Acyclovir–Dexamethasone Combination Therapy for Alzheimer’s Neuroinflammation

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Solution Overview

Problem

Current treatments for Alzheimer's disease (AD) only alleviate symptoms and do not prevent or delay its progression, and the effectiveness of existing drugs like cholinesterase inhibitors and N-methyl-D-aspartate receptor antagonists is limited.

Innovation Solution

A combination therapy using acyclovir and dexamethasone (DXMT) is administered to treat AD, targeting neuroinflammation, synaptic protein expression, and cognitive impairment by inhibiting Aβ oligomers, reducing pro-inflammatory cytokines, and preserving PSD-95 expression.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of operation

If cholinesterase inhibitors and NMDA receptor antagonists are used to treat AD, then cognitive symptoms are alleviated, but the disease progression cannot be prevented or delayed

Engineering Contradiction:
Improvesymptom reliefVSAvoiddisease progression prevention
Core Design Contradiction:
Ease of operationVSReliability

Solution Approach 1:

The patent combines acyclovir and dexamethasone into a synergistic therapy regimen. Acyclovir targets HSV-1 replication while dexamethasone provides anti-inflammatory and immunomodulatory effects, creating a multi-mechanism approach that addresses both viral etiology and neuroinflammation, thereby achieving both symptom relief and disease progression prevention

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The patent modifies the treatment approach by changing the pharmacological parameters from conventional single-drug therapy to a combination therapy with specific dosing ratios (acyclovir 5-10 mg/kg/day and dexamethasone 0.05-0.2 mg/kg/day). This parameter change enables simultaneous achievement of antiviral, anti-inflammatory, and neuroprotective effects that were not possible with single agents

Inventive Principle:
Principle #35Parameter changes

2Reliability

If acyclovir is used alone to treat AD, then HSV-1 replication is inhibited, but weight loss and gastrointestinal side effects occur

Engineering Contradiction:
Improveantiviral effectVSAvoidweight loss and gastrointestinal side effects
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

Dexamethasone acts as an intermediary substance that mitigates the harmful effects of acyclovir. It provides glucocorticoid-mediated protection against acyclovir-induced weight loss and gastrointestinal irritation, allowing the antiviral therapy to be maintained at effective doses without excessive toxicity

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent creates a composite therapeutic formulation combining acyclovir and dexamethasone in specific proportions. This composite approach integrates the antiviral properties of acyclovir with the protective and anti-inflammatory properties of dexamethasone, achieving a balanced therapeutic profile that maximizes benefit while minimizing harm

Inventive Principle:
Principle #40Composite materials

3Object-affected harmful factors

If dexamethasone is used alone to treat AD, then neuroinflammation is reduced, but cognitive impairment may be exacerbated

Engineering Contradiction:
ImproveneuroinflammationVSAvoidcognitive function
Core Design Contradiction:
Object-affected harmful factorsVSEase of operation

Solution Approach 1:

The patent segments the therapeutic function into two distinct components: acyclovir handles the antiviral and neuroprotective aspects, while dexamethasone handles the anti-inflammatory aspects. This segmentation allows each drug to operate at optimal doses for its specific function, with acyclovir counteracting the cognitive side effects of dexamethasone while dexamethasone amplifies the neuroprotective effects of acyclovir

Inventive Principle:
Principle #1Segmentation

4Reliability

If combination therapy with acyclovir and dexamethasone is used, then spatial cognitive impairment and neuroinflammation are improved, but treatment complexity increases

Engineering Contradiction:
Improvecognitive protection and neuroinflammation reductionVSAvoidtreatment regimen
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent demonstrates that the acyclovir-dexamethasone combination serves multiple functions simultaneously: antiviral activity, anti-inflammatory activity, neuroprotective activity, and cognitive protection. This multi-functionality justifies the treatment complexity by delivering multiple therapeutic benefits through a single combination regimen rather than requiring multiple separate therapies

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

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 of acyclovir and DXMT significantly alleviates spatial cognitive impairment, reduces neuroinflammation, and prevents Aβ oligomer-induced decreases in PSD-95 expression, offering a new therapeutic approach for AD.

Implementation Method 1

acyclovir could inhibit tryptophan-2,3-dioxygenase activity both in vitro and in vivo, leading to increases of serotonin and 5-hydroxyindole acetic acid levels

Methodology Applied
Scientific EffectEnzyme inhibition: Enzyme

Implementation Method 2

Dexamethasone (DXMT), a synthetic glucocorticoid, is clinically used for treatment of allergic reactions and inflammatory skin conditions

Methodology Applied
Scientific EffectAnti-inflammatory effect:

Implementation Method 3

the acyclovir and the DXMT can also prevent Aβ oligomer-inducedhyperactivation of microglia and astrocytes, and overexpression of pro-inflammatory cytokines

Methodology Applied
Scientific EffectNeuroinflammation inhibition:

Implementation Method 4

combined use of the acyclovir and the DXMT can block a Aβ oligomer-induced decrease of PSD95 expression, suggesting a protective effect of a drug combination on synapses

Methodology Applied
Scientific EffectSynaptic protection:

Data Source

PatentEP4035669B1Combination of acyclovir and dexamethasone for use in treating alzheimer's disease
Publication Date: 2025.10.08 PLANTARX LTD
  • EP4035669B1 patent drawingFigure 1~3B
  • EP4035669B1 patent drawingFigure 4A~4D
  • EP4035669B1 patent drawingFigure 5A~5D

AI summary

The present disclosure provides use of a combination of acyclovir and dexamethasone (DXMT) in preparation of a drug for treating Alzheimer's disease (AD); where the use includes all symptoms of a patient with the AD, especially following symptoms: cognitive impairment and neuroinflammation. Combination of the acyclovir and the DXMT has a synergistic effect, to exert anti-inflammatory and immunoregulation effects to achieve an therapeutic effect.