Fusion Protein Blocking VEGF and FGF Angiogenesis Pathways

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Solution Overview

Problem

Current anti-angiogenesis treatments, such as those targeting VEGF, are limited in long-term effectiveness due to compensatory responses from other angiogenic factors, leading to tumor resistance and the need for dual or multi-target inhibition strategies, which often result in unforeseen side effects from small molecule medicaments.

Innovation Solution

Development of a fusion protein combining VEGF and FGF receptor units with an Fc fusion protein to simultaneously inhibit both VEGF and FGF signaling pathways, utilizing a completely human-derived protein sequence for enhanced specificity and affinity.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If single-target anti-VEGF treatment is used, then initial anti-angiogenesis effect is achieved, but tumor resistance develops and long-term effectiveness is limited

Engineering Contradiction:

Improvelong-term effectivenessVSAvoidduration of anti-angiogenesis effect

Core Design Contradiction:

ReliabilityVSDuration of action of moving object

Solution Approach 1:

The fusion protein combines VEGFR extracellular domain and FGFR extracellular domain into a single molecule, enabling it to bind both VEGF and FGF simultaneously. This multi-functional design prevents compensatory angiogenic responses and maintains long-term anti-angiogenesis effectiveness without developing resistance

Inventive Principle:

Principle #6Universality (Multi-functionality)

Solution Approach 2:

The patent merges two separate receptor functions (VEGFR and FGFR) into one fusion protein molecule. By combining these targeting capabilities in a single agent, the treatment achieves sustained anti-angiogenesis effect and avoids the resistance problem associated with sequential single-target therapies

Inventive Principle:

Principle #5Merging (Combining)

2Reliability

If dual or multi-target inhibition is implemented, then long-term anti-angiogenesis effectiveness is improved, but unforeseen side effects occur from small molecule medicaments

Engineering Contradiction:

Improvelong-term effectivenessVSAvoidside effects

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent changes the molecular form from small molecule medicaments to a protein-based fusion protein. This parameter change maintains multi-target inhibition capability while improving safety profile, as the fusion protein exhibits higher specificity and fewer off-target effects compared to small molecule antagonists

Inventive Principle:

Principle #35Parameter changes

3Adaptability or versatility

If small molecule multi-target antagonists are used, then dual-target inhibition is achieved, but lack of specificity causes unexpected side effects

Engineering Contradiction:

Improvemulti-target inhibition capabilityVSAvoidspecificity

Core Design Contradiction:

Adaptability or versatilityVSReliability

Solution Approach 1:

The fusion protein is constructed as a composite of VEGFR extracellular domain and FGFR extracellular domain, creating a molecule with built-in specificity for both VEGF and FGF. This composite structure provides inherent selectivity through receptor-ligand binding mechanisms, avoiding the non-specific binding issues of small molecule multi-target antagonists

Inventive Principle:

Principle #40Composite materials

Data Source

PatentEP2711377B1Fusion protein for antagonizing angiogenesis inducible factors and uses thereof

Publication Date: 2017.10.18 REMEGEN CO LTD

AI summary

Disclosed are a fusion protein for inhibiting angiogenesis and uses thereof, and further disclosed are a fusion protein for VEGF receptor and FGF receptor and uses of the same in the treatment of diseases associated with regulation of angiogenesis.