Methocinnamox Opioid Receptor Antagonist for Prolonged Overdose Protection

Solution Overview

Problem

Current treatments for opioid abuse and overdose, such as naltrexone and naloxone, have limitations including short duration of action and potential for adverse interactions, and fail to effectively counteract long-acting opioids or potent agonists, necessitating repeated administration and increased risk of overdose.

Innovation Solution

Methocinnamox (MCAM), a pseudo-irreversible and selective opioid receptor antagonist, binds functionally to μ-opioid receptors, providing long-lasting blockade of opioid agonist effects and protection against respiratory depression, with a single administration capable of reversing and preventing opioid-induced toxicity and overdose.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Duration of action of moving object

If current treatments like naltrexone and naloxone are used, then opioid overdose can be treated, but the duration of action is short requiring repeated administration

Engineering Contradiction:

Core Design Contradiction:

Duration of action of moving objectVSLoss of time

Solution Approach 1:

The patent modifies the chemical structure of known opioid antagonists by introducing a methoxy group and a phenylpiperazine moiety to create MCAM. This structural parameter change results in pseudo-irreversible binding to μ-opioid receptors, dramatically extending the duration of action from hours to days, thereby eliminating the need for repeated administrations.

Inventive Principle:

Principle #35Parameter changes

2Reliability

If current treatments are used, then opioid effects are blocked, but adverse interactions with other drugs may occur

Engineering Contradiction:

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

MCAM exhibits selective affinity primarily for μ-opioid receptors with minimal interaction at other receptor types. This localized specificity ensures reliable blockade of opioid effects while avoiding adverse interactions with non-opioid medications, thereby improving the safety profile compared to less selective antagonists.

Inventive Principle:

Principle #3Local quality

3Duration of action of moving object

If long-acting opioids are used, then prolonged pain relief is achieved, but the risk of overdose and respiratory depression increases

Engineering Contradiction:

Core Design Contradiction:

Duration of action of moving objectVSObject-affected harmful factors

Solution Approach 1:

MCAM can be administered as a preventive measure before exposure to long-acting opioids or in settings where opioid overdose risk is concerns (e.g., harm reduction programs). The pseudo-irreversible blockade is established in advance, providing prolonged protection against respiratory depression and overdose without requiring continuous monitoring or repeated dosing.

Inventive Principle:

Principle #9Preliminary anti-action

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

MCAM offers prolonged protection against opioid-induced respiratory depression and abuse, avoiding adverse interactions with non-opioid drugs, and reducing the need for repeated dosing, making it a safer and more effective treatment for opioid abuse and overdose.

Implementation Method 1

Methocinnamox (MCAM), a pseudo-irreversible and selective opioid receptor antagonist, binds functionally to μ-opioid receptors

Methodology Applied

Scientific EffectPseudo-irreversible binding:

Data Source

PatentUS11123334B2Compositions and methods for treating opioid overdose and opioid abuse

Publication Date: 2021.09.21

AI summary

The disclosure relates to compositions and methods of preventing or treating a subject suffering from opioid toxicity or overdose. The method comprises administering to a patient in need of treatment an effective amount of methocinnamox.