Sequential GLP-1 Agonist and DPP-4 Inhibitor Therapy for Weight Maintenance

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Solution Overview

Problem

Current treatments for type 2 diabetes and obesity often fail to achieve long-term glycemic control, are associated with weight gain, and have limitations in efficacy and tolerability, particularly in obese or overweight patients, who also face challenges in maintaining weight loss and preventing rebound weight gain after treatment cessation.

Innovation Solution

The sequential or combined use of a GLP-1 receptor agonist followed by a DPP-4 inhibitor, such as linagliptin, to induce weight loss and maintain reduced body weight, or to prevent weight gain, offering a therapeutic approach that addresses the limitations of existing treatments by improving glycemic control and reducing body fat.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current treatments for type 2 diabetes and obesity are used, then glycemic control is achieved, but weight gain occurs and long-term control is difficult to maintain

Engineering Contradiction:
Improvelong-term glycemic controlVSAvoidbody weight
Core Design Contradiction:
ReliabilityVSWeight of moving object

Solution Approach 1:

The patent combines two different therapeutic agents (GLP-1 receptor agonist and DPP-4 inhibitor) into a sequential treatment regimen. The GLP-1 receptor agonist is administered first to induce weight loss and improve glycemic control, followed by a DPP-4 inhibitor to maintain the achieved weight loss and sustain glycemic control, thereby resolving the contradiction between achieving glycemic control and avoiding weight gain

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The treatment protocol employs preliminary action by first administering the GLP-1 receptor agonist to achieve initial weight loss and glycemic improvement before transitioning to the DPP-4 inhibitor. This preliminary phase creates a favorable baseline that enables long-term maintenance of both weight control and glycemic stability

Inventive Principle:
Principle #10Preliminary action

2Weight of moving object

If weight loss treatment is administered to obese patients, then body weight is reduced, but rebound weight gain occurs after treatment cessation

Engineering Contradiction:
Improvebody weightVSAvoidduration of weight loss maintenance
Core Design Contradiction:
Weight of moving objectVSDuration of action of stationary object

Solution Approach 1:

The patent ensures continuity of useful action by transitioning from the GLP-1 receptor agonist to the DPP-4 inhibitor without treatment interruption. The DPP-4 inhibitor continues the weight management benefit after the initial weight loss phase, preventing rebound weight gain and extending the duration of weight loss maintenance

Inventive Principle:
Principle #20Continuity of useful action

Solution Approach 2:

The treatment protocol changes therapeutic parameters by switching from a GLP-1 receptor agonist to a DPP-4 inhibitor. This parameter change allows the body to adapt to a new therapeutic mechanism that sustains weight loss effects and prevents rebound, thereby extending the duration of beneficial action

Inventive Principle:
Principle #35Parameter changes

3Reliability

If existing diabetes and obesity treatments are used, then some therapeutic effect is achieved, but tolerability and safety are compromised

Engineering Contradiction:
Improvetherapeutic efficacyVSAvoidside effects and tolerability
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent employs a sequential treatment approach where the GLP-1 receptor agonist is used for a limited initial period to achieve weight loss, then discontinued in favor of the DPP-4 inhibitor for long-term maintenance. This disposable use of the GLP-1 agonist minimizes exposure to its side effects while still achieving therapeutic benefits, thereby improving overall tolerability

Inventive Principle:
Principle #27Cheap short-living objects (Disposable)

Data Source

PatentEP2566469B1Combination therapy
Publication Date: 2022.12.21 BOEHRINGER INGELHEIM INT GMBH
  • EP2566469B1 patent drawingFigure 1
  • EP2566469B1 patent drawingFigure 2~3
  • EP2566469B1 patent drawingFigure 4

AI summary

The present invention relates to methods for treating and/or preventing metabolic diseases comprising the combined administration of a GLP-1 receptor agonist and a DPP-4 inhibitor.