R(+) Pramipexole Enantiomer for Eosinophil Reduction

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Solution Overview

Problem

Current treatments for conditions characterized by elevated levels of eosinophils, basophils, or neutrophils often result in adverse side effects and fail to effectively manage these conditions, particularly in inflammatory disorders.

Innovation Solution

Administration of R(+) pramipexole or its pharmaceutically acceptable salt, which acts as a dopamine agonist, to reduce eosinophil, basophil, or neutrophil counts, with dosages ranging from 50 mg to 1,500 mg per day, administered in fractions or as a maintenance regimen, potentially combined with other therapeutic agents to manage inflammatory conditions.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Quantity of substance

If current treatments are used to reduce eosinophil levels, then eosinophil counts decrease, but adverse side effects increase

Engineering Contradiction:
Improveeosinophil countVSAvoidadverse side effects
Core Design Contradiction:
Quantity of substanceVSObject-affected harmful factors

Solution Approach 1:

The patent changes the chemical parameter by using R(+) pramipexole, a specific enantiomer of pramipexole, which has different pharmacological properties compared to the racemic mixture or other dopaminergic agents. This parameter change (using the pure R(+) enantiomer) achieves eosinophil reduction while minimizing adverse side effects through more selective dopaminergic receptor activation

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent extracts and isolates the therapeutically beneficial R(+) enantiomer from the racemic pramipexole mixture. By separating and using only the R(+) form, the treatment achieves the desired eosinophil-reducing effect while eliminating or reducing the adverse effects associated with the S(-) enantiomer

Inventive Principle:
Principle #2Taking out (Extraction)

2Object-generated harmful factors

If current treatments are used to manage inflammatory disorders, then inflammation is reduced, but treatment effectiveness is insufficient

Engineering Contradiction:
ImproveinflammationVSAvoidtreatment effectiveness
Core Design Contradiction:
Object-generated harmful factorsVSReliability

Solution Approach 1:

The patent changes the dosing parameter by administering R(+) pramipexole at doses of 50-1500 mg per day in divided doses, which optimizes the therapeutic effect on eosinophil-associated inflammation while maintaining safety. This dosing regimen provides sustained eosinophil reduction and reliable treatment effectiveness for inflammatory disorders

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent employs an induction step where a second therapeutic agent is administered for 1 week to 6 months before or concurrent with R(+) pramipexole treatment. This preliminary action rapidly reduces eosinophil levels to a safe range, after which R(+) pramipexole maintains long-term control with reliable effectiveness

Inventive Principle:
Principle #10Preliminary action

Data Source

PatentUS10980783B2Compositions and methods for treating conditions related to increased eosinophils
Publication Date: 2021.04.20 ARETEIA THERAPEUTICS INC
  • US10980783B2 patent drawing
  • US10980783B2 patent drawing
  • US10980783B2 patent drawing

AI summary

Disclosed herein are methods of treating diseases associated with increased numbers of eosinophils basophils, and/or neutrophils with R(+) pramipexole.