GLP-1 Fusion Peptide Coupled Cyclic PYY Conjugates for Extended Half-Life

Solution Overview

Problem

Current GLP-1 and PYY3-36 therapeutic agents have short circulating half-lives due to rapid metabolism, limiting their therapeutic potential for modulating GLP-1 and Y2 receptors for conditions like obesity and diabetes.

Innovation Solution

Development of GLP-1 fusion peptide coupled cyclic PYY conjugates with specific linker peptides and a hinge-Fc region, enhancing metabolic stability and pharmacokinetic profile, allowing for prolonged receptor modulation.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Duration of action of moving object

If GLP-1 and PYY3-36 are used as therapeutic agents, then receptor modulation activity is achieved, but circulating half-life is short due to rapid metabolism

Engineering Contradiction:

Improvecirculating half-lifeVSAvoidmetabolic stability

Core Design Contradiction:

Duration of action of moving objectVSReliability

Solution Approach 1:

The patent merges GLP-1 fusion peptide with cyclic PYY conjugate into a single molecular entity, combining the receptor modulating activities of both peptides while achieving extended half-life through the conjugate structure. The fusion peptide contains both GLP-1 and PYY sequences integrated into one molecule that circulates longer in the body.

Inventive Principle:

Principle #5Merging (Combining)

Solution Approach 2:

The conjugate acts as a composite peptide molecule combining different functional domains (GLP-1 fusion peptide and cyclic PYY) to achieve properties that neither component alone possesses, specifically extended circulating half-life while maintaining receptor modulation activity.

Inventive Principle:

Principle #40Composite materials

2Productivity

If GLP-1 and PYY3-36 are used as therapeutic agents, then receptor modulation activity is achieved, but therapeutic potential is limited due to short circulating half-life

Engineering Contradiction:

Improvetherapeutic potentialVSAvoidcirculating half-life

Core Design Contradiction:

ProductivityVSDuration of action of moving object

Solution Approach 1:

The patent merges GLP-1 fusion peptide with cyclic PYY conjugate into a single molecular entity, combining the receptor modulating activities of both peptides while achieving extended half-life through the conjugate structure. The fusion peptide contains both GLP-1 and PYY sequences integrated into one molecule that circulates longer in the body.

Inventive Principle:

Principle #5Merging (Combining)

Data Source

PatentUS20240117000A1Glucagon like peptide 1 (GLP-1) fusion peptide coupled cyclic peptide tyrosine tyrosine conjugates and uses thereof

Publication Date: 2024.04.11 JANSSEN SCI IRELAND UC

AI summary

The present invention comprises conjugates comprising a glucagon-like peptide 1 (GLP-1) fusion peptide coupled to a cyclic PYY peptide. The invention also relates to pharmaceutical compositions and methods for use thereof. The novel conjugates are useful for preventing, treating or ameliorating diseases and disorders disclosed herein.