Retinoid Composition for Reducing Left Ventricular Stiffness

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Solution Overview

Problem

There is a lack of effective therapeutic options for heart failure with diastolic dysfunction, particularly heart failure with preserved left ventricular ejection fraction (HFpEF), which is associated with high mortality and poor quality of life, and existing treatments for other forms of heart failure do not provide sufficient efficacy.

Innovation Solution

A pharmaceutical composition comprising retinoids, specifically tamibarotene or peretinoin, is administered to treat heart failure with diastolic dysfunction, including HFpEF, HFrEF, and HFmrEF, by improving diastolic function and reducing tissue fibrosis.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional heart failure drugs (ARNIs, β-blockers, MRAs) are administered to HFpEF patients, then standard heart failure treatment protocols are followed, but treatment efficacy is not clear and no effective therapy exists

Engineering Contradiction:
Improvetreatment efficacyVSAvoiddrug effectiveness for HFpEF
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent applies parameter changes by switching from conventional heart failure drugs to retinoid-based therapy, fundamentally changing the pharmacological approach. Clinical studies demonstrated that retinoids significantly improved diastolic function parameters (E/e' ratio, stiffness constant β) in HFpEF patients, achieving effective treatment where conventional drugs failed

Inventive Principle:
Principle #35Parameter changes

2Reliability

If SGLT2 inhibitors are used for HFpEF treatment, then some efficacy is observed in clinical studies, but the mechanism for improving diastolic function is insufficient

Engineering Contradiction:
Improveclinical efficacyVSAvoiddiastolic dysfunction persistence
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent replaces the metabolic mechanism of SGLT2 inhibitors with a direct mechanical effect mechanism. Retinoids directly improve myocardial relaxation and reduce stiffness through their action on cardiac tissue, providing a more direct and effective approach to correcting diastolic dysfunction compared to the indirect metabolic effects of SGLT2 inhibitors

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

Data Source

PatentUS20250295620A1Pharmaceutical composition for treatment of heart failure with diastolic dysfunction
Publication Date: 2025.09.25 TOKO PHARMA IND
  • US20250295620A1 patent drawing
  • US20250295620A1 patent drawing
  • US20250295620A1 patent drawing

AI summary

The present invention provides a pharmaceutical composition for treating heart failure with diastolic dysfunction, comprising a retinoid as an active ingredient. The heart failure with diastolic dysfunction may be heart failure with preserved left ventricular ejection fraction, heart failure with mid-range left ventricular ejection fraction, or heart failure with reduced left ventricular ejection fraction.