. The invention converts this harmful effect into a beneficial one by selectively blocking VEGF's pathogenic actions while preserving its therapeutic potential, thereby treating vision loss without compromising tissue regeneration capabilities

Inventive Principle:
Principle #22Blessing in disguise (Convert harm into benefit)

Solution Approach 2:

The patent applies parameter changes by modulating VEGF levels and activity through pharmacological intervention. By adjusting VEGF concentration and signaling pathway activity to optimal ranges, the invention prevents excessive neovascularization that causes vision loss while maintaining sufficient vascularization for tissue health, thus resolving the contradiction between neovascularization rate and vision preservation

Inventive Principle:
Principle #35Parameter changes

2Object-affected harmful factors

If IP receptor antagonists are administered to inhibit VEGF secretion, then neovascularization is reduced, but potential side effects from receptor blockade may occur

Engineering Contradiction:
ImproveneovascularizationVSAvoidreceptor blockade side effects
Core Design Contradiction:
Object-affected harmful factorsVSObject-generated harmful factors

Solution Approach 1:

The patent applies local quality by achieving selective blocking of VEGF signaling at specific tissue locations and molecular targets. The IP receptor antagonist is designed to selectively inhibit VEGF secretion and signaling in the retina and choroid while minimizing systemic effects, thereby reducing neovascularization without causing widespread receptor blockade side effects

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The patent uses an intermediary approach by introducing a pharmacological agent that mediates between VEGF signaling and the desired therapeutic outcome. The IP receptor antagonist acts as a selective mediator that blocks VEGF's harmful neovascularization effects while preserving other physiological functions, thus reducing harmful factors without generating excessive side effects

Inventive Principle:
Principle #24Intermediary (Mediator)

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

The IP receptor antagonist effectively decreases VEGF secretion and inhibits neovascularization, as demonstrated by reducing the area of laser-induced choroidal neovascularization, thereby addressing the issue of vision loss associated with excessive VEGF levels.

Implementation Method 1

administering to the subject an effective amount of an IP receptor antagonist, thereby decreasing the neovascularization

Methodology Applied
Scientific EffectReceptor antagonism:

Data Source

PatentUS9321745B2Inhibition of neovascularization by inhibition of prostanoid IP receptors
Publication Date: 2016.04.26 ALLERGAN INC
  • US9321745B2 patent drawing
  • US9321745B2 patent drawing
  • US9321745B2 patent drawing

AI summary

There are provided inter alia methods and compounds useful for decreasing choroidal neovascularization in a subject in need thereof.