Imatinib Eye Drops for Dry Eye Corneal Damage

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Solution Overview

Problem

Current treatments for dry eye syndrome and associated ocular diseases, such as keratoconjunctivitis sicca, are insufficient in effectively addressing corneal damage and inflammation due to a lack of tear film, leading to discomfort and potential vision loss.

Innovation Solution

A pharmaceutical composition and eye drop formulation containing imatinib as the active ingredient, which selectively inhibits tyrosine kinase activity, is developed to prevent and treat dry eye syndrome and associated ocular diseases by protecting the corneal epithelium and reducing inflammation.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If artificial tears and conventional treatments are used to treat dry eye syndrome, then subjective symptoms are temporarily relieved, but corneal damage and inflammation are not effectively prevented

Engineering Contradiction:
Improveeffectiveness of treatmentVSAvoidcorneal damage and inflammation
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent introduces a completely new therapeutic parameter by using imatinib, a tyrosine kinase inhibitor, which targets the underlying pathological mechanism of dry eye syndrome. This differs from conventional treatments that only address symptoms, as imatinib blocks the signaling pathways that lead to corneal epithelial cell death and inflammation, thereby effectively preventing corneal damage while treating the disease.

Inventive Principle:
Principle #35Parameter changes

2Reliability

If imatinib is used as an eye drop to treat dry eye syndrome, then corneal damage and inflammation are effectively inhibited, but this represents a novel application of a leukemia treatment drug

Engineering Contradiction:
Improveprotection of corneal epitheliumVSAvoidnovelty of drug application
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent demonstrates the multi-functionality of imatinib by applying it to a completely different disease indication beyond its original use for chronic myelogenous leukemia and gastrointestinal stromal tumors. The drug's ability to inhibit tyrosine kinase signaling pathways makes it effective for both cancer treatment and dry eye syndrome, showcasing its universal applicability across different pathological conditions.

Inventive Principle:
Principle #6Universality (Multi-functionality)

3Object-affected harmful factors

If the tear film is insufficient due to increased evaporation or low secretion, then ocular surface friction increases causing inflammation, but current treatments do not sufficiently address the underlying mechanism

Engineering Contradiction:
Improveocular surface friction and inflammationVSAvoidadequacy of current treatments
Core Design Contradiction:
Object-affected harmful factorsVSReliability

Solution Approach 1:

The patent replaces the mechanical approach of lubrication (artificial tears) with a biochemical mechanism (tyrosine kinase inhibition). Instead of merely reducing friction through lubricating agents, imatinib blocks the cellular signaling pathways that lead to epithelial cell death and inflammation, addressing the root cause rather than just the mechanical symptom of friction.

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

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 imatinib eye drop effectively inhibits corneal damage, degeneration, and inflammation, providing a novel therapeutic approach for dry eye syndrome and associated ocular diseases, as demonstrated in animal models, with concentration-dependent effects.

Implementation Method 1

imatinib selectively inhibits the activity of a tyrosine kinase produced by the Philadelphia gene

Methodology Applied
Scientific EffectTyrosine kinase inhibition:

Data Source

PatentEP3311817B1Pharmaceutical composition for preventing and treating dry eye diseases, containing imatinib as active ingredient
Publication Date: 2019.12.11 AVIXGEN
  • EP3311817B1 patent drawingFigure 1
  • EP3311817B1 patent drawingFigure 2
  • EP3311817B1 patent drawingFigure 3

AI summary

The present invention relates to a composition for preventing or treating dry eye syndrome or eye diseases caused by dry dyes, containing imatinib as an active ingredient and, more specifically, to an eye bath lotion for preventing or treating dry eye syndrome or eye diseases associated with dry eye syndrome, containing imatinib an active ingredient. Imatinib of the present invention effectively protects the corneal epithelia and inhibits the degeneration thereof, thereby being usable for a use of alleviating or treating dry eye syndrome or eye diseases associated with dry eye syndrome.