Colchicine Derivative Therapy for Plaque Inflammation Control

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Solution Overview

Problem

Existing treatments for atherosclerotic vascular disease, such as anti-platelet and statin therapy, fail to effectively target inflammatory pathways, leading to a continued risk of cardiovascular events despite routine use.

Innovation Solution

Administering a therapeutically effective amount of a colchicine derivative or its salt, optionally combined with statins and anti-platelet agents, to treat or prevent cardiovascular events by reducing cholesterol crystal-induced inflammation in atherosclerotic plaques.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If anti-platelet and statin therapy are used routinely, then cardiovascular disease management is standard, but inflammatory pathways remain untargeted and cardiovascular events continue to occur

Engineering Contradiction:

Improveeffectiveness of cardiovascular treatmentVSAvoidcoverage of inflammatory pathways

Core Design Contradiction:

ReliabilityVSAdaptability or versatility

Solution Approach 1:

The treatment approach is segmented into multiple independent therapeutic agents: anti-platelet agents (aspirin, clopidogrel), statins (atorvastatin, simvastatin), and colchicine. Each agent targets a specific pathway (platelet aggregation, cholesterol synthesis, and inflammatory response respectively), allowing comprehensive coverage without requiring a single multi-functional drug.

Inventive Principle:

Principle #1Segmentation

Solution Approach 2:

The patent employs a composite treatment regimen combining three distinct drug classes with complementary mechanisms of action. This multi-component therapeutic strategy addresses multiple pathological processes simultaneously: platelet activation, lipid metabolism, and inflammation, creating a synergistic effect that overcomes the limitations of monotherapy.

Inventive Principle:

Principle #40Composite materials

2Ease of operation

If additional treatments (antiplatelet agents, anticoagulants, ACEIs, ARAs, beta-blockers, calcium channel blockers, nitrates) are used, then acute conditions are addressed, but long-term reduction in cardiovascular events in stable disease is not achieved

Engineering Contradiction:

Improveavailability of treatment optionsVSAvoidlong-term prevention effect

Core Design Contradiction:

Ease of operationVSDuration of action of stationary object

Solution Approach 1:

Colchicine is introduced as a proactive preventive agent that targets subclinical inflammation in stable atherosclerotic disease before acute events occur. The treatment addresses the underlying inflammatory drive of atherosclerosis progression, preventing plaque instability and rupture before they lead to acute cardiovascular events.

Inventive Principle:

Principle #10Preliminary action

Solution Approach 2:

The patent utilizes conventional, well-established drug classes with known safety profiles and cost-effective formulations. Colchicine, in particular, is an inexpensive agent with a long track record of use that can be administered orally for prolonged periods, making it suitable for chronic prevention in stable disease.

Inventive Principle:

Principle #27Cheap short-living objects (Disposable)

3Stability of the object's composition

If neutrophil infiltration and activation are allowed to proceed, then plaque response to injury occurs, but plaque instability increases leading to enlargement and rupture

Engineering Contradiction:

Improveplaque structural integrityVSAvoidinflammatory response from neutrophils

Core Design Contradiction:

Stability of the object's compositionVSObject-generated harmful factors

Solution Approach 1:

Colchicine acts as an intermediary agent that specifically interferes with neutrophil function and activation. It binds to tubulin and disrupts microtubule formation, thereby inhibiting neutrophil chemotaxis, adhesion, and degranulation. This mediation prevents neutrophils from exacerbating plaque inflammation and instability while allowing essential immune surveillance to continue.

Inventive Principle:

Principle #24Intermediary (Mediator)

Data Source

PatentUS20250302776A1Treatment or prevention of cardiovascular events via the administration of a colchicine derivative

Publication Date: 2025.10.02 MURRAY & POOLE ENTERPRISES LTD

AI summary

A method for reducing a composite endpoint risk of myocardial infarction (MI), stroke, coronary revascularization, unstable angina requiring hospitalization, cardiac arrest, and cardiovascular death in a subject including administering, orally once per day to the subject, a composition comprising about 0.5 total mg of (i) colchicine, (ii) a pharmaceutically acceptable salt of (i), or any combination of (i) and (ii), wherein the patient has at least one history of diabetes, a past myocardial infarction, an unstable angina, a coronary bypass surgery, and a coronary angioplasty; wherein the patient is also administered a daily dose of statin therapy; and wherein the composite endpoint risk in the subject is reduced relative to a dosing regimen where the patient receives standard secondary prevention therapy of a statin.