Fusion Peptide for Bone Tissue Regeneration

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Solution Overview

Problem

Current treatments for bone diseases, such as osteoporosis, face challenges with the short half-life and side effects of parathyroid hormone (PTH) therapies, and insufficient bone regeneration from physiologically active factors in medical devices, leading to poor patient compliance and limited efficacy.

Innovation Solution

A pharmaceutical composition and biomaterial featuring a fusion peptide with a bone-tissue selective peptide bound to PTH or a fragment thereof, enhancing stability and selectivity for bone tissue regeneration, which is chemically synthesized and linked using crosslinking agents for improved bone formation and integration.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Productivity

If PTH is administered to promote bone formation, then bone regeneration efficacy is improved, but half-life is short and side effects increase

Engineering Contradiction:
Improvebone regeneration efficacyVSAvoidhalf-life
Core Design Contradiction:
ProductivityVSDuration of action of moving object

Solution Approach 1:

The patent creates a fusion peptide that combines PTH (responsible for bone formation) with a bone-targeting peptide sequence. This composite structure allows the PTH component to maintain its bone-regenerative activity while the bone-targeting peptide component directs selective binding to bone tissue and extends circulation half-life, thereby resolving the contradiction between efficacy and duration

Inventive Principle:
Principle #40Composite materials

Solution Approach 2:

The bone-targeting peptide acts as an intermediary that mediates between the PTH molecule and the bone tissue. It extends the circulation time of PTH by protecting it from degradation and facilitates selective delivery to bone tissue, thus improving both half-life and targeted efficacy while reducing systemic side effects

Inventive Principle:
Principle #24Intermediary (Mediator)

2Productivity

If PTH is administered to promote bone formation, then bone regeneration efficacy is improved, but side effects increase

Engineering Contradiction:
Improvebone regeneration efficacyVSAvoidside effects
Core Design Contradiction:
ProductivityVSObject-generated harmful factors

Solution Approach 1:

The fusion peptide incorporates a bone-targeting peptide sequence that provides local specificity to bone tissue. This allows the PTH component to exert its bone-forming effects specifically at the bone site while minimizing exposure to other tissues, thereby reducing systemic side effects while maintaining local efficacy

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The bone-targeting peptide serves as a mediator that directs PTH specifically to bone tissue through selective binding. This targeted delivery mechanism ensures that bone regeneration effects are concentrated at the intended site while reducing off-target effects and systemic side effects

Inventive Principle:
Principle #24Intermediary (Mediator)

3Reliability

If physiologically active factors are released from medical device surfaces, then bone integration is improved, but stability is insufficient due to decomposition

Engineering Contradiction:
Improvebone integrationVSAvoidstability
Core Design Contradiction:
ReliabilityVSStability of the object's composition

Solution Approach 1:

The fusion peptide combines PTH with a bone-targeting peptide to create a more stable composite molecule. The bone-targeting peptide component provides structural stability and protects the PTH component from enzymatic degradation, while maintaining the ability to bind to bone tissue and promote integration

Inventive Principle:
Principle #40Composite materials

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 fusion peptide composition demonstrates extended half-life and increased bone regeneration efficacy, reducing side effects and improving patient compliance, while selectively binding to bone tissue for enhanced osteoanagenesis and osseointegration in medical devices.

Implementation Method 1

a fusion peptide in which a bone tissue-selective peptide bound to parathyroid hormone (PTH) or a fragment thereof

Methodology Applied
Scientific EffectChemical bonding: Chemical Bonding

Implementation Method 2

selectively binding to bone tissue for enhanced osteoanagenesis and osseointegration in medical devices

Methodology Applied
Scientific EffectSelective binding: Adsorption

Data Source

PatentEP3498291B1Pharmaceutical composition and biomaterial comprising fusion peptide having parathyroid hormone (PTH) conjugated with peptide selective for bone tissue
Publication Date: 2024.01.03 NIBEC
  • EP3498291B1 patent drawingFigure 1(A)~1(B)
  • EP3498291B1 patent drawingFigure 2(A)~2(B)
  • EP3498291B1 patent drawingFigure 3~4(D)

AI summary

The present invention relates to a pharmaceutical composition for preventing or treating bone diseases comprising a fusion peptide in which a bone tissue-selective peptide bound to parathyroid hormone (PTH) or a fragment thereof. More particularly, the present invention relates to a pharmaceutical composition and biomaterial for preventing or treating bone diseases comprising a fusion peptide in which a bone tissue-selective peptide represented by an amino acid sequence of SEQ ID NO. 3 bound to parathyroid hormone (PTH) or a fragment thereof represented by an amino acid sequence of SEQ ID NO. 4 or 5. The fusion peptide can improve effects of PTH by selectively binding to bone tissue and can reduce administration frequency by increasing the half-life. The fusion peptide can be used as a subcutaneous or intravenous injection-type pharmaceutical composition for treating osteoporosis and fracture, and can be used in combination with a medical device for tissue recovery to increase formation of bone tissue. In addition, when the fusion peptide is bound to the surface of dental and orthopedic medical devices, transplantation stability of the medical device can be improved through improved osseointegration between the medical device and new bone.