pH-Optimized Soluble VEGFR-3 Trap Composition for Ambient Storage

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Solution Overview

Problem

Current pharmaceutical formulations of soluble VEGFR-3 trap molecules like OPT-302 face challenges in achieving stability at room temperature and are prone to dimer formation, necessitating low-temperature storage, which complicates their development and distribution.

Innovation Solution

A pharmaceutical formulation comprising a soluble VEGFR-3 trap molecule, trehalose, a buffer, and water, with a pH range of 6.5 to 8.0 and trehalose concentration of at least 7.0% w/v, which stabilizes the molecule without requiring low-temperature storage.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of operation

If soluble VEGFR-3 trap molecules are formulated in aqueous solutions, then they can be administered conveniently, but they form dimers rapidly and require low-temperature storage

Engineering Contradiction:

Improveconvenience of administrationVSAvoidstability of the molecule

Core Design Contradiction:

Ease of operationVSStability of the object's composition

Solution Approach 1:

The patent changes the pH parameter of the aqueous formulation to a range of 6.5-8.0, which prevents dimer formation of the soluble VEGFR-3 trap molecule while maintaining its stability at ambient temperatures. This parameter optimization resolves the contradiction by allowing convenient aqueous administration without requiring low-temperature storage.

Inventive Principle:

Principle #35Parameter changes

2Stability of the object's composition

If the molecule is stored at low temperatures, then dimer formation is prevented, but storage and distribution become complicated

Engineering Contradiction:

Improveprevention of dimer formationVSAvoidcomplexity of storage and distribution

Core Design Contradiction:

Stability of the object's compositionVSDevice complexity

Solution Approach 1:

By optimizing the pH parameter to 6.5-8.0 and using specific excipients, the formulation achieves dimer prevention at ambient temperatures, eliminating the need for complex cold chain storage and distribution infrastructure.

Inventive Principle:

Principle #35Parameter changes

3Stability of the object's composition

If the pH is adjusted to prevent dimer formation, then stability is improved, but the formulation may become less compatible with administration requirements

Engineering Contradiction:

Improvestability of the moleculeVSAvoidcompatibility with administration

Core Design Contradiction:

Stability of the object's compositionVSObject-affected harmful factors

Solution Approach 1:

The pH is optimized to a range of 6.5-8.0 that simultaneously prevents dimer formation and maintains compatibility with intravitreal administration, avoiding harmful effects while ensuring stability.

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The formulation uses a composite approach combining the soluble VEGFR-3 trap molecule with specific excipients and buffer systems that work together to maintain both stability and biocompatibility at the optimized pH range.

Inventive Principle:

Principle #40Composite materials

Data Source

PatentUS20250296979A1Pharmaceutical Composition and Method of Using Same

Publication Date: 2025.09.25 VEGENICS PTY LTD

AI summary

Provided herein are pharmaceutical compositions comprising an active agent which is a soluble VEGFR-3 trap molecule. Also provided herein are therapeutic methods and uses involving the pharmaceutical compositions, in particular ocular diseases and disorders, and port devices comprising the pharmaceutical compositions.