CCK2 Receptor Antagonists for Depression and Nerve Pain

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Solution Overview

Problem

Current antidepressant drugs, such as SSRIs, have significant side effects and fail to effectively treat major and minor forms of depression and chronic pain associated with nerve injury, necessitating a novel approach.

Innovation Solution

Administration of cholecystokinin-2 (CCK2) receptor antagonists, specifically compounds like YM022 and YF476, which selectively inhibit CCK2 receptors, providing a long-acting treatment for depression and pain by reducing symptoms and improving quality of life.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If SSRIs are used to treat depression, then depression symptoms are reduced, but side effects such as nausea, tremors, nervousness, insomnia and sexual problems occur

Engineering Contradiction:

Improveeffectiveness in treating depressionVSAvoidside effects

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent changes the therapeutic parameter from serotonin reuptake inhibition to CCK2 receptor antagonism. By targeting a different receptor system (CCK2 rather than serotonin transporters), the mechanism of action is fundamentally altered, which resolves the contradiction by achieving antidepressant efficacy through a different physiological pathway that does not produce the harmful side effects associated with SSRIs

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent introduces CCK2 receptor antagonists as an intermediary substance between the patient and the depression condition. Instead of directly modifying serotonin reuptake, the CCK2 antagonist acts as a mediator that blocks CCK2 receptors, thereby indirectly achieving antidepressant effects through modulation of the CCK-CCK2 receptor pathway, which is distinct from the SSRI mechanism

Inventive Principle:

Principle #24Intermediary (Mediator)

2Reliability

If daily antidepressant regimens are used, then depression is treated, but treatment burden and cost increase

Engineering Contradiction:

Improvetreatment effectivenessVSAvoidtreatment duration and frequency

Core Design Contradiction:

ReliabilityVSLoss of time

Solution Approach 1:

The patent transitions from continuous daily administration to periodic subcutaneous injection. The long-acting formulation allows for administration at extended intervals (e.g., weekly or monthly), transforming the treatment pattern from continuous to periodic, which reduces the time commitment and burden on the patient while maintaining therapeutic effectiveness

Inventive Principle:

Principle #19Periodic action

Solution Approach 2:

The patent introduces a long-acting formulation that dynamically extends the duration of action. By using a formulation with prolonged half-life and sustained release characteristics, the treatment effect is extended over weeks, allowing for reduced frequency of administration while maintaining consistent therapeutic levels in the body

Inventive Principle:

Principle #15Dynamics

3Reliability

If conventional antidepressants are used, then depression is treated, but they do not effectively alleviate chronic pain associated with nerve injury

Engineering Contradiction:

Improvedepression treatment efficacyVSAvoidpain relief capability

Core Design Contradiction:

ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent identifies CCK2 receptor antagonism as a universal mechanism that addresses multiple conditions simultaneously. The same pharmacological action (CCK2 blockade) provides both antidepressant effects and analgesic effects, making the treatment approach versatile enough to handle both depression and chronic pain associated with nerve injury without requiring separate treatments

Inventive Principle:

Principle #6Universality (Multi-functionality)

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

CCK2 receptor antagonists effectively treat depression and chronic pain with prolonged half-life, offering stable relief from depressive disorders and analgesic effects, potentially replacing daily antidepressant regimens with a single subcutaneous administration for up to 8 weeks.

Implementation Method 1

cholecystokinin-2 (CCK2) receptor antagonist are useful in treating mental disorder and pain associated with nerve injury

Methodology Applied

Scientific EffectReceptor antagonism:

Data Source

PatentUS11285161B2Method and composition for treating mental disorder and pain associated with nerve damage

Publication Date: 2022.03.29 CITY UNIVERSITY OF HONG KONG

AI summary

A method of treating a subject suffering from mental disorder including the step of administering an effective amount of a cholecystokinin-2 receptor antagonist or a pharmaceutical acceptable salt thereof to the subject. A method of treating a subject suffering from pain associated with nerve injury including the step of administering an effective amount of a cholecystokinin-2 receptor antagonist or a pharmaceutical acceptable salt thereof to the subject. A pharmaceutical composition including the cholecystokinin-2 receptor antagonist or a pharmaceutical acceptable salt thereof as active ingredient, one or more antidepressant compounds, and a pharmaceutically acceptable excipient.