13-Cis-Retinoic Acid-Ascorbic Acid Conjugate for Soluble Cancer Therapy

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Solution Overview

Problem

Current epigenetic modifying drugs targeting retinoic acid signaling in cancer treatment are only partly effective, and there is a need for better understanding of mechanisms to enhance the therapeutic potential of retinoic acids in treating malignancies like acute myeloid leukemia (AML).

Innovation Solution

Conjugate compounds comprising 13-cis-retinoic acid and vitamin C (ascorbic acid) are developed, which increase water solubility and reduce the effective dosage, providing therapeutic activity against various cancers.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If epigenetic modifying drugs are used alone to target retinoic acid signaling in cancer treatment, then they can alter chromatin structure and gene expression, but they are only partly effective against different cancers

Engineering Contradiction:

Improvetherapeutic effectivenessVSAvoidbroad-spectrum cancer treatment capability

Core Design Contradiction:

ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent combines 13-cis-retinoic acid with ascorbic acid (vitamin C) to create a conjugate compound. This merging of two distinct compounds aims to achieve synergistic effects where the combination overcomes the limited effectiveness of epigenetic modifying drugs used alone, while maintaining the ability to target multiple cancer types through dual mechanisms of action.

Inventive Principle:

Principle #5Merging (Combining)

2Reliability

If the dosage of 13-cis-retinoic acid is increased to enhance therapeutic activity, then anticancer effects are improved, but toxicity increases

Engineering Contradiction:

Improveanticancer therapeutic activityVSAvoidtoxicity

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The invention creates a composite conjugate compound where 13-cis-retinoic acid is chemically linked to ascorbic acid. This composite structure allows the therapeutic components to work together at lower doses, achieving the desired anticancer effect while reducing the toxicity associated with high doses of 13-cis-retinoic acid alone.

Inventive Principle:

Principle #40Composite materials

3Reliability

If retinoic acid derivatives are used to treat cancer, then they exert specific effects on cell proliferation and differentiation, but their water solubility is limited

Engineering Contradiction:

Improvetherapeutic activityVSAvoidwater solubility

Core Design Contradiction:

ReliabilityVSQuantity of substance

Solution Approach 1:

Ascorbic acid serves as an intermediary molecule that improves the water solubility of the conjugate compound. By attaching ascorbic acid to 13-cis-retinoic acid, the conjugate gains enhanced aqueous solubility while retaining the therapeutic activity of the retinoic acid component, facilitating better drug delivery and bioavailability.

Inventive Principle:

Principle #24Intermediary (Mediator)

Data Source

PatentUS20260001854A1Conjugate compound comprising 13-cis-retinoic acid and ascorbic acid

Publication Date: 2026.01.01 MASTERY BIOTECH CO LTD

AI summary

The present invention relates to a conjugate compound comprising 13-cis-retinoic acid and vitamin C, and its pharmaceutically acceptable salts thereof. The present invention also relates to a pharmaceutical composition comprising the compound and a pharmaceutically acceptable carrier. The present compound has a much better water solubility than that of retinoic acid, and thus reduces an effective dosage of retinoic acid and minimizes side effects. The present compound increases the efficiency and concentration of 13-cis-retinoic acid to cross the cell membrane into the cell. The present compound is useful in treating cancer such as pancreatic cancer.