uPAR-PET/CT Tracers for HNSCC Relapse Risk Stratification

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Solution Overview

Problem

Current methods lack reliable prognostic tools for identifying candidates for de-escalated treatment in head and neck squamous cell carcinoma (HNSCC), particularly for HPV-positive tumors, and existing biomarkers like 18F-FDG-PET provide inconsistent results.

Innovation Solution

Development of uPAR-PET tracers, such as 68Ga-NOTA-AE105, for PET/CT imaging to assess uPAR expression, which correlates with relapse-free survival (RFS) in HNSCC patients, allowing for risk stratification and de-escalated treatment selection.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Measurement precision

If 18F-FDG-PET is used for prognostication in HNSCC patients, then metabolic activity can be assessed, but the results are inconsistent and lack reliability

Engineering Contradiction:
Improveprognostication accuracyVSAvoidconsistency of results
Core Design Contradiction:
Measurement precisionVSReliability

Solution Approach 1:

The patent changes the biochemical parameter being measured from general glucose metabolism (18F-FDG) to specific uPAR receptor expression (68Ga-NOTA-AE105). This parameter change targets the specific molecular mechanism driving tumor invasion and metastasis, providing more consistent and reliable prognostic information for HNSCC patients.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent introduces uPAR as an intermediary biomarker that specifically mediates the relationship between tumor biology and clinical outcome. By using 68Ga-NOTA-AE105 to target uPAR, the system provides a more direct and reliable connection to tumor aggressiveness and relapse risk compared to the non-specific 18F-FDG metabolic imaging.

Inventive Principle:
Principle #24Intermediary (Mediator)

2Object-affected harmful factors

If de-escalated treatment regimens are applied to HPV-positive HNSCC patients, then treatment toxicity is reduced, but survival outcomes deteriorate due to lack of reliable risk stratification

Engineering Contradiction:
Improvetreatment toxicityVSAvoidsurvival outcome
Core Design Contradiction:
Object-affected harmful factorsVSReliability

Solution Approach 1:

The patent applies local quality by using 68Ga-NOTA-AE105 PET imaging to identify specific subgroups of patients with low uPAR expression who would benefit from de-escalated treatment. This allows treatment intensity to be locally optimized based on individual tumor biology rather than applying uniform de-escalation to all HPV-positive patients, maintaining survival outcomes while reducing toxicity in appropriate candidates.

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The patent implements feedback by using uPAR-PET imaging results to guide treatment decisions. The imaging provides real-time biological feedback about tumor aggressiveness, allowing clinicians to adjust treatment intensity accordingly - reducing therapy for low-uPAR patients and maintaining aggressive therapy for high-uPAR patients, thus preserving survival outcomes while minimizing unnecessary toxicity.

Inventive Principle:
Principle #23Feedback

3Measurement precision

If 68Ga-NOTA-AE105 is used for uPAR-PET imaging, then relapse-free survival prediction is improved, but the complexity of the imaging protocol increases

Engineering Contradiction:
Improverelapse-free survival predictionVSAvoidimaging protocol complexity
Core Design Contradiction:
Measurement precisionVSDevice complexity

Solution Approach 1:

The patent leverages the universality of 68Ga labeling chemistry and PET imaging technology. The 68Ga radionuclide can be easily chelated to the NOTA-peptide conjugate using established protocols, and the imaging is performed on standard PET/CT scanners already available in clinical settings. This multi-functionality approach maintains high prognostic precision while minimizing protocol complexity by using universally available technologies.

Inventive Principle:
Principle #6Universality (Multi-functionality)

Data Source

PatentEP4440628B1Urokinase-type plasminogen activator receptor (UPAR)-pet/CT in head and neck squamous cell carcinomas (hnsccs)
Publication Date: 2025.12.31 CURASIGHT APS
  • EP4440628B1 patent drawingFigure 1
  • EP4440628B1 patent drawingFigure 2
  • EP4440628B1 patent drawingFigure 3A~3B

AI summary

The present invention relates to the a positron-emitting imaging agent for use in the prognosis of a head and neck cancer (HNSCC) in a subject by PET imaging of the cancer, wherein said imaging agent comprises a uPAR bindingpeptide coupled via the chelating agent NOTA or DOTA to the radionuclide 568Ga or 64Cu.