IP and EP4 Receptor Antagonist Combination for 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) secretion.

Innovation Solution

Administering a combination of IP receptor antagonists and EP4 receptor antagonists to decrease VEGF secretion, thereby inhibiting neovascularization, with specific pharmaceutical compositions and formulations for ophthalmic use.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If IP receptor antagonist alone is administered, then some inhibition of neovascularization is achieved, but the inhibition is insufficient to effectively treat choroidal neovascularization

Engineering Contradiction:
Improveeffectiveness of neovascularization inhibitionVSAvoidtreatment regimen complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent combines IP receptor antagonist and EP4 receptor antagonist into a single pharmaceutical composition for co-administration. This merging of two therapeutic agents into one formulation achieves synergistic inhibition of neovascularization while simplifying the treatment regimen, as the combination formula can be administered together rather than requiring separate dosing schedules

Inventive Principle:
Principle #5Merging (Combining)

2Object-affected harmful factors

If VEGF secretion is not adequately inhibited, then neovascularization progresses leading to vision loss, but current single-agent treatments fail to sufficiently decrease VEGF levels

Engineering Contradiction:
ImproveVEGF-mediated neovascularization damageVSAvoidVEGF secretion levels
Core Design Contradiction:
Object-affected harmful factorsVSQuantity of substance

Solution Approach 1:

The patent introduces EP4 receptor antagonist as an intermediary mechanism to enhance the inhibition of VEGF secretion. By blocking EP4 receptors in addition to IP receptors, the treatment intercepts another prostanoid signaling pathway that contributes to VEGF production, thereby achieving more complete suppression of VEGF levels and downstream neovascularization

Inventive Principle:
Principle #24Intermediary (Mediator)

Data Source

PatentUS9295665B2Inhibition of neovascularization by simultaneous inhibition of prostanoid IP and EP4 receptors
Publication Date: 2016.03.29 ALLERGAN INC
  • US9295665B2 patent drawing
  • US9295665B2 patent drawing
  • US9295665B2 patent drawing

AI summary

There are provided inter alia methods and compounds useful for decreasing neovascularization (e.g., choroidal neovascularization) in a subject in need thereof.