MC4r and GLP-1 Agonist Combination for Weight Loss
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Solution Overview
Problem
Current treatments for obesity and diabetes, particularly those targeting melanocortin receptor 4 (MC4r) and glucagon-like peptide-1 (GLP-1) receptors, have limitations in efficacy and side effects when used as monotherapies for obesity and metabolic syndrome.
Innovation Solution
A pharmaceutical composition combining a MC4r agonist and a GLP-1 receptor agonist, such as Peptide No. 154 with liraglutide or exenatide, administered subcutaneously, to induce synergistic anti-obesity and glycemic control effects without significant weight gain.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If a MC4r agonist is used as monotherapy for obesity treatment, then weight loss effect is achieved, but side effects increase and efficacy is limited
Solution Approach 1:
The patent combines a MC4r agonist and a GLP-1 receptor agonist into a single pharmaceutical composition for combination therapy. This merging of two different therapeutic agents allows the treatment to achieve synergistic weight loss effects while each component can be optimized to reduce their individual side effect profiles, thereby improving overall reliability and reducing harmful factors.
2Reliability
If a GLP-1 receptor agonist is used as monotherapy for diabetes treatment, then glycemic control is achieved, but weight loss effect is insufficient
Solution Approach 1:
The pharmaceutical composition merges a GLP-1 receptor agonist (for glycemic control) with a MC4r agonist (for weight loss) into a single formulation. This combination allows the treatment to simultaneously achieve both glycemic control and significant weight loss, overcoming the limitation of GLP-1 receptor agonist monotherapy where glycemic control is achieved but weight loss is insufficient.
3Productivity
If higher doses of MC4r agonist are administered to improve weight loss efficacy, then weight loss increases, but side effects worsen
Solution Approach 1:
The patent combines a MC4r agonist with a GLP-1 receptor agonist in a fixed-ratio formulation, allowing the MC4r agonist to be administered at optimized doses that achieve effective weight loss when combined with the GLP-1 receptor agonist, rather than requiring higher doses that would cause excessive side effects. The synergistic interaction between the two agents enables effective weight loss at tolerable dose levels.
Solution Approach 2:
The invention changes the dosing parameters by establishing specific dose ranges for the MC4r agonist (0.01-10 mg/day) when used in combination with a GLP-1 receptor agonist. This parameter optimization allows the treatment to achieve effective weight loss while maintaining side effects at acceptable levels, unlike higher doses used in monotherapy.
4Reliability
If combination therapy with MC4r agonist and GLP-1 receptor agonist is used, then synergistic weight loss and glycemic control are achieved, but treatment complexity increases
Solution Approach 1:
The patent merges two separate therapeutic agents (MC4r agonist and GLP-1 receptor agonist) into a single pharmaceutical composition that can be administered as one treatment. This merging approach achieves synergistic therapeutic effects for both weight loss and glycemic control while simplifying the treatment regimen compared to administering two separate medications, thereby reducing treatment complexity.
Data Source
AI summary
The invention relates to methods, uses, compositions and formulations including a melanocortin receptor-4 agonist and a glucagon-like peptide-1 receptor agonist for treatment of obesity, diabetes, metabolic syndrome and related indications, diseases or disorders.


