Combination TRPM8 and nAChR Agonists for Weight Loss

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Solution Overview

Problem

Current therapeutic strategies for obesity and related disorders, such as those involving orlistat and sibutramine, are inadequate due to insufficient efficacy and severe side effects, necessitating the development of alternative treatments that can effectively manage weight loss without undesirable side effects.

Innovation Solution

A combination of a TRPM8-agonist and a nicotinic acetylcholine receptor (nAChR)-agonist is administered to promote significant weight loss, improve glucose metabolism, and inhibit weight gain, while minimizing side effects like nausea and steatorrhea.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Weight of moving object

If monotherapy with orlistat or sibutramine is used, then weight loss is achieved, but severe side effects occur

Engineering Contradiction:
Improveweight lossVSAvoidside effects
Core Design Contradiction:
Weight of moving objectVSObject-affected harmful factors

Solution Approach 1:

The patent combines two different active compounds (a TRPM8-agonist and an nAChR-agonist) into a single pharmaceutical composition. This combination approach allows the synergistic effect of both compounds to work together, achieving weight loss while distributing the side effect profile across multiple mechanisms, thereby reducing the severity of individual side effects compared to monotherapy with either compound alone.

Inventive Principle:
Principle #5Merging (Combining)

2Weight of moving object

If combination therapy with TRPM8-agonist and nAChR-agonist is used, then synergistic weight loss is achieved, but treatment complexity increases

Engineering Contradiction:
Improveweight lossVSAvoidtreatment complexity
Core Design Contradiction:
Weight of moving objectVSDevice complexity

Solution Approach 1:

The patent merges two active compounds into a single pharmaceutical composition that can be administered as one treatment regimen. This consolidation simplifies the treatment protocol compared to administering two separate medications, while still capturing the synergistic benefits of combining a TRPM8-agonist and an nAChR-agonist for weight loss.

Inventive Principle:
Principle #5Merging (Combining)

Data Source

PatentUS10568852B2Combination compositions and their use in methods for treating obesity and obesity-related disorders
Publication Date: 2020.02.25 HELMHOLTZ ZENT MUENCHEN DEUT FORSCHUNGSZENTRUM FUER GESUNDHEIT & UMWELT (GMBH)
  • US10568852B2 patent drawing
  • US10568852B2 patent drawing
  • US10568852B2 patent drawing

AI summary

The present invention relates to compositions comprising at least two different active compounds and the use of such combination compositions in medicine, in particular in methods for treating obesity and obesity-related disorders and/or in methods for inhibiting weight gain.