Ascomycin Therapy for BMPR2 Signaling in Pulmonary Hypertension

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Solution Overview

Problem

Current therapies for pulmonary hypertension, particularly pulmonary arterial hypertension, are unsatisfactory due to limitations and side effects, and there is a need for new treatments that can effectively increase BMPR2 signaling to address this condition.

Innovation Solution

Administering a therapeutically effective amount of ascomycin or its pharmaceutically acceptable salts, solvates, analogs, or prodrugs to increase BMPR2 signaling in patients with pulmonary hypertension, thereby treating or preventing conditions associated with reduced BMPR2 expression.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current therapies for pulmonary hypertension are used, then some symptomatic relief is provided, but they have limitations and side effects that make them unsatisfactory

Engineering Contradiction:

Improvetherapeutic effectivenessVSAvoidside effects

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent changes the therapeutic parameter from existing PH treatments to BMPR2 pathway activation using ascomycin and related compounds. This parameter change targets the underlying molecular mechanism of PAH (reduced BMPR2 signaling) rather than just symptomatic management, thereby improving therapeutic effectiveness while avoiding the side effects of current therapies

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent uses ascomycin, a compound originally developed for immunosuppression, and copies/adapts it for PAH treatment by exploiting its ability to activate BMPR2 signaling. This repurposing approach allows leveraging a well-characterized compound with known safety profile for a new indication, reducing the need for entirely new drug development

Inventive Principle:

Principle #26Copying

2Reliability

If BMPR2 signaling is increased to treat pulmonary arterial hypertension, then disease progression is addressed, but new therapeutic agents are required

Engineering Contradiction:

Improvedisease modificationVSAvoidtherapeutic approach complexity

Core Design Contradiction:

ReliabilityVSDevice complexity

Solution Approach 1:

The patent exploits the body's endogenous BMPR2 pathway, which is naturally present but dysfunctional in PAH. By using ascomycin to reactivate this existing physiological pathway rather than introducing entirely new complex mechanisms, the treatment achieves disease modification through a relatively simple approach that leverages the body's own repair systems

Inventive Principle:

Principle #25Self-service

Solution Approach 2:

Instead of trying to block the harmful pathways involved in PAH (vasoconstriction, proliferation), the patent inverts the approach by activating the protective BMPR2 pathway that is normally suppressed in PAH. This inverse strategy addresses the root cause of the disease by restoring normal physiological signaling rather than merely counteracting pathological effects

Inventive Principle:

Principle #13The other way round (Inversion)

Data Source

PatentUS20260021078A1Compositions and methods for the treatment or prevention of pulmonary hypertension

Publication Date: 2026.01.22 VIVUS LLC

AI summary

The present invention provides compositions and methods for the treatment or prevention of pulmonary hypertension comprising administering an ascomycin, or a pharmaceutically acceptable salt, solvate, analog, or prodrug thereof to the patient with pulmonary hypertension.