Adenosine A1 Agonist Ophthalmic Composition for Glaucoma
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Solution Overview
Problem
Current glaucoma treatments, such as miotics, carbonic anhydrase inhibitors, and beta-blockers, often come with undesirable side effects, leading to decreased patient compliance and ineffective management of elevated intraocular pressure (IOP) in glaucoma and ocular hypertension.
Innovation Solution
The use of a selective adenosine A1 agonist, specifically ((2R,3S,4R,5R)-5-(6-(cyclopentylamino)-9H-purin-9-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyl nitrate, administered topically as an ophthalmic pharmaceutical composition, to reduce IOP in humans with glaucoma or ocular hypertension.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If existing glaucoma treatments (miotics, carbonic anhydrase inhibitors, beta-blockers) are used to reduce intraocular pressure, then IOP reduction is achieved, but undesirable side effects occur leading to decreased patient compliance
Solution Approach 1:
The patent applies parameter changes by switching from conventional glaucoma treatment mechanisms to adenosine A1 receptor agonism. This represents a fundamental change in the pharmacological parameter (receptor target) while maintaining the therapeutic goal of IOP reduction, thereby achieving effectiveness while avoiding the side effects associated with traditional agents
Solution Approach 2:
The patent introduces adenosine A1 receptor agonists as an intermediary mechanism. Instead of directly affecting aqueous humor production or outflow through conventional pathways, the treatment uses adenosine receptor activation as an intermediate step to achieve IOP reduction, which provides a safer alternative with fewer side effects
2Reliability
If existing glaucoma treatments are used to control IOP, then pressure reduction is achieved, but patient compliance decreases due to side effects
Solution Approach 1:
The patent changes the pharmacological parameter from conventional agents to adenosine A1 receptor agonists, which provides effective IOP control while having a more favorable side effect profile, thereby improving patient compliance without sacrificing therapeutic reliability
3Reliability
If conventional glaucoma therapies are administered to reduce IOP, then therapeutic effect is achieved, but treatment safety decreases due to serious side effects
Solution Approach 1:
The patent uses adenosine A1 receptor agonism as an intermediary mechanism that achieves IOP reduction through a different physiological pathway, avoiding the direct toxic effects on pulmonary tissue, ocular structures, and other systems associated with conventional therapies
Solution Approach 2:
The patent extracts the essential therapeutic function (IOP reduction) from the harmful components of conventional treatments by selecting a different mechanism of action that achieves the same goal without the associated side effects
Data Source
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AI summary
Provided herein are compounds of Formula I, compositions comprising an effective amount of a compound of Formula I, and methods for reducing intraocular pressure comprising administering an effective amount of compounds of Formula I to a subject in need thereof.