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

VSEngineering 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

Engineering Contradiction:
ImproveefficacyVSAvoidside effects
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

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.

Inventive Principle:
Principle #5Merging (Combining)

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

Engineering Contradiction:
Improveglycemic controlVSAvoidweight loss
Core Design Contradiction:
ReliabilityVSQuantity of substance

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.

Inventive Principle:
Principle #5Merging (Combining)

3Productivity

If higher doses of MC4r agonist are administered to improve weight loss efficacy, then weight loss increases, but side effects worsen

Engineering Contradiction:
Improveweight loss efficacyVSAvoidside effects
Core Design Contradiction:
ProductivityVSObject-affected harmful factors

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.

Inventive Principle:
Principle #5Merging (Combining)

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.

Inventive Principle:
Principle #35Parameter changes

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

Engineering Contradiction:
Improvetherapeutic effectVSAvoidtreatment complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

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.

Inventive Principle:
Principle #5Merging (Combining)

Data Source

PatentUS10660939B2Therapies for obesity, diabetes and related indications
Publication Date: 2020.05.26 PALATIN TECHNOLOGIES INC
  • US10660939B2 patent drawing
  • US10660939B2 patent drawing
  • US10660939B2 patent drawing

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.