Compositions, methods and kits for treating complement related disorders

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Solution Overview

Problem

Current treatments for complement-related disorders, such as age-related macular degeneration and rheumatoid arthritis, are limited by the availability of effective FDA-approved inhibitors and often require frequent injections with significant side effects, while existing recombinant proteins like STAC have non-functional CD59 portions and require membrane targeting for efficacy.

Innovation Solution

Development of a recombinant chimeric protein combining the complement regulatory properties of CD46, CD55, and CD59, engineered to be membrane-independent, with specific mutations in the GPI anchoring domains, and delivered via a gene therapy approach using AAV vectors to target both classical and alternative complement pathways.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If recombinant proteins like STAC are used to inhibit complement activation, then complement-related disorders can be treated, but the CD59 portion is non-functional and membrane targeting is required

Engineering Contradiction:
Improvecomplement inhibition efficacyVSAvoidprotein structure complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The invention divides the complement regulation function into separate functional domains (CD46, CD55, CD59) and combines them in a segmented chimeric protein structure, where each domain contributes specific inhibitory activities against different complement pathways

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The invention extracts and removes the GPI anchoring domain from the CD59 portion of the chimeric protein, making it membrane-independent and soluble, thereby eliminating the requirement for membrane targeting while preserving complement inhibition function

Inventive Principle:
Principle #2Taking out (Extraction)

2Duration of action of moving object

If frequent injections of complement inhibitors are administered, then chronic complement-related disorders can be treated, but significant side effects occur

Engineering Contradiction:
Improveduration of complement inhibitionVSAvoidside effects
Core Design Contradiction:
Duration of action of moving objectVSObject-affected harmful factors

Solution Approach 1:

The invention changes the pharmacokinetic parameters of complement inhibition by using a chimeric protein with extended half-life characteristics, reducing the frequency of administration and cumulative side effects while maintaining therapeutic efficacy

Inventive Principle:
Principle #35Parameter changes

3Reliability

If membrane-targeted complement inhibitors are used, then complement activation can be inhibited at the cell surface, but delivery efficiency is reduced

Engineering Contradiction:
Improvecomplement inhibition efficacyVSAvoiddelivery efficiency
Core Design Contradiction:
ReliabilityVSProductivity

Solution Approach 1:

The invention inverts the traditional membrane-targeted approach by creating a soluble, membrane-independent chimeric protein that circulates in body fluids and inhibits complement activation in the extracellular space, thereby improving delivery efficiency to target tissues

Inventive Principle:
Principle #13The other way round (Inversion)

Data Source

PatentEP3186269B1Compositions, methods and kits for treating complement related disorders
Publication Date: 2021.03.10 TUFTS UNIV
  • EP3186269B1 patent drawingFigure 1A~1B
  • EP3186269B1 patent drawingFigure 2A~2D
  • EP3186269B1 patent drawingFigure 3A~3C

AI summary

Compositions, methods and kits are provided for treating complement related disorders in a subject with protein in combination having protein fusions of at least two of a CD46 protein, a CD55 protein and a CD59 protein or with a recombinant chimeric protein having at least two of a CD46 protein, a CD55 protein and a CD59 protein or with nucleic acids encoding these proteins. The composition negatively modulates classical and alternative complement pathways thereby treating complement related disorder such as macular degeneration, age-related macular degeneration, diabetic retinopathy, inflammatory bowel disease, thyroiditis, cryoglobulinaemia, fetal loss, organ graft rejection, cancer, etc.