D1/D5 Receptor Antagonists for Stuttering Treatment

Resolve Bottlenecks,
Find Innovative Solutions
Generate Solutions

Solution Overview

Problem

Current treatments for stuttering lack effective pharmacological solutions, with known D2 antagonists often inducing stuttering and D2-preferring dopamine agonists providing variable efficacy and severe side effects, while behavioral techniques and anxiety medications offer limited relief.

Innovation Solution

Administration of therapeutically effective amounts of D1/D5 receptor antagonists or partial agonists, such as ecopipam, to inhibit dopamine access and treat stuttering symptoms, which can be combined with behavioral or surgical therapies.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If D2 antagonists are used to treat stuttering, then stuttering symptoms may be reduced, but stuttering can be induced or worsened

Engineering Contradiction:
Improveeffectiveness in treating stutteringVSAvoidinduction of stuttering
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

Instead of blocking D2 receptors (which causes stuttering), the patent applies D1/D5 receptor antagonism, effectively inverting the approach to dopamine receptor blockade and achieving therapeutic effect without inducing stuttering

Inventive Principle:
Principle #13The other way round (Inversion)

Solution Approach 2:

The patent changes the target parameter from D2 receptor affinity to D1/D5 receptor affinity, shifting the mechanism of action to achieve both treatment effectiveness and avoidance of harmful stuttering induction

Inventive Principle:
Principle #35Parameter changes

2Reliability

If D2-preferring dopamine agonists are used to treat stuttering, then stuttering symptoms may be relieved, but severe side effects occur

Engineering Contradiction:
Improverelief of stuttering symptomsVSAvoidsevere side effects
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent changes the receptor target from D2-preferring agonists to D1/D5-selective antagonists, fundamentally altering the pharmacological parameter to achieve symptom relief with improved safety profile

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent employs selectively D1/D5 receptor-targeting compounds that provide targeted, temporary action at the specific receptor subtype, avoiding the broad and prolonged side effects of non-selective D2 agonists

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

3Reliability

If behavioral techniques are used to treat stuttering, then some improvement is achieved, but limited relief is provided

Engineering Contradiction:
Improveimprovement in stutteringVSAvoidlevel of relief
Core Design Contradiction:
ReliabilityVSProductivity

Solution Approach 1:

The patent replaces behavioral therapy mechanisms with a pharmacological mechanism targeting dopamine receptors, providing a different mode of action that achieves more significant symptom relief for severely afflicted patients

Inventive Principle:
Principle #28Mechanics substitution (Replace mechanical system)

4Reliability

If anxiety medications are used to treat stuttering, then stress-related stuttering may be reduced, but limited and non-specific relief is provided

Engineering Contradiction:
Improvereduction of stress-related stutteringVSAvoidspecificity for stuttering treatment
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent changes the mechanism from general anxiety reduction to specific D1/D5 receptor blockade, providing targeted treatment for stuttering with a more precise pharmacological action that addresses the core pathophysiology

Inventive Principle:
Principle #35Parameter changes

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 use of D1/D5 receptor antagonists or partial agonists provides significant relief from stuttering symptoms, reducing frequency and severity, and can be used across various age groups and types of stuttering disorders without severe toxicity.

Implementation Method 1

compounds that selectively bind the D1/D5 receptor and subsequently inhibit dopamine access to the D1/D5 receptor

Methodology Applied
Scientific EffectReceptor binding:

Data Source

PatentEP3057595B1Fused benzazepines for treatment of stuttering
Publication Date: 2020.04.29 EMALEX BIOSCIENCES INC
  • EP3057595B1 patent drawing
  • EP3057595B1 patent drawing
  • EP3057595B1 patent drawing

AI summary

The present invention encompasses methods of treating a subject who stutters. The methods can include the steps of: (a) identifying a subject in need of treatment; and (b) administering to the subject a therapeutically effective amount of a composition comprising a D1/D5 receptor antagonist, a D1/D5 receptor partial agonist, or a mixture thereof. For example, the D1/D5 receptor antagonist can be ecopipam or a pharmaceutically acceptable salt, solvate, hydrate, prodrug, structural analog, metabolite, or polymorph thereof.