Polymer-Linked Ubenimex Composition for Solid Cancer Activity

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Solution Overview

Problem

Ubenimex, a drug used for leukemia, is ineffective at treating solid cancers due to insufficient concentration when administered at standard doses, necessitating higher concentrations several hundred times that of leukemia treatment to achieve an anticancer effect.

Innovation Solution

A compound is developed by linking multiple ubenimex molecules to a chain polymer, specifically a polypeptide containing lysine residues, to enhance its anticancer effect on solid cancers.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If ubenimex is administered at standard doses for leukemia, then it can treat acute leukemia effectively, but it cannot exert an effective anticancer effect on solid cancer due to insufficient concentration

Engineering Contradiction:
Improveanticancer effect on solid cancerVSAvoidconcentration of ubenimex
Core Design Contradiction:
ReliabilityVSQuantity of substance

Solution Approach 1:

Multiple ubenimex molecules are linked to a single polymer carrier to form a conjugate, effectively combining multiple drug molecules into one delivery vehicle. This allows the drug to reach target cells at much higher effective concentrations without requiring hundreds of times higher systemic dosing

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The invention creates a composite material consisting of a polymer carrier conjugated with multiple ubenimex molecules. This composite structure enables the drug to achieve high local concentration at the target site while maintaining manageable systemic exposure levels

Inventive Principle:
Principle #40Composite materials

2Reliability

If ubenimex is administered at concentrations several hundred times higher than leukemia treatment to achieve solid cancer effect, then it can inhibit CD13/APN in solid cancers, but it results in impractical dosing requirements

Engineering Contradiction:
ImproveCD13/APN inhibition in solid cancerVSAvoiddosing feasibility
Core Design Contradiction:
ReliabilityVSEase of operation

Solution Approach 1:

The drug delivery system is segmented into a carrier component and multiple drug molecules, allowing the therapeutic effect to be concentrated at the target site while the carrier handles delivery and distribution, making dosing feasible at standard clinical levels

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The polymer carrier acts as an intermediary that binds multiple ubenimex molecules and delivers them to target cells, enabling high local concentration without requiring high systemic doses, thus making clinical dosing practical

Inventive Principle:
Principle #24Intermediary (Mediator)

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

The compound exhibits a higher anticancer effect on solid cancers, including synergistic effects when combined with other anticancer agents, and acts as a CD13/APN activity inhibitor.

Implementation Method 1

a compound comprising a chain structure in which a plurality of ubenimex molecules is linked to a polypeptide containing a lysine residue

Methodology Applied
Scientific EffectCovalent bonding: Chemical Bonding

Data Source

PatentEP3747909B1Anticancer agent
Publication Date: 2026.03.04 OSAKA UNIVERSITY
  • EP3747909B1 patent drawingFigure 1
  • EP3747909B1 patent drawingFigure 2-1A~2-1B
  • EP3747909B1 patent drawingFigure 2-2C~2-2D

AI summary

An object to be achieved by the present invention is to provide a technique for enhancing the anticancer effect of ubenimex; in particular, enhancing its anticancer effect on solid cancer. This object can be achieved by a compound containing a chain structure in which a plurality of ubenimex molecules is linked to a chain polymer.