Chemically Modified mRNA for CFTR Gene Delivery

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Solution Overview

Problem

Current treatments for diseases associated with the CFTR gene, such as cystic fibrosis, congenital absence of the vas deferens, and chronic obstructive lung disease, are ineffective and costly, with viral gene therapy approaches leading to immune reactions and insufficient hCFTR expression.

Innovation Solution

Chemically modified mRNA encoding the CFTR gene, complexed with PLGA-based nanoparticles, is administered intratracheally or intravenously to enhance stability, reduce immunogenicity, and achieve targeted expression of functional CFTR protein in lung tissues.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If viral vectors (adenoviruses or adeno-associated viruses) are used to deliver CFTR gene, then gene delivery is achieved, but immune reactions occur and hCFTR expression is insufficient

Engineering Contradiction:
ImprovehCFTR expression levelVSAvoidimmune reaction
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent uses chemically modified mRNA as an intermediary carrier to deliver CFTR gene information, avoiding direct viral vector delivery. The mRNA is complexed with biocompatible PLGA nanoparticles, which serve as a non-immunogenic delivery vehicle, thereby eliminating immune reactions while achieving sufficient hCFTR protein expression in lung tissues

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent employs chemically modified nucleotides (such as pseudouridine, 5-methylcytidine, and N6-methyladenosine) to alter the chemical parameters of mRNA. These modifications enhance mRNA stability, reduce immunogenicity, and improve translation efficiency, thereby achieving reliable hCFTR expression without triggering immune responses

Inventive Principle:
Principle #35Parameter changes

2Duration of action of stationary object

If repeated administration of viral vectors is performed, then gene delivery is maintained, but immune reactions worsen

Engineering Contradiction:
Improvegene delivery durationVSAvoidimmune reaction intensity
Core Design Contradiction:
Duration of action of stationary objectVSObject-affected harmful factors

Solution Approach 1:

The patent replaces repeated viral vector administration with repeatable mRNA nanoparticle delivery. The PLGA nanoparticle-mRNA complex serves as a reusable delivery system that can be administered multiple times without eliciting progressive immune responses, enabling sustained gene delivery over time

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent uses transient mRNA molecules packaged in biodegradable PLGA nanoparticles as disposable delivery vehicles. Each administration provides temporary but sufficient hCFTR expression, and the nanoparticles degrade naturally after delivery, allowing repeated administrations without cumulative immune reactions

Inventive Principle:
Principle #27Cheap short-living objects (Disposable)

Data Source

PatentEP3398963B1Chemically modified mRNA for use in the treatment of a disease associated with the CFTR gene
Publication Date: 2021.09.29 EBERHARD KARLS UNIV TUBINGEN MEDIZINISCHE FAKULTAT
  • EP3398963B1 patent drawingFigure 1A
  • EP3398963B1 patent drawingFigure 1B
  • EP3398963B1 patent drawingFigure 1C

AI summary

The present invention relates to a chemically modified mRNA, a nucleic acid molecule encoding the CFTR cmRNA, a vector comprising said nucleic acid molecule, a host cell comprising said vector, a pharmaceutical composition comprising the CFTR cmRNA, nucleic acid molecule or vector, and to a method for the treatment of a disease associated with the CFTR gene.