Oral L-DOPA and Melatonin AMD Treatment

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Solution Overview

Problem

Current treatments for age-related macular degeneration (AMD) are limited, particularly for dry AMD, and existing therapies like intraocular injections are expensive, painful, and risky, highlighting the need for improved compositions and methods for treating AMD.

Innovation Solution

Pharmaceutical compositions comprising GPR143 receptor agonists such as L-DOPA or its analogues, melatonin, or melatonin analogues, combined with a pharmaceutically acceptable carrier, administered orally or as eye drops, to regulate retinal pigment epithelial cell functions and control VEGF expression, potentially delaying AMD progression.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If intraocular injections of antibodies or proteins are used to treat wet AMD, then treatment effectiveness is improved, but treatment cost increases, patient comfort deteriorates, and infection risk increases

Engineering Contradiction:
Improvetreatment effectivenessVSAvoidinfection risk
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent replaces the mechanical/invasive intraocular injection system with a non-invasive oral or topical administration system. The composition uses orally bioavailable compounds (L-DOPA, melatonin) that can be administered through the gastrointestinal tract or topical eye application, eliminating the need for needle injections and associated infection risks while maintaining therapeutic effectiveness through systemic or localized delivery to the retina

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

Solution Approach 2:

The patent introduces intermediary compounds (L-DOPA as a prodrug that converts to dopamine, and melatonin) that can be administered systemically and then transported to the retinal tissue. These intermediaries serve as safe carriers that avoid direct injection into the eye while still delivering the therapeutic effect through conversion to active forms at the target site

Inventive Principle:
Principle #24Intermediary (Mediator)

2Reliability

If intraocular injections are administered repeatedly, then treatment effectiveness is maintained, but treatment cost increases and patient burden increases

Engineering Contradiction:
Improvetreatment effectivenessVSAvoidtreatment frequency
Core Design Contradiction:
ReliabilityVSLoss of time

Solution Approach 1:

The patent enables continuous therapeutic action through oral or topical administration of L-DOPA and melatonin, which can be taken daily without interruption. This continuous delivery system maintains steady drug levels in the retina over time, eliminating the need for repeated clinical visits and injections, thereby reducing time loss while sustaining treatment effectiveness

Inventive Principle:
Principle #20Continuity of useful action

Solution Approach 2:

The patent employs compounds with long half-lives and sustained release characteristics that allow patients to self-administer treatment at home without requiring frequent professional intervention. The oral formulation enables patients to maintain their own therapy continuously, reducing dependency on healthcare facilities and minimizing time spent on treatment procedures

Inventive Principle:
Principle #25Self-service

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 compositions induce a circadian rhythm in retinal pigment epithelial cells, reducing the risk or delaying the progression of AMD by coordinating key cellular functions, providing a safer and more effective treatment option compared to existing therapies.

Implementation Method 1

The compositions induce a circadian rhythm in retinal pigment epithelial cells, reducing the risk or delaying the progression of AMD by coordinating key cellular functions

Methodology Applied
Scientific EffectCircadian rhythm:

Data Source

PatentUS11969401B2Compositions and methods for treating or limiting development of age-related macular degeneration
Publication Date: 2024.04.30 THE ARIZONA BOARD OF REGENTS ON BEHALF OF THE UNIV OF ARIZONA
  • US11969401B2 patent drawing
  • US11969401B2 patent drawing
  • US11969401B2 patent drawing

AI summary

The disclosure provides methods for treating or limiting development age-related macular degeneration, comprising (a) a GPR143 receptor agonist, including but not limited to L-DOPA, L-DOPA analogues, or a pharmaceutically acceptable salt thereof, and (b) melatonin, a melatonin analogue, or a pharmaceutically acceptable salt thereof, and related compositions.