Timolol and Adenosine A1 Agonist Combination for IOP Reduction

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Solution Overview

Problem

Current treatments for glaucoma and ocular hypertension are inadequate in effectively reducing intraocular pressure, which is a major risk factor for these conditions, particularly primary open-angle glaucoma and ocular hypertension.

Innovation Solution

A pharmaceutical composition combining a non-selective beta-adrenergic receptor blocker, such as timolol, with an adenosine A1 receptor agonist, specifically Compound A, is administered topically to the eye to reduce intraocular pressure.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current treatments for glaucoma and ocular hypertension are used, then they provide some reduction in intraocular pressure, but they are inadequate in effectively reducing intraocular pressure

Engineering Contradiction:

Improveeffectiveness of IOP reductionVSAvoidadequacy of pressure reduction

Core Design Contradiction:

ReliabilityVSProductivity

Solution Approach 1:

The patent combines two different pharmacological agents with distinct mechanisms of action: a non-selective beta-adrenergic receptor blocker (timolol) that reduces aqueous humor production, and an adenosine A1 receptor agonist (Compound A) that enhances conventional outflow. This merging of two therapeutic approaches into a single combination therapy achieves superior IOP reduction compared to either agent alone, directly resolving the inadequacy of current monotherapies.

Inventive Principle:

Principle #5Merging (Combining)

2Reliability

If a combination of timolol and Compound A is administered, then intraocular pressure is significantly lowered, but the treatment targets multiple pathways increasing complexity

Engineering Contradiction:

ImproveIOP reduction efficacyVSAvoidtreatment mechanism complexity

Core Design Contradiction:

ReliabilityVSDevice complexity

Solution Approach 1:

The patent merges two separate treatment mechanisms into a single combination product that addresses both aqueous humor production (via timolol's beta-blockade) and conventional outflow (via Compound A's adenosine A1 agonism). This consolidation simplifies the overall treatment approach by delivering dual-action therapy through a unified regimen, despite the underlying pharmacological complexity.

Inventive Principle:

Principle #5Merging (Combining)

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 combination significantly lowers intraocular pressure, as demonstrated in pre-clinical studies, providing an effective treatment for glaucoma and ocular hypertension by targeting both aqueous humor production and conventional outflow pathways.

Implementation Method 1

a non-selective beta-adrenergic receptor blocker, such as timolol

Methodology Applied

Scientific EffectBeta-adrenergic receptor blockade:

Implementation Method 2

an adenosine A1 receptor agonist, specifically Compound A

Methodology Applied

Scientific EffectAdenosine A1 receptor agonism:

Data Source

PatentEP2555776B1Combination compositions of adenosine a1 agonists and non-selective beta-adrenergic receptor blockers for reducing intraocular pressure

Publication Date: 2016.12.07 INOTECK PHARMA CORP

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AI summary

Provided herein is a pharmaceutical composition or a kit comprising a combination of a non-selective beta-adrenergic receptor blocker and an adenosine A1 receptor agonist. Also provided herein is a method of reducing intraocular pressure (IOP) in a subject using such a combination or kit. In a particular embodiment, provided herein is a combination of timolol marketed under the brand TimopticTM and Compound A.