PEPITEM Peptide Bone Formation Stimulation

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Solution Overview

Problem

Current therapies for osteoporosis and bone-related diseases primarily focus on reducing bone resorption without effectively stimulating bone formation, leading to limitations in bone repair and remodeling, and are associated with side effects such as increased fracture risk and abnormal bone density.

Innovation Solution

Administration of a peptide with the amino acid sequence SVTEQGAELSNEER (PEPITEM) or its variants to patients and bone cells, which stimulates osteoblast activity and balances osteoclast and osteoblast activity to promote bone production and reduce bone loss.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Loss of substance

If anti-resorptive bisphosphonates are used to treat osteoporosis, then bone resorption is reduced, but bone formation is hindered and fracture risk increases

Engineering Contradiction:
Improvebone resorptionVSAvoidbone strength
Core Design Contradiction:
Loss of substanceVSStrength

Solution Approach 1:

Instead of only inhibiting bone resorption (conventional approach), the patent applies inversion by simultaneously stimulating bone formation through peptide administration. This dual-action approach reverses the imbalance caused by conventional therapies, promoting both bone production and reduced resorption to improve overall bone strength.

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

Solution Approach 2:

The patent changes the therapeutic parameter from single-target inhibition (bisphosphonates targeting osteoclasts) to dual-target modulation (peptide targeting both osteoblasts and osteoclasts). This parameter change enables simultaneous enhancement of bone formation and inhibition of resorption, resolving the contradiction between reducing bone loss and maintaining bone strength.

Inventive Principle:
Principle #35Parameter changes

2Loss of substance

If anti-RANKL antibody (denosumab) is used, then bone resorption is reduced, but bone formation is not affected

Engineering Contradiction:
Improvebone resorptionVSAvoidbone formation
Core Design Contradiction:
Loss of substanceVSProductivity

Solution Approach 1:

The patent merges the functions of bone resorption inhibition and bone formation stimulation into a single therapeutic approach. The peptide compound simultaneously targets both osteoclasts (to reduce resorption) and osteoblasts (to enhance formation), combining two previously separate therapeutic actions into one integrated treatment.

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The peptide compound exhibits multi-functionality by acting on both osteoclasts and osteoblasts. This universal approach allows a single agent to perform multiple functions: inhibiting bone resorption while simultaneously stimulating bone formation, thereby addressing both aspects of bone health rather than treating them separately.

Inventive Principle:
Principle #6Universality (Multi-functionality)

3Loss of substance

If cathespin K inhibitor (odanacatib) is used, then bone resorption is reduced, but stroke risk increases

Engineering Contradiction:
Improvebone resorptionVSAvoidstroke risk
Core Design Contradiction:
Loss of substanceVSObject-affected harmful factors

Solution Approach 1:

The patent introduces a peptide compound as an intermediary therapeutic agent that mediates between bone resorption inhibition and bone formation stimulation. This intermediary approach allows reduction of bone loss while avoiding the severe side effects (such as stroke risk) associated with direct cathespin K inhibition, by using a more balanced dual-action mechanism.

Inventive Principle:
Principle #24Intermediary (Mediator)

4Object-affected harmful factors

If existing therapies focus on reducing joint pain and slowing bone damage, then symptom relief is achieved, but bone repair and remodeling are not effectively stimulated

Engineering Contradiction:
Improvejoint pain and bone damageVSAvoidbone repair and remodeling
Core Design Contradiction:
Object-affected harmful factorsVSProductivity

Solution Approach 1:

The patent applies preliminary action by stimulating bone formation before and during the repair process. Instead of only providing symptomatic relief and slowing damage, the peptide therapy proactively promotes bone production and remodeling activities, preparing and supporting the bone repair process rather than merely preventing deterioration.

Inventive Principle:
Principle #10Preliminary action

Data Source

PatentUS20240226227A9Bone disease treatment
Publication Date: 2024.07.11 THE UNIV OF BIRMINGHAM
  • US20240226227A9 patent drawing
  • US20240226227A9 patent drawing
  • US20240226227A9 patent drawing

AI summary

The present invention concerns methods of reducing bone loss and/or stimulating bone production comprising administering an effective amount of a peptide comprising the amino acid sequence SVTEQGAELSNEER (SEQ ID NO:1), or variants thereof, to a patient and/or bone cells. The present invention also concerns methods of treatment and/or prophylaxis of musculoskeletal loss and/or damage in a patient, comprising administering an effective amount of the peptide.