18-MC Negative Allosteric Modulation for Substance Use Disorders

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Solution Overview

Problem

Current pharmacotherapies for substance use disorders (SUDs) are limited, with only modest efficacy for nicotine and opiate use disorders, and there are no approved therapies for cocaine disorders, necessitating a safe, effective, orally-available, and low-cost approach.

Innovation Solution

Administration of 18-Methoxycoronaridine salt (18-MC) in a pharmaceutical carrier to treat substance use disorders by preventing addictive behavior and craving, utilizing its mechanism as a specific negative allosteric modulator of α3β4 nicotinic cholinergic receptors to reduce drug self-administration and attenuate cue-induced relapse.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current pharmacotherapies are used for substance use disorders, then treatment is available, but efficacy is only modest and limited to nicotine and opiate use disorders

Engineering Contradiction:
Improvetreatment efficacyVSAvoidapplicability to different substance use disorders
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent applies universality by developing a single pharmacotherapeutic approach using 18-MC that can treat multiple substance use disorders including cocaine, nicotine, and opiate disorders. The compound targets the α3β4 nicotinic cholinergic receptor subtype which is involved in the reinforcing effects of multiple drugs of abuse, making the treatment versatile across different addiction types rather than substance-specific

Inventive Principle:
Principle #6Universality (Multi-functionality)

2Reliability

If new pharmacotherapies are developed for substance use disorders, then treatment efficacy may improve, but safety concerns and side effects may increase

Engineering Contradiction:
Improvetreatment efficacyVSAvoidside effects and safety concerns
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies local quality by targeting a specific receptor subtype (α3β4 nicotinic cholinergic receptor) rather than using broad-spectrum medications. This selective targeting allows the drug to act on specific neural pathways involved in addiction while minimizing off-target effects. The selective α3β4 antagonism provides therapeutic benefit with a more favorable side effect profile compared to non-selective medications

Inventive Principle:
Principle #3Local quality

3Reliability

If effective pharmacotherapies are developed, then substance use disorders can be treated, but current options are limited and costly

Engineering Contradiction:
Improvetreatment effectivenessVSAvoidcost and availability
Core Design Contradiction:
ReliabilityVSEase of manufacture

Solution Approach 1:

The patent applies this principle by developing 18-MC as an orally available small molecule compound that can be manufactured through established pharmaceutical processes. The compound's oral availability eliminates the need for expensive and complex injection infrastructure, making treatment more accessible and cost-effective for widespread use in treating substance use disorders

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

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

18-MC effectively reduces drug self-administration and craving in animal models and has shown potential in human studies, offering a novel approach for treating substance use disorders, including cocaine abuse, with a favorable safety profile.

Implementation Method 1

utilizing its mechanism as a specific negative allosteric modulator of α3β4 nicotinic cholinergic receptors to reduce drug self-administration and attenuate cue-induced relapse

Methodology Applied
Scientific EffectNegative allosteric modulation:

Data Source

PatentUS11596638B218-MC for treatment of substance use disorders
Publication Date: 2023.03.07 DEFINIUM THERAPEUTICS US INC
  • US11596638B2 patent drawing
  • US11596638B2 patent drawing
  • US11596638B2 patent drawing

AI summary

A composition for treating substance use disorders of an effective amount of 18-Methoxycoronaridine salt (18-MC) in a pharmaceutical carrier. A method of treating substance use disorders, by administering an effective amount of 18-Methoxycoronaridine salt (18-MC) in a pharmaceutical carrier to an individual and preventing substance abuse in the individual. A method of preventing addictive behavior in an individual. A method of preventing craving in an individual. A composition of a metabolite of 18-MC salt. A method of treating substance use disorders by administering an effective amount of a metabolite of 18-MC salt in a pharmaceutical carrier to an individual and preventing substance abuse in the individual. A composition having various pharmacokinetic profiles as shown in the Figures.