TrkB Ligand Conjugated Compounds for Targeted CNS Delivery

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Solution Overview

Problem

Current methods for delivering therapeutic, prophylactic, or diagnostic compounds in vivo often result in unintended consequences, such as off-target effects, due to lack of specificity in targeting desired cells or tissues.

Innovation Solution

Development of compounds comprising a Tropomyosin Receptor Kinase B (TrkB) ligand linked to a therapeutic, prophylactic, or diagnostic agent, which selectively targets cells expressing TrkB, thereby enhancing the specificity and efficacy of compound delivery.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If compounds are administered systemically to deliver therapeutic agents in vivo, then the therapeutic compound can reach desired cells, but off-target effects occur due to lack of specificity

Engineering Contradiction:
Improvespecificity of compound deliveryVSAvoidoff-target effects
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent employs a targeting ligand as an intermediary component that specifically binds to TrkB receptors on desired cells. This ligand acts as a mediator between the therapeutic compound and the target cell, enabling selective delivery while preventing systemic distribution to non-target tissues, thereby eliminating off-target effects

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The compound is segmented into distinct functional components: a targeting ligand portion that provides specificity through TrkB receptor binding, and a therapeutic agent portion that delivers the therapeutic effect. This segmentation allows the targeting function and therapeutic function to be independently optimized and combined

Inventive Principle:
Principle #1Segmentation

2Device complexity

If compounds are delivered without targeting ligands, then the delivery process is simpler, but the therapeutic effect is reduced due to inability to reach desired cells efficiently

Engineering Contradiction:
Improvecompound structure complexityVSAvoidefficacy of compound delivery
Core Design Contradiction:
Device complexityVSReliability

Solution Approach 1:

The patent merges the targeting ligand and therapeutic agent into a single conjugated compound. This combination integrates the cell-specific targeting capability of the ligand with the therapeutic functionality of the agent, enabling efficient delivery to desired cells while maintaining a unified compound structure that can be administered as a single entity

Inventive Principle:
Principle #5Merging (Combining)

Data Source

PatentUS20250161459A1Trkb ligand conjugated compounds and uses thereof
Publication Date: 2025.05.22 ADARX PHARMACEUTICALS INC
  • US20250161459A1 patent drawing
  • US20250161459A1 patent drawing
  • US20250161459A1 patent drawing

AI summary

Provided herein are TrkB ligand-containing compounds, methods of delivering said compounds, and methods of treating diseases, disorders, and symptoms (e.g., central nervous system diseases, disorders, and symptoms) in a subject using said compounds.