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Updated: May 30, 2026

MR Molecular Imaging of Prostate Cancer with a Small Molecular CLT1 Peptide Targeted Contrast Agent
Published on: September 3, 2013
A novel indium-111-labeled gonadotropin-releasing hormone peptide for human prostate cancer imaging
Haixun Guo1, Fabio Gallazzi, Larry A Sklar
1College of Pharmacy, University of New Mexico, Albuquerque, NM 87131, USA.
Abstract:
The purpose of this study was to evaluate the tumor targeting and imaging properties of a novel (111)In-labeled gonadotropin-releasing hormone (GnRH) peptide {1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA)-Ahx-(D-Lys(6)-GnRH1)} for human prostate cancer. The biodistribution and tumor imaging properties of (111)In-DOTA-Ahx-(D-Lys(6)-GnRH1) were determined in DU145 human prostate cancer-xenografted nude mice. (111)In-DOTA-Ahx-(d-Lys(6)-GnRH1) exhibited rapid tumor uptake (1.27 ± 0.40% ID/g at 0.5h post-injection) coupled with fast whole-body clearance through the urinary system. The DU145 human prostate cancer-xenografted tumor lesions were clearly visualized by single photon emission computed tomography (SPECT)/CT at 0.5h post-injection of (111)In-DOTA-Ahx-(D-Lys(6)-GnRH1). The successful imaging of DU145 human prostate cancer-xenografted tumor lesions using (111)In-DOTA-Ahx-(d-Lys(6)-GnRH1) highlighted its potential as a novel imaging probe for human prostate cancer imaging.
Insights
A new imaging agent, indium-111 labeled DOTA-Ahx-(D-Lys(6)-GnRH1), effectively targets and visualizes prostate cancer in mice. This novel probe shows rapid uptake and clearance, enabling clear imaging of tumors via SPECT/CT.
Area of Science:
- Nuclear medicine
- Oncology
- Radiopharmaceutical chemistry
Background:
- Prostate cancer remains a significant health concern globally.
- Effective diagnostic tools are crucial for early detection and treatment planning.
- Gonadotropin-releasing hormone (GnRH) analogs show promise for targeted cancer therapies and imaging.
Purpose of the Study:
- To assess the tumor targeting and imaging capabilities of a novel indium-111 labeled GnRH peptide, {1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA)-Ahx-(D-Lys(6)-GnRH1)}.
- To evaluate its potential as an imaging agent for human prostate cancer.
Main Methods:
- The study utilized DU145 human prostate cancer-xenografted nude mice.
- Biodistribution and tumor imaging properties of (111)In-DOTA-Ahx-(D-Lys(6)-GnRH1) were determined.
- Single photon emission computed tomography (SPECT)/CT imaging was performed post-injection.
Main Results:
- The radiotracer (111)In-DOTA-Ahx-(D-Lys(6)-GnRH1) demonstrated rapid tumor uptake, reaching 1.27 ± 0.40% ID/g at 0.5 hours post-injection.
- Fast whole-body clearance was observed, primarily via the urinary system.
- DU145 xenografted tumor lesions were clearly visualized using SPECT/CT at 0.5 hours post-injection.
Conclusions:
- The (111)In-labeled GnRH peptide exhibits excellent tumor targeting and imaging properties for prostate cancer.
- Its rapid clearance and clear visualization capabilities suggest potential as a novel diagnostic imaging probe.
- This agent holds promise for enhancing the imaging of human prostate cancer.

