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MR Molecular Imaging of Prostate Cancer with a Small Molecular CLT1 Peptide Targeted Contrast Agent

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Published on: September 3, 2013

Engineering NIR Probes to Enhance Affinity and Clinical Workflow Compatibility for Prostate Cancer Imaging.

Gauri S Malankar¹, Dani A Szafran¹, Gourav Kumar¹

¹Department Biomedical Engineering, Oregon Health & Science University, Portland, Oregon, 97201, USA.

Angewandte Chemie (International Ed. in English)

|December 12, 2025

Summary

Researchers developed a novel fluorescent probe for prostate cancer surgery. This probe targets prostate specific membrane antigen (PSMA) and clears rapidly from the body, improving fluorescence-guided surgery (FGS) compatibility with radical prostatectomy (RARP) timelines.

Keywords:

Fluorescence‐guided surgery (FGS)Fluorescent probe Near Infrared (NIR) imaging Pharmacokinetic modulation Prostate cancer

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A Bright NIR-II Fluorescence Probe for Vascular and Tumor Imaging

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Published on: March 17, 2023

Area of Science:

Oncology
Medical Imaging
Chemical Biology

Background:

Positive surgical margins in radical prostatectomy correlate with increased risk of biochemical recurrence and disease progression.
Fluorescence-guided surgery (FGS) offers benefits for various cancers, but current prostate cancer probes have limitations.
Existing probes' long pharmacokinetic (PK) profiles hinder integration into clinical workflows due to lengthy waiting times.

Purpose of the Study:

To develop novel near-infrared (NIR) fluorescent probes for prostate cancer with improved pharmacokinetic properties.
To design probes that enable rapid off-target tissue clearance while maintaining high tumor specificity.
To create probes compatible with the clinical timelines of robotic-assisted radical prostatectomy (RARP).

Main Methods:

Developed a library of NIR water-soluble fluorescent probes using a tri-compartment design.
Incorporated a glutamic acid-urea-lysine (EuK) ligand targeting prostate specific membrane antigen (PSMA).
Optimized fluorophore and PK modulators for enhanced binding, rapid clearance, and in vivo tumor targeting.

Main Results:

Probes with PK modulators demonstrated superior tumor-specific fluorescence and accumulation compared to controls.
Molecular docking, photophysical properties, and cell staining showed comparable performance across designs.
Identified a lead probe with robust tumor targeting and accelerated off-target clearance.

Conclusions:

The developed probe design strategy successfully created a probe with optimal tumor-specific signal and contrast.
The lead probe's rapid clearance and effective targeting are compatible with RARP procedures.
This advancement addresses the clinical compatibility challenge of current prostate cancer imaging probes.