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Published on: January 7, 2019
177Lu-labeled RGD-BBN heterodimeric peptide for targeting prostate carcinoma
Lei Jiang1, Zheng Miao, Hongguang Liu
1Department of Nuclear Medicine, Zhongshan Hospital, Fudan University, Shanghai, China.
Introduction:
Radiolabeled Arg-Gly-Asp (RGD) and bombesin (BBN) heterodimers have been investigated for dual targeting of tumor integrin αvβ3 receptors and gastrin-releasing peptide receptors. The goal of this study was to evaluate the potential use of a Lu-labeled RGD-BBN heterodimer for targeted prostate cancer therapy.
Materials And Methods:
A 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid-conjugated RGD-BBN peptide (DO3A-RGD-BBN) was radiolabeled with Lu and purified by high-performance liquid chromatography. The in-vivo biodistribution study of Lu-DO3A-RGD-BBN was carried out in mice bearing human prostate cancer PC3 xenografts. The receptor-targeting specificity of the radiolabeled peptide was assayed by injecting the tracer with the unlabeled RGD-BBN peptide. Radiation absorbed doses in adult male patients, based on biodistribution data from mice, were also calculated.
Results:
DO3A-RGD-BBN peptides were successfully labeled with Lu, and high radiochemical purity (>95%) could be achieved after high-performance liquid chromatography purification. In human PC3 xenograft-bearing mice, the tumor accumulation of Lu-DO3A-RGD-BBN was 5.88±1.12, 2.77±0.30, 2.04±0.19, and 1.18±0.19%ID/g at 0.5, 2, 24, and 48 h, respectively. With rapid clearance from normal tissues, the radiolabeled probe displayed high tumor-to-blood and tumor-to-muscle ratios. On calculating the radiation absorbed doses for Lu-DO3A-RGD-BBN, we found that the prostate tumor and the pancreas were the organs receiving the highest radiation absorbed doses.
Conclusion:
Dual integrin αvβ3 and GPRP-targeted agent Lu-DO3A-RGD-BBN shows excellent prostate cancer-targeting ability, and it is worthy of further evaluation for prostate cancer-targeted therapy.
Insights
Lutetium-177-labeled Arg-Gly-Asp (RGD) and bombesin (BBN) heterodimer (Lu-DO3A-RGD-BBN) effectively targets prostate cancer by binding to integrin αvβ3 and gastrin-releasing peptide receptors. This dual-targeting agent shows promising results for targeted prostate cancer therapy.
Area of Science:
- Nuclear medicine
- Oncology
- Radiopharmaceutical chemistry
Background:
- Radiolabeled Arg-Gly-Asp (RGD) and bombesin (BBN) heterodimers target integrin αvβ3 and gastrin-releasing peptide receptors (GRPR) on tumors.
- Dual-targeting agents are being investigated for enhanced tumor specificity in cancer therapy.
Purpose of the Study:
- To evaluate the potential of a Lutetium-177 (Lu)-labeled RGD-BBN heterodimer (Lu-DO3A-RGD-BBN) for targeted prostate cancer therapy.
- To assess the biodistribution and tumor-targeting capabilities of Lu-DO3A-RGD-BBN in a prostate cancer xenograft model.
Main Methods:
- A 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DO3A)-conjugated RGD-BBN peptide was synthesized and radiolabeled with Lu.
- High-performance liquid chromatography (HPLC) was used for purification and quality control.
- In vivo biodistribution studies were performed in mice bearing human prostate cancer PC3 xenografts.
- Receptor-targeting specificity was confirmed by co-injection with unlabeled RGD-BBN.
- Radiation absorbed doses were calculated based on biodistribution data.
Main Results:
- Lu-DO3A-RGD-BBN was successfully synthesized with high radiochemical purity (>95%) after HPLC purification.
- Significant tumor accumulation of Lu-DO3A-RGD-BBN was observed in PC3 xenografts, with peak uptake at 0.5 h post-injection.
- The radiolabeled peptide demonstrated rapid clearance from normal tissues, resulting in high tumor-to-blood and tumor-to-muscle ratios.
- Calculations indicated that the prostate tumor and pancreas received the highest radiation absorbed doses.
Conclusions:
- Lu-DO3A-RGD-BBN exhibits excellent targeting ability for prostate cancer through dual targeting of integrin αvβ3 and GRPR.
- The agent demonstrates favorable biodistribution characteristics for targeted radiotherapy.
- Lu-DO3A-RGD-BBN warrants further investigation for its therapeutic potential in prostate cancer treatment.
