Opioid Modulators for Antipsychotic-Induced Weight Gain

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Solution Overview

Problem

Atypical antipsychotic medications cause significant weight gain in patients, leading to obesity and related health issues, with existing treatments failing to effectively address this side effect.

Innovation Solution

Administration of compounds of Formula I, which act as opioid receptor modulators, to reduce pharmacologically induced weight gain by lowering ghrelin levels and suppressing food intake, thereby mitigating weight gain associated with atypical antipsychotic use.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If atypical antipsychotic medications are administered to treat psychotic disorders, then treatment effectiveness and relapse prevention are improved, but weight gain and obesity risk increase significantly

Engineering Contradiction:
Improvetreatment effectivenessVSAvoidpatient weight
Core Design Contradiction:
ReliabilityVSWeight of moving object

Solution Approach 1:

The patent introduces ghrelin as an intermediary substance that mediates the weight gain effect. Atypical antipsychotics increase ghrelin levels, which in turn stimulates appetite and weight gain. By targeting ghrelin with specific compounds (Formula I), the patent interrupts this mediating pathway to reduce weight gain while maintaining antipsychotic treatment effectiveness.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent changes the ghrelin parameter (circulating ghrelin levels) by administering compounds that lower ghrelin concentrations. This parameter change directly addresses the weight gain issue while allowing the antipsychotic treatment to continue effectively, as the ghrelin-lowering compounds do not interfere with antipsychotic efficacy.

Inventive Principle:
Principle #35Parameter changes

2Ease of operation

If atypical antipsychotic medications are administered to improve tolerability and adherence, then patient compliance is improved, but metabolic changes and obesity risk increase

Engineering Contradiction:
Improvepatient adherenceVSAvoidmetabolic changes
Core Design Contradiction:
Ease of operationVSObject-affected harmful factors

Solution Approach 1:

Ghrelin serves as the intermediary that transmits the harmful metabolic effects. The patent targets this intermediary by lowering ghrelin levels through specific compounds, thereby preventing metabolic changes and obesity while preserving the improved tolerability and adherence benefits of atypical antipsychotics.

Inventive Principle:
Principle #24Intermediary (Mediator)

3Weight of moving object

If conventional weight loss treatments are used to address antipsychotic-induced weight gain, then weight reduction is achieved, but treatment complexity and side effects increase

Engineering Contradiction:
Improvepatient weightVSAvoidtreatment complexity
Core Design Contradiction:
Weight of moving objectVSDevice complexity

Solution Approach 1:

The patent extracts the weight gain mechanism from the complex interaction between antipsychotics and metabolism by isolating ghrelin as the key driver. By targeting ghrelin specifically with compounds of Formula I, the treatment simplifies the approach to weight management, avoiding the complexity of conventional multi-component weight loss therapies while achieving effective weight control.

Inventive Principle:
Principle #2Taking out (Extraction)

Applied Scientific Principles

This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.

Function Achieved in This Case

The compounds effectively prevent or reduce weight gain in patients treated with atypical antipsychotics, maintaining a healthy body mass index and reducing body fat percentage, while also addressing metabolic changes associated with these medications.

Implementation Method 1

administration of compounds of Formula I, which act as opioid receptor modulators, to reduce pharmacologically induced weight gain by lowering ghrelin levels and suppressing food intake

Methodology Applied
Scientific EffectOpioid receptor modulation:

Data Source

PatentUS12194035B2Methods for treating antipsychotic-induced weight gain
Publication Date: 2025.01.14 ALKERMES PHARMA IRELAND LTD
  • US12194035B2 patent drawing
  • US12194035B2 patent drawing
  • US12194035B2 patent drawing

AI summary

The present invention relates to the discovery of a novel opioid modulator effective in reducing pharmacologically induced weight gain associated with atypical antipsychotic use. The present invention provides methods of reducing antipsychotic induced weight gain, methods for suppressing food intake and reducing ghrelin levels induced by atypical antipsychotic medications in a patient.