Transferrin Receptor-Binding Peptide for Blood-Brain Barrier Transport

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Solution Overview

Problem

The blood-brain barrier restricts the delivery of therapeutic compounds to the central nervous system, limiting the effectiveness of treatments for conditions like Hunter syndrome and Alzheimer's disease, as most drugs cannot pass through.

Innovation Solution

A peptide with an affinity for the human transferrin receptor, comprising specific variable regions of an anti-hTfR heavy chain antibody, is developed to efficiently traverse the blood-brain barrier, allowing compounds to reach the central nervous system.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If the blood-brain barrier is present to protect the central nervous system, then the safety and homeostasis of the CNS is improved, but the delivery of therapeutic compounds to the CNS is hindered

Engineering Contradiction:
ImproveCNS homeostasis protectionVSAvoidDrug delivery efficiency
Core Design Contradiction:
ReliabilityVSProductivity

Solution Approach 1:

The patent uses transferrin receptor-mediated transcytosis as an intermediary mechanism to transport therapeutic compounds across the blood-brain barrier. The transferrin receptor acts as a mediator that facilitates the passage of drugs from the bloodstream into the CNS without compromising the barrier's protective function, thereby resolving the contradiction between protection and delivery.

Inventive Principle:
Principle #24Intermediary (Mediator)

2Adaptability or versatility

If conventional drugs are administered systemically, then the treatment coverage is improved, but the ability to reach the central nervous system is lost

Engineering Contradiction:
ImproveTreatment coverageVSAvoidCNS target achievement
Core Design Contradiction:
Adaptability or versatilityVSReliability

Solution Approach 1:

The patent changes the physical-chemical parameters of drugs by conjugating them with transferrin or transferrin-binding proteins. This modification alters the drugs' ability to interact with the blood-brain barrier, enabling them to undergo transcytosis and reach the CNS while maintaining systemic administration benefits.

Inventive Principle:
Principle #35Parameter changes

3Stability of the object's composition

If the blood-brain barrier restricts substance exchange, then the biochemical homeostasis of CNS cells is maintained, but the effectiveness of enzyme replacement therapy is reduced

Engineering Contradiction:
ImproveCNS biochemical homeostasisVSAvoidEnzyme replacement therapy effectiveness
Core Design Contradiction:
Stability of the object's compositionVSReliability

Solution Approach 1:

The patent employs transferrin-receptor-mediated transcytosis as an intermediary pathway to deliver enzyme replacement therapy agents across the blood-brain barrier. This mechanism allows therapeutic enzymes to reach the CNS while the barrier continues to maintain biochemical homeostasis by selectively facilitating this specific transport pathway.

Inventive Principle:
Principle #24Intermediary (Mediator)

Applied Scientific Principles

This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.

Function Achieved in This Case

The peptide effectively transports therapeutic compounds across the blood-brain barrier, enhancing the delivery of drugs and proteins to the brain, thereby improving treatment efficacy for central nervous system disorders.

Implementation Method 1

a peptide having an affinity for a human transferrin receptor

Methodology Applied
Scientific EffectAffinity binding: Adsorption

Data Source

PatentEP4653533A1Human transferrin receptor-avid peptide
Publication Date: 2025.11.26 JCR PHARMACEUTICALS CO LTD
  • EP4653533A1 patent drawingFigure 1(1)~1(4)
  • EP4653533A1 patent drawingFigure 2(a)~2(d)
  • EP4653533A1 patent drawingFigure 3(1)~3(3)

AI summary

Provided are a peptide having an affinity for a human transferrin receptor, which can be used for binding to any of compounds (a protein, a nucleic acid, a low-molecular-weight compound, and the like) that needs to exhibit its function in a central nervous system (CNS) and to be allowed to pass through a blood brain barrier, and a use thereof. The peptide is a peptide including, for example, an amino acid sequence selected from the group consisting of amino acid sequences set forth in SEQ ID NOs: 4 to 6, or a variant thereof.