LMTX Compounds Enhance Oxygen Saturation via Hemoglobin Binding

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Solution Overview

Problem

Current methods fail to effectively enhance oxygen carrying capacity of blood to alleviate hypoxemia, a condition characterized by low oxygen levels in tissues, which can lead to tissue damage and morbidity.

Innovation Solution

The use of hydromethylthionine salts, specifically LMTX compounds, which are administered orally to enhance oxygen saturation by facilitating the binding of oxygen to haemoglobin, thereby increasing oxygen delivery to tissues, even at lower doses compared to traditional methylthionium chloride.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Quantity of substance

If traditional methylthionium chloride (MTC) is used to enhance oxygen carrying capacity, then oxygen saturation improves, but the drug requires high doses and has poor oral absorption and red cell penetration

Engineering Contradiction:
Improveoxygen saturationVSAvoidoral absorption and red cell penetration
Core Design Contradiction:
Quantity of substanceVSEase of operation

Solution Approach 1:

The patent modifies the chemical structure of methylthionium chloride by changing the counterion from chloride to hydromethanesulfonate, creating LMTX compounds. This parameter change in chemical structure improves oral absorption, red cell penetration, and deep compartment distribution while maintaining the ability to enhance oxygen saturation at lower doses

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent creates a new compound class (LMTX) that copies the active MT moiety of MTC but with improved pharmacokinetic properties through different counterions and structural modifications, achieving better absorption and distribution without sacrificing the therapeutic effect

Inventive Principle:
Principle #26Copying

2Quantity of substance

If high doses of MTC are used to achieve therapeutic effect, then oxygen carrying capacity increases, but tolerance decreases due to side effects

Engineering Contradiction:
Improveoxygen carrying capacityVSAvoidtolerance and side effects
Core Design Contradiction:
Quantity of substanceVSObject-affected harmful factors

Solution Approach 1:

The patent changes the dosing parameter by demonstrating that LMTX compounds achieve the same oxygen saturation enhancement at substantially lower doses than MTC, thereby improving tolerance and reducing side effects while maintaining therapeutic efficacy

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The LMTX compound acts as an intermediary that bridges the gap between the active MT moiety and the body's oxygen transport system, achieving effective oxygen saturation enhancement with reduced dose and improved safety profile

Inventive Principle:
Principle #24Intermediary (Mediator)

3Quantity of substance

If methylene blue-vitamin C-N-acetyl Cysteine (MCN) is used to reduce methaemoglobin, then oxygen saturation improves, but the mechanism is complex and requires multiple components

Engineering Contradiction:
Improveoxygen saturationVSAvoidnumber of components
Core Design Contradiction:
Quantity of substanceVSDevice complexity

Solution Approach 1:

The patent extracts and isolates the active MT moiety function from the complex MCN combination, creating LMTX compounds that achieve oxygen saturation enhancement through a simpler, single-agent mechanism that does not require vitamin C or N-acetyl Cysteine

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The patent segments the complex MCN therapeutic mechanism into a distinct LMTX-based approach, separating the oxygen saturation enhancement function from the methaemoglobin reduction function, and achieving oxygen saturation improvement through a more straightforward mechanism

Inventive Principle:
Principle #1Segmentation

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

LMTX compounds significantly increase oxygen saturation in the blood within 4 hours, providing therapeutic benefits for hypoxemia and related conditions without significant side effects, such as methaemoglobin elevation, and can be used to treat various diseases associated with low oxygen levels.

Implementation Method 1

the binding of the LMT moiety to haemoglobin overcomes the initial energy barrier for oxygen binding

Methodology Applied
Scientific EffectChemical binding: Chemical Bonding

Data Source

PatentEP4146225B1Methylthioninium compounds for use in the treatment of hypoxemia
Publication Date: 2024.10.09 WISTA LAB LTD
  • EP4146225B1 patent drawingFigure 1
  • EP4146225B1 patent drawingFigure 2
  • EP4146225B1 patent drawingFigure 3

AI summary

The present invention provides methods of alleviating hypoxemia in a subject through oral administration of a methylthioninium compound.