Aromatic-Cationic Peptides for Atherosclerosis Plaque Reduction

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Solution Overview

Problem

Current treatments for atherosclerosis are inadequate in effectively preventing or treating the condition, particularly in terms of managing atherosclerotic plaques and mitigating statin-related side effects.

Innovation Solution

Administration of aromatic-cationic peptides, such as D-Arg-2′6′-Dmt-Lys-Phe-NH2, either alone or in combination with antihyperlipidemic drugs like statins, to reduce atherosclerotic plaque size and cholesterol content, and to alleviate statin side effects.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Quantity of substance

If statins are administered to treat atherosclerosis, then lipid levels are improved, but statin-related side effects occur

Engineering Contradiction:
Improvelipid levelsVSAvoidstatin-related side effects
Core Design Contradiction:
Quantity of substanceVSObject-affected harmful factors

Solution Approach 1:

The aromatic-cationic peptide acts as an intermediary substance that mediates between the statin treatment and the patient's physiological system. The peptide specifically binds to and clears foam cells in atherosclerotic plaques, thereby reducing plaque burden and cholesterol content independently of statin mechanism, while allowing statins to be used at optimal doses for lipid management without being limited by side effect constraints

Inventive Principle:
Principle #24Intermediary (Mediator)

2Reliability

If current treatments are used for atherosclerosis, then some therapeutic effect is achieved, but effectiveness in preventing or treating the condition is inadequate

Engineering Contradiction:
Improvetherapeutic effectVSAvoideffectiveness in preventing or treating
Core Design Contradiction:
ReliabilityVSProductivity

Solution Approach 1:

The invention merges two distinct therapeutic approaches: statin therapy for lipid management and aromatic-cationic peptide therapy for direct plaque and foam cell clearance. This combination creates a synergistic effect where statins continue to lower circulating lipids while the peptide directly removes existing atherosclerotic plaques and foam cells, thereby simultaneously improving prevention and treatment effectiveness beyond what either treatment could achieve alone

Inventive Principle:
Principle #5Merging (Combining)

3Quantity of substance

If statin dosage is increased to improve lipid management, then lipid level control is improved, but statin side effects increase

Engineering Contradiction:
Improvelipid level managementVSAvoidstatin side effects
Core Design Contradiction:
Quantity of substanceVSObject-affected harmful factors

Solution Approach 1:

The aromatic-cationic peptide serves as a mediator that takes over the plaque-clearing function, allowing statins to be dosed optimally for lipid management without being constrained by side effect thresholds. The peptide's direct action on foam cells and plaques provides an alternative pathway for achieving therapeutic goals that does not share the same side effect profile as statins

Inventive Principle:
Principle #24Intermediary (Mediator)

Data Source

PatentUS10201585B2Methods for treatment of atherosclerosis
Publication Date: 2019.02.12 STEALTH BIOTHERAPEUTICS INC
  • US10201585B2 patent drawing
  • US10201585B2 patent drawing
  • US10201585B2 patent drawing

AI summary

Disclosed herein are methods and compositions for preventing or treating atherosclerosis in a mammalian subject. The methods comprise administering to the subject an effective amount of an aromatic-cationic peptide and, in some applications, a second active agent, to subjects in need thereof. The present technology relates to the treatment or prevention of atherosclerosis in mammals through the administration of a therapeutically effective amount of aromatic cationic peptides and, in some embodiments, a second active agent.