TCO Conjugates for Selective Therapeutic Delivery

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Solution Overview

Problem

Current methods for delivering therapeutic or diagnostic agents to specific tissues or organs lack precision and efficiency, often resulting in unintended distribution and reduced effectiveness.

Innovation Solution

A composition comprising a biocompatible solid support with a linker and binding agents, such as trans-cyclooctene and tetrazine, that covalently link therapeutic or diagnostic agents, allowing for selective delivery by implanting the solid support and administering a complementary binding agent, enabling targeted release at the desired location.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Measurement precision

If conventional delivery methods are used, then the therapeutic agent can be administered systemically, but the delivery precision and effectiveness are reduced due to unintended distribution

Engineering Contradiction:
Improvedelivery precisionVSAvoidunintended distribution
Core Design Contradiction:
Measurement precisionVSLoss of substance

Solution Approach 1:

The patent employs binding agents (such as trans-cyclooctene and tetrazine) as intermediary molecules that mediate between the solid support implant and the therapeutic agent. These binding agents enable selective binding and release of the therapeutic agent at the targeted location, achieving precise delivery while preventing unintended distribution throughout the body.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The invention implements local quality by creating a localized delivery system where the solid support implant is placed at a specific target location. The binding agents are designed to selectively interact with complementary molecules only at this local site, concentrating the therapeutic agent exactly where needed and avoiding systemic distribution.

Inventive Principle:
Principle #3Local quality

2Productivity

If the linker is made shorter (1-10 linking atoms), then the binding and release kinetics are enhanced, but the synthesis complexity increases

Engineering Contradiction:
Improvebinding and release kineticsVSAvoidsynthesis complexity
Core Design Contradiction:
ProductivityVSDevice complexity

Solution Approach 1:

The patent applies parameter changes by systematically varying the linker length parameter to optimize performance. By selecting linkers with 1-10 linking atoms, the invention achieves enhanced binding and release kinetics. The synthesis complexity is managed by focusing on this specific range rather than exploring all possible linker lengths, thereby optimizing the trade-off between kinetic performance and synthetic feasibility.

Inventive Principle:
Principle #35Parameter changes

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

This approach enables precise and enhanced delivery of therapeutic or diagnostic agents to targeted tissues or organs, increasing the concentration at the site of need while minimizing distribution to other areas, as demonstrated by increased binding and release kinetics in in-vitro and in-vivo studies.

Implementation Method 1

a linker having from about 1 to about 10 linking atoms, covalently linking each binding agent to the biocompatible solid support

Methodology Applied
Scientific EffectCovalent bonding: Chemical Bonding

Implementation Method 2

the first and second binding agents bind to one another upon contact

Methodology Applied
Scientific EffectComplementary binding: Chemical Bonding

Data Source

PatentUS12257326B2TCO conjugates and methods for delivery of therapeutic agents
Publication Date: 2025.03.25 THE RES FOUNDATION FOR THE STATE UNIV OF NEW YORK
  • US12257326B2 patent drawing
  • US12257326B2 patent drawing
  • US12257326B2 patent drawing

AI summary

The present invention provides a method for selective delivery of a therapeutic or diagnostic agent to a targeted organ or tissue by implanting a biocompatible solid support in the patient being linked to a first binding agent, and administering a second binding agent to the patient linked to the therapeutic or diagnostic agent, such that the therapeutic or diagnostic agent accumulates at the targeted organ or tissue.