Ring-Modified Peptide-Urea Derivatives for PSMA Tumor Retention

Solution Overview

Problem

Existing peptide-urea derivatives for prostate cancer diagnosis and treatment lack structural diversity, leading to unsatisfactory pharmacokinetics, with excessive accumulation in non-target organs like the kidney and insufficient retention time on target tumor cells.

Innovation Solution

A novel peptide-urea derivative with specific ring structures and chelating capabilities, designed to enhance uptake and retention on target cells while reducing accumulation in non-target organs, facilitating both imaging and treatment of prostate cancer.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If existing peptide-urea derivatives are used for prostate cancer imaging and treatment, then they can bind to PSMA on tumor cells, but they accumulate excessively in non-target organs like the kidney and remain too long, causing potential harm

Engineering Contradiction:

Improvetargeting accuracyVSAvoidaccumulation in non-target organs

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent introduces different ring structures (cyclic carbon chains or cyclic heteroatom chains) at specific positions of the peptide-urea derivative to create local structural variations. These local structural changes modify the pharmacokinetic properties of the molecule, reducing its accumulation in non-target organs like the kidney while preserving its binding affinity to PSMA on tumor cells.

Inventive Principle:

Principle #3Local quality

Solution Approach 2:

The patent systematically varies structural parameters of the peptide-urea derivative, including the type of ring structure (carbon-based vs. heteroatom-based), the position of the ring structure, and the size of the ring (number of atoms). These parameter changes optimize the balance between targeting efficiency and clearance rate, reducing harmful accumulation in non-target organs.

Inventive Principle:

Principle #35Parameter changes

2Reliability

If existing peptide-urea derivatives are used for prostate cancer imaging and treatment, then they can bind to PSMA on tumor cells, but their retention time on target tumor cells is insufficient

Engineering Contradiction:

Improvetargeting accuracyVSAvoidretention time on target cells

Core Design Contradiction:

ReliabilityVSDuration of action of moving object

Solution Approach 1:

The patent introduces different ring structures (cyclic carbon chains or cyclic heteroatom chains) at specific positions of the peptide-urea derivative to create local structural variations. These local structural changes modify the pharmacokinetic properties of the molecule, reducing its accumulation in non-target organs like the kidney while preserving its binding affinity to PSMA on tumor cells.

Inventive Principle:

Principle #3Local quality

Solution Approach 2:

The patent systematically varies structural parameters of the peptide-urea derivative, including the type of ring structure (carbon-based vs. heteroatom-based), the position of the ring structure, and the size of the ring (number of atoms). These parameter changes optimize the balance between targeting efficiency and clearance rate, reducing harmful accumulation in non-target organs.

Inventive Principle:

Principle #35Parameter changes

3Adaptability or versatility

If existing peptide-urea derivatives are used, then they have a basic structure for PSMA binding, but they lack structural diversity leading to unsatisfactory pharmacokinetics

Engineering Contradiction:

Improvestructural diversityVSAvoidpharmacokinetics performance

Core Design Contradiction:

Adaptability or versatilityVSReliability

Solution Approach 1:

The patent introduces different ring structures (cyclic carbon chains or cyclic heteroatom chains) at specific positions of the peptide-urea derivative to create local structural variations. These local structural changes modify the pharmacokinetic properties of the molecule, reducing its accumulation in non-target organs like the kidney while preserving its binding affinity to PSMA on tumor cells.

Inventive Principle:

Principle #3Local quality

Solution Approach 2:

The patent systematically varies structural parameters of the peptide-urea derivative, including the type of ring structure (carbon-based vs. heteroatom-based), the position of the ring structure, and the size of the ring (number of atoms). These parameter changes optimize the balance between targeting efficiency and clearance rate, reducing harmful accumulation in non-target organs.

Inventive Principle:

Principle #35Parameter changes

Data Source

PatentUS20250319194A1Peptide-urea derivative, pharmaceutical composition containing same and application thereof

Publication Date: 2025.10.16 BIVISION PHARM INC

AI summary

A peptide-urea derivative, a pharmaceutical composition containing same and an application thereof are provided, the derivative being as shown in formula I. The derivative can be used for preoperative imaging diagnosis and grading of PSMA-positive prostate cancer, and can also be used for the treatment of various types and stages of prostate cancer, achieving the integration of diagnosis and treatment, and having broad application prospects.