Stapled Peptide Conjugates for Extended Half-Life Therapeutics
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Solution Overview
Problem
Therapeutic agents often have short half-lives, requiring frequent administration and higher dosages, which can lead to reduced compliance, higher costs, and increased side effects.
Innovation Solution
Development of peptide conjugates comprising a peptide that modulates receptors like PYY, GLP-1, or GCG, stabilized by a staple at sulfhydryl-containing amino acids, enhancing half-life and stability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If therapeutic agents are administered at higher dosages more frequently, then therapeutic efficacy is maintained, but compliance decreases and costs increase
Solution Approach 1:
The patent applies parameter changes by modifying the molecular structure of peptide therapeutic agents through conjugation with half-life extending moieties. This chemical modification changes the pharmacokinetic parameters of the peptide, specifically extending its biological half-life from minutes to hours or days, thereby reducing the frequency of administration while maintaining therapeutic efficacy and improving patient compliance
2Reliability
If therapeutic agents are administered more frequently, then therapeutic efficacy is maintained, but the risk of side effects increases
Solution Approach 1:
The patent changes the pharmacokinetic parameters of the peptide therapeutic agent by conjugating it with half-life extending moieties. This modification extends the duration of action of the peptide, allowing for less frequent dosing intervals. By reducing the frequency of administration, the cumulative risk of side effects is minimized while maintaining effective therapeutic levels through extended circulation time
3Duration of action of stationary object
If the biological half-life of a therapeutic agent is extended, then the frequency of administration is reduced, but the complexity of the agent increases
Solution Approach 1:
The patent creates a composite therapeutic agent by chemically conjugating a peptide with a half-life extending moiety. This composite structure combines the biological activity of the peptide with the pharmacokinetic benefits of the modifying moiety, achieving extended half-life while managing the complexity through established conjugation chemistry and modular design
Data Source
AI summary
Peptide conjugates comprising a peptide selected from a peptide that modulates the PYY receptor, a peptide that modulates both the GLP-1 receptor and the GCG receptor, a peptide that modulates both the GLP-1 receptor and the GIP receptor, and a peptide that modulates the GLP-1 receptor; and a staple attached to the peptide at a first amino acid and a second amino acid are disclosed herein. Also provided are peptide conjugates comprising prolactin-releasing peptide. The peptide conjugates may be used for treating conditions such as obesity. Further provided are stapled prolactin-releasing peptide.