Bispecific Anti-VEGFA/VEGFC Formulation for Long-Term Stability

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Solution Overview

Problem

Bispecific antibodies targeting VEGFA and VEGFC face challenges in long-term storage due to instability, leading to aggregation and degradation, which affects their safety and efficacy in clinical applications.

Innovation Solution

A pharmaceutical preparation comprising an anti-VEGFA/VEGFC bispecific binding protein, a buffering agent, a stabilizer, and a surfactant, formulated at a pH of 5.5 to 7.0, which includes specific antigen binding components and a dimeric structure to enhance stability.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Duration of action of stationary object

If bisspecific antibodies are stored for long-term use, then therapeutic efficacy can be maintained, but protein instability causes aggregation and degradation

Engineering Contradiction:

Improvestorage durationVSAvoidprotein stability

Core Design Contradiction:

Duration of action of stationary objectVSReliability

Solution Approach 1:

The patent introduces a buffering agent as an intermediary substance in the pharmaceutical preparation. The buffer maintains optimal pH conditions (pH 5.5-7.0) that prevent protein denaturation and aggregation, thereby stabilizing the bispecific antibody during long-term storage without affecting its therapeutic function.

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent optimizes the pH parameter of the pharmaceutical preparation to a specific range (pH 5.5-7.0) where the bisspecific antibody exhibits maximum stability. By controlling this critical parameter, the patent prevents protein degradation and aggregation that would otherwise occur during long-term storage, resolving the contradiction between storage duration and protein stability.

Inventive Principle:

Principle #35Parameter changes

2Adaptability or versatility

If individual anti-VEGF-A and anti-VEGF-C molecules are used separately, then each target can be blocked, but administration complexity increases

Engineering Contradiction:

Improvetarget coverageVSAvoidadministration complexity

Core Design Contradiction:

Adaptability or versatilityVSDevice complexity

Solution Approach 1:

The patent merges two separate antibody functions into a single bisspecific antibody molecule that can simultaneously bind to both VEGF-A and VEGF-C. This consolidation eliminates the need for separate administration of two different antibodies, reducing administration complexity while maintaining the ability to block both targets effectively.

Inventive Principle:

Principle #5Merging (Combining)

Solution Approach 2:

The bisspecific antibody serves multiple functions within a single molecule: it can bind to VEGF-A, bind to VEGF-C, and potentially block both simultaneously. This multi-functionality allows a single pharmaceutical preparation to achieve what would otherwise require two separate treatments, simplifying the administration process.

Inventive Principle:

Principle #6Universality (Multi-functionality)

Data Source

PatentEP4663202A1Pharmaceutical preparation containing Anti-vegfa and Anti-vegfc bispecific binding protein

Publication Date: 2025.12.17 INNOVENT BIOLOGICS (SUZHOU) CO LTD

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AI summary

The present application provides a pharmaceutical preparation, a use thereof, and a kit comprising the pharmaceutical preparation. The pharmaceutical preparation comprises: (1) an anti-VEGFA/VEGFC bispecific binding protein, (2) a buffering agent, (3) a stabilizer, (4) a surfactant, wherein the pharmaceutical preparation has a pH of 5.5 to 7.0. The pharmaceutical preparation shows long-term stability and exhibits anti-neovascularization effects.