PDE5 and AChEI Inhibitor Composition for Neurodegenerative Disease
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Solution Overview
Problem
Current treatments for neurodegenerative diseases such as dementia, Parkinson's disease, and Alzheimer's disease primarily focus on symptom relief and are not effective in halting the progression of the diseases, and they often come with significant side effects.
Innovation Solution
A composition combining a phosphodiesterase 5 inhibitor (PDE5) and an acetylcholinesterase inhibitor (AChEI), such as mirodenafil with donepezil, galantamine, or rivastigmine, is used to reduce neuroinflammation, inhibit proinflammatory cytokines, and decrease toxic protein expression, particularly beta-amyloid, thereby protecting nerve cells and enhancing synaptic plasticity.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If conventional therapeutic agents are used to regulate symptoms of neurodegenerative diseases, then symptom relief is achieved, but the disease progression cannot be halted and significant side effects occur
Solution Approach 1:
The patent combines two different therapeutic agents with distinct mechanisms of action into a single composition: (1) an acetylcholinesterase inhibitor that increases acetylcholine levels to improve cognitive symptoms, and (2) an anti-inflammatory agent that targets neuroinflammation to potentially halt disease progression. This merged approach addresses both symptom relief and disease modification simultaneously, resolving the contradiction between ease of operation and reliability
2Ease of operation
If acetylcholinesterase inhibitors are used alone to treat neurodegenerative diseases, then cognitive symptoms are improved, but neuroinflammation and disease progression are not effectively addressed
Solution Approach 1:
The invention merges an acetylcholinesterase inhibitor (for cognitive symptom improvement) with an anti-inflammatory agent (for neuroinflammation control) into a single composition. The acetylcholinesterase inhibitor component maintains cognitive function by increasing acetylcholine levels, while the anti-inflammatory component addresses neuroinflammation through multiple mechanisms including inhibition of proinflammatory cytokines and activation of anti-inflammatory pathways, thereby resolving the contradiction between symptom improvement and harmful factor control
Data Source
AI summary
The present invention provides a composition for preventing or treating a neurodegenerative disease containing a phosphodiesterase 5 inhibitor (PDE5 inhibitors) and an acetylcholinesterase inhibitor (AChEI) and a method using thereof, wherein the PDE5 inhibitor is selected from among mirodenafil, sildenafil, vardenafil, tadalafil, udenafil, dasantafil, avanafil, pharmaceutically acceptable salts, solvates, hydrates, and a mixture thereof; and the AchEI is selected from among donepezil, rivastigmine, galantamine, physostigmine, tacrine, metrifonate, phenserine, tolserine, eseroline, huperizine A and B, galangin, cardanol, donepezil-AP2238, donepezil-tacrine, tacrine-ferulic acid hybrid, tacrine-hydroxyquinoline, ladostigil, indenyl derivatives, pharmaceutically acceptable salts, solvates, hydrates and a mixture thereof; and the neurodegenerative disease is dementia, Parkinson's disease (PD), Alzheimer's disease (AD), Huntington's disease (HD) or Multiple sclerosis (MS).