Rapamycin Enteric Delivery for Long-Term Intestinal Polyp Prevention

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Solution Overview

Problem

Current therapies for preventing intestinal polyps and intestinal cancer are inadequate, with existing chemopreventive agents like NSAIDs and COX-2 inhibitors posing cardiovascular risks and lacking long-term effectiveness.

Innovation Solution

Administration of rapamycin or its analogs, potentially in encapsulated or nanoparticle form, to patients at risk for developing intestinal polyps or cancer, utilizing enteric coatings to enhance bioavailability and minimize side effects.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If NSAIDs and COX-2 inhibitors are used for chemoprevention of intestinal polyps, then polyp progression is delayed, but cardiovascular toxicity increases

Engineering Contradiction:

Improvechemopreventive effectivenessVSAvoidcardiovascular toxicity

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent extracts the harmful cardiovascular side effects from the chemopreventive treatment by replacing NSAIDs/COX-2 inhibitors with mTOR inhibitors (rapamycin and analogs) that do not share the same adverse effect profile, thereby maintaining polyp prevention efficacy while eliminating cardiovascular toxicity

Inventive Principle:

Principle #2Taking out (Extraction)

Solution Approach 2:

The patent changes the pharmacological parameter from COX inhibition to mTOR inhibition, switching to a different molecular target and mechanism of action that achieves chemoprevention through a pathway unrelated to cardiovascular side effects

Inventive Principle:

Principle #35Parameter changes

2Duration of action of stationary object

If rapamycin or analogs are administered long-term for chemoprevention, then polyp development is prevented, but drug tolerance and side effects may increase

Engineering Contradiction:

Improvechemoprevention durationVSAvoiddrug toxicity

Core Design Contradiction:

Duration of action of stationary objectVSObject-affected harmful factors

Solution Approach 1:

The patent employs periodic administration of rapamycin or its analogs, using dosing schedules that maintain therapeutic levels while allowing drug-free intervals to minimize cumulative toxicity and maintain long-term tolerability

Inventive Principle:

Principle #19Periodic action

Solution Approach 2:

The patent uses enteric coating as an intermediary delivery system that protects the rapamycin analogs from degradation in the stomach, enables targeted release in the intestine, and reduces gastrointestinal side effects, thereby facilitating long-term administration

Inventive Principle:

Principle #24Intermediary (Mediator)

3Quantity of substance

If enteric coating is applied to rapamycin composition, then bioavailability is enhanced, but manufacturing complexity increases

Engineering Contradiction:

Improvedrug bioavailabilityVSAvoidcoating process complexity

Core Design Contradiction:

Quantity of substanceVSEase of manufacture

Solution Approach 1:

The patent optimizes the enteric coating parameters including polymer composition, thickness, and dissolution pH to achieve reliable intestinal release of rapamycin analogs while maintaining manufacturability through standardized coating processes

Inventive Principle:

Principle #35Parameter changes

Data Source

PatentUS12383538B2Use of mTOR inhibitors for prevention of intestinal polyp growth and cancer

Publication Date: 2025.08.12 BOARD OF RGT THE UNIV OF TEXAS SYST

AI summary

Disclosed are methods and compositions for the treatment or prevention of intestinal polyps or prevention of cancer in a patient who has been identified as being at risk for developing intestinal polyps or intestinal cancer. The disclosed methods and compositions include rapamycin, a rapamycin analog, or another such inhibitor of the target of rapamycin (TOR).