Retinal Protective Peptides With Aqueous Stability for Intravitreal Use

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Solution Overview

Problem

Existing Fas inhibitors, such as Met-12, have poor aqueous solubility and stability, making them difficult to formulate into effective solutions for intravitreal injections, which are necessary for treating ocular disorders like glaucoma and retinal diseases.

Innovation Solution

Development of oligopeptides or peptidomimetics with specific amino acid sequences and linkers that enhance solubility and stability, allowing for effective formulation in aqueous solutions suitable for intravitreal administration.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If existing Fas inhibitors like Met-12 are used, then they can inhibit Fas-mediated cell death, but they have poor aqueous solubility and stability making them difficult to formulate for intravitreal injection

Engineering Contradiction:

Improveinhibition of Fas-mediated cell deathVSAvoidformulation into aqueous solutions

Core Design Contradiction:

ReliabilityVSEase of manufacture

Solution Approach 1:

The patent modifies the physical and chemical parameters of the Fas inhibitor by changing its molecular structure from Met-12 to oligopeptides with specific amino acid sequences (Formulas I and II). These structural parameter changes improve aqueous solubility and stability while maintaining Fas inhibition activity, enabling effective intravitreal formulation

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent creates composite oligopeptide structures combining multiple amino acid residues with specific properties (hydrophilic, hydrophobic, charged residues) in defined sequences. This composite approach achieves both solubility enhancement and biological activity retention, resolving the formulation challenge

Inventive Principle:

Principle #40Composite materials

2Reliability

If existing Fas inhibitors like Met-12 are used, then they can protect photoreceptor cells, but they have poor stability making them difficult to administer

Engineering Contradiction:

Improveprotection of photoreceptor cellsVSAvoidstability of Fas inhibitor

Core Design Contradiction:

ReliabilityVSStability of the object's composition

Solution Approach 1:

The patent changes the stability parameters of the Fas inhibitor by designing oligopeptides with specific amino acid compositions and sequences (Formulas I and II) that resist degradation and maintain structural integrity in aqueous environments, thereby improving stability while preserving photoreceptor protection capability

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent introduces stabilizing amino acid residues and structural motifs as intermediaries that protect the active Fas-inhibiting portion of the molecule from degradation, enhancing overall stability without compromising the core protective function

Inventive Principle:

Principle #24Intermediary (Mediator)

Data Source

PatentUS20260049106A1Peptide compositions and methods of use

Publication Date: 2026.02.19 ONL THERAPEUTICS INC

AI summary

Provided herein are compositions including peptides, pharmaceutical preparations thereof, and methods of preventing photoreceptor death therewith and protecting of retinal cells, including, but not limited to, photoreceptors and retinal pigment epithelium, from Fas- or TRAIL-mediated apoptosis.