Intravaginal DHEA Localized Conversion for Sexual Dysfunction

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Solution Overview

Problem

Current treatments for female sexual dysfunction (FSD) in menopausal women, particularly female sexual arousal disorder, hypoactive sexual desire disorder, and female orgasmic disorder, often focus on systemic hormone administration, which can have limited success and systemic side effects, and do not effectively address the distinct mechanisms of vaginal atrophy and sexual dysfunction.

Innovation Solution

The intravaginal administration of prasterone (DHEA) provides localized conversion to androgens and estrogens, bypassing systemic exposure, thereby addressing the hormonal deficiencies contributing to FSD independently of vaginal atrophy symptoms.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If systemic hormone administration is used to treat female sexual dysfunction, then hormonal deficiencies are addressed, but systemic side effects occur and success is limited

Engineering Contradiction:
Improvetreatment effectivenessVSAvoidsystemic side effects
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies local quality by administering DHEA directly to the vaginal tissue through intravaginal suppositories, creating a localized high concentration of the hormone precursor at the target site. This local administration allows the vaginal epithelium to convert DHEA into active androgens and estrogens through intracrine mechanisms, achieving effective local hormone levels without requiring systemic distribution. The approach transforms the treatment from a systemic to a localized intervention, thereby maintaining effectiveness while eliminating systemic side effects.

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The patent utilizes DHEA as an intermediary substance that serves as a precursor for local hormone synthesis. Rather than administering active hormones systemically, DHEA is introduced into the vaginal tissue where it acts as a mediator that is locally converted into the biologically active forms (testosterone, dihydrotestosterone, and estrogens) through enzymatic processes within the vaginal epithelium. This intermediary approach allows for controlled local hormone production without the need for systemic hormone delivery.

Inventive Principle:
Principle #24Intermediary (Mediator)

2Object-affected harmful factors

If intravaginal DHEA is administered, then local conversion to androgens and estrogens occurs without systemic exposure, but the mechanism differs from conventional systemic treatment approaches

Engineering Contradiction:
Improvesystemic exposureVSAvoidtreatment mechanism complexity
Core Design Contradiction:
Object-affected harmful factorsVSDevice complexity

Solution Approach 1:

The patent employs self-service by enabling the vaginal tissue to autonomously convert the administered DHEA into active hormones through its own intracrine enzymatic systems. The vaginal epithelium contains the necessary enzymes (such as 3β-hydroxysteroid dehydrogenase and aromatase) to transform DHEA into testosterone, dihydrotestosterone, and estrogens locally. This self-conversion mechanism eliminates the need for external hormone activation or complex delivery systems, as the target tissue itself performs the necessary biochemical transformations.

Inventive Principle:
Principle #25Self-service

Solution Approach 2:

The patent utilizes parameter changes by altering the physical and chemical state of hormone delivery from systemic circulation to localized tissue deposition. By changing the administration route from oral or injectable to intravaginal suppository form, the treatment achieves a fundamentally different pharmacokinetic profile: high local concentration with minimal systemic absorption. This parameter change in delivery method enables the unique intracrine conversion mechanism to dominate over systemic hormonal effects.

Inventive Principle:
Principle #35Parameter changes

3Area of stationary object

If DHEA is used at doses that act exclusively in the vagina, then vaginal dysfunction is treated, but the existing CNS-based paradigm for sexual dysfunction treatment is challenged

Engineering Contradiction:
Improvevaginal treatment areaVSAvoidparadigm understanding
Core Design Contradiction:
Area of stationary objectVSLoss of information

Solution Approach 1:

The patent applies segmentation by separating the treatment of vaginal dysfunction from the treatment of central nervous system-mediated sexual dysfunction. By demonstrating that intravaginal DHEA effectively treats vaginal atrophy and related symptoms through purely local intracrine mechanisms without significant systemic absorption, the invention divides the previously unified treatment approach into distinct pathways: local vaginal treatment for tissue-related symptoms and potential CNS-targeted treatments for desire and arousal disorders. This segmentation allows for more precise, mechanism-specific therapeutic interventions.

Inventive Principle:
Principle #1Segmentation

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

Intravaginal DHEA treatment significantly improves sexual desire, arousal, and orgasmic function in menopausal women, demonstrating a distinct mechanism of action that separates vaginal atrophy and sexual dysfunction as two separate entities, with benefits observed regardless of the presence or severity of vaginal pain or atrophy.

Implementation Method 1

DHEA acts exclusively in the vagina following its local conversion into androgens and/or estrogens by the mechanisms of intracrinology

Methodology Applied
Scientific EffectIntracrine conversion: Catalysis

Data Source

PatentEP2877183B1Improvement of sexual arousal, sexual desire, orgasm and/or pleasure following intravaginal prasterone (DHEA) administration in women not suffering or independently from dyspareunia or other symptoms of vulvo-vaginal atrophy
Publication Date: 2020.12.16 ENDORECHERCHE INC
  • EP2877183B1 patent drawingFigure 1
  • EP2877183B1 patent drawingFigure 2
  • EP2877183B1 patent drawingFigure 3

AI summary

Intravaginal DHEA is used for the treatment of at least one condition selected from the group consisting of female hypoactive sexual desire disorder, female sexual arousal disorder, female orgasm disorder and female sexual interest arousal disorder in a woman who either (1) is not suffering from symptoms of vulvo-vaginal atrophy and/or (2) is not suffering from moderate to severe dyspareunia.