Modified GLP-1 Peptide Composition for Glucose and Lipid Control

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Solution Overview

Problem

Existing GLP-1 drugs for treating metabolic diseases like diabetes and obesity have slow weight-loss effects, severe gastrointestinal side effects, and require higher doses for obesity treatment, leading to patient non-compliance and rebound weight gain, while statins and fibrates have side effects and increase diabetes risk.

Innovation Solution

Development of peptide compounds with specific sequences and modifications, such as Y-aib-E-G-T-F-X11-S-D-X1-S-X12-X2-L-X3-X4-E-A-X5-X6-X7-X8-W-L-X9-A-G-X10, which can lower blood glucose, reduce triglycerides and total cholesterol, and decrease body fat, suitable for diabetic and pre-diabetic patients.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If GLP-1 receptor agonists are used to control blood glucose and promote weight loss, then blood glucose levels improve and insulin sensitivity increases, but gastrointestinal side effects occur and weight loss effect is slow

Engineering Contradiction:

Improveblood glucose controlVSAvoidgastrointestinal side effects

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent modifies the chemical structure of GLP-1 receptor agonists by changing amino acid residues and adding fatty acid amide groups at the C-terminus, thereby altering the pharmacokinetic parameters including half-life and receptor binding affinity, which resolves the contradiction between efficacy and side effects

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent creates composite peptide structures by combining GLP-1 receptor agonist sequences with fatty acid amide moieties (such as octanoic acid, decanoic acid, or dodecanoic acid), forming a hybrid molecule that simultaneously achieves rapid glucose control and reduced gastrointestinal toxicity

Inventive Principle:

Principle #40Composite materials

2Weight of moving object

If higher doses of GLP-1 drugs are used for obesity treatment, then weight loss effect is enhanced, but gastrointestinal side effects become more severe

Engineering Contradiction:

Improvebody weight reductionVSAvoidgastrointestinal side effects

Core Design Contradiction:

Weight of moving objectVSObject-affected harmful factors

Solution Approach 1:

The patent optimizes the lipid tail chain length and composition of the GLP-1 derivative, where specific chain lengths (C8-C12) provide enhanced weight loss efficacy at lower doses while minimizing gastrointestinal irritation, thus resolving the dose-dependent contradiction

Inventive Principle:

Principle #35Parameter changes

3Quantity of substance

If statin and fibrate drugs are used to control blood lipids, then lipid levels are reduced, but side effects occur and patient intolerance increases

Engineering Contradiction:

Improveblood lipid reductionVSAvoidside effects and intolerance

Core Design Contradiction:

Quantity of substanceVSObject-affected harmful factors

Solution Approach 1:

The patent designs a multi-functional peptide compound that simultaneously acts as a GLP-1 receptor agonist for glucose control and a lipid-lowering agent, replacing the need for separate statin or fibrate medications, thereby reducing cumulative side effects and improving patient tolerance

Inventive Principle:

Principle #6Universality (Multi-functionality)

Data Source

PatentUS12612441B2Polypeptide and therapeutic uses thereof

Publication Date: 2026.04.28 VITALIXIR BEIJING CO LTD

AI summary

The present application provides a peptide compound of formula (VII) and its use in medical treatment.