CTP-Modified Growth Hormone for Reduced Dosing Frequency

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Solution Overview

Problem

Peptide drugs face challenges due to short circulatory half-lives and instability, leading to frequent administration and discomfort, as well as potential immune responses and toxic side effects, limiting their therapeutic effectiveness.

Innovation Solution

Modification of growth hormone with chorionic gonadotropin carboxy-terminal peptides (CTPs) to extend half-life, enhance stability, and reduce dosing frequency, while maintaining biological activity.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If growth hormone is administered frequently to maintain effective plasma concentration, then therapeutic efficacy is maintained, but patient comfort deteriorates and dosing complexity increases

Engineering Contradiction:
Improvetherapeutic efficacyVSAvoidpatient comfort
Core Design Contradiction:
ReliabilityVSEase of operation

Solution Approach 1:

The patent modifies the growth hormone molecule by attaching carboxy-terminal peptides from chorionic gonadotropin, which changes the pharmacokinetic parameters of the hormone. This structural modification extends the circulatory half-life from several hours to a prolonged duration, allowing less frequent administration while maintaining therapeutic efficacy

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The invention creates a composite peptide structure by combining growth hormone with carboxy-terminal peptides from chorionic gonadotropin. This hybrid molecule integrates the therapeutic function of growth hormone with the extended circulation properties of the chorionic gonadotropin peptide, achieving both efficacy and reduced dosing frequency

Inventive Principle:
Principle #40Composite materials

2Reliability

If growth hormone is administered frequently to maintain therapeutic levels, then pharmacological efficacy is maintained, but treatment complexity increases

Engineering Contradiction:
Improvepharmacological efficacyVSAvoiddosing regimen complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

By modifying the molecular structure of growth hormone with attached peptides, the patent changes the clearance rate and half-life parameters. This allows the drug to maintain therapeutic levels for extended periods, simplifying the dosing regimen from frequent administrations to less frequent injections

Inventive Principle:
Principle #35Parameter changes

3Reliability

If peptide drugs are administered by frequent infusion, then effective plasma concentration is maintained, but patient comfort and compliance deteriorate

Engineering Contradiction:
Improveeffective plasma concentrationVSAvoidpatient comfort
Core Design Contradiction:
ReliabilityVSEase of operation

Solution Approach 1:

The patent alters the pharmacokinetic parameters of growth hormone by attaching carboxy-terminal peptides, extending the circulatory half-life and enabling sustained effective plasma concentrations with less frequent dosing, thereby improving patient comfort and compliance

Inventive Principle:
Principle #35Parameter changes

4Reliability

If dosing frequency is increased to maintain therapeutic levels, then treatment reliability is improved, but loss of time and treatment burden increase

Engineering Contradiction:
Improvetreatment reliabilityVSAvoiddosing time
Core Design Contradiction:
ReliabilityVSLoss of time

Solution Approach 1:

The structural modification of growth hormone with carboxy-terminal peptides changes the elimination kinetics, extending the duration of action. This allows treatment reliability to be maintained with reduced dosing frequency, thereby reducing the time burden on patients

Inventive Principle:
Principle #35Parameter changes

Data Source

PatentEP3482765B1Long-acting growth hormone and methods of producing same
Publication Date: 2024.02.28 OPKO BIOLOGICS LTD
  • EP3482765B1 patent drawingFigure 1~2
  • EP3482765B1 patent drawingFigure 3
  • EP3482765B1 patent drawingFigure 4A~4B

AI summary

A chorionic gonadotropin carboxy terminal peptide (CTP)-modified polypeptide comprising a growth hormone for use in a method of reducing the dosing frequency of a growth hormone in a human adult subject, wherein the CTP-modified polypeptide comprises one chorionic gonadotropin carboxy terminal peptide (CTP) attached to the amino terminus of the growth hormone, and two chorionic gonadotropin CTPs attached to the carboxy terminus of the growth hormone, and optionally a signal peptide attached to the amino terminus of the amino terminal CTP, wherein the method comprises administering to the subject a therapeutically effective amount of the CTP-modified polypeptide.