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99mTc-LHRH in tumor receptor imaging
Dawei Hao1, Lingfei Sun1, Xiang Hu1
1Department of Radiotherapy, Xuzhou Central Hospital, Xuzhou, Jiangsu 221009, P.R. China.
Oncology Letters
|July 12, 2017
Summary
This study developed a novel method for radiolabeling LHRH with 99mTc, demonstrating its high purity, stability, and receptor binding affinity. This 99mTc-LHRH shows promise as a diagnostic imaging agent for various cancers expressing GnRH receptors.
Area of Science:
- Nuclear medicine
- Oncology
- Radiochemistry
Background:
- Gonadotropin-releasing hormone (GnRH), also known as luteinizing hormone-releasing hormone (LHRH), plays a role in various physiological processes.
- Aberrant expression of GnRH receptors (GnRH-R) has been observed in several human cancers, suggesting their potential as therapeutic and diagnostic targets.
Purpose of the Study:
- To develop and evaluate a direct radioiodination method for LHRH using Technetium-99m (99mTc).
- To assess the feasibility of using 99mTc-LHRH as an imaging agent for GnRH receptor-positive tumors.
Main Methods:
- Immunohistochemical staining was performed on tumor tissues from patients with hepatocellular carcinoma, breast, prostate, lung, and endometrial cancers to determine LHRH-R expression levels.
- A pre-tin method was employed for direct radio labeling of LHRH with 99mTc, optimizing labeling conditions for radiochemical purity and stability.
- In vitro receptor binding assays using rat pituitary cell membranes were conducted to evaluate the binding affinity of 99mTc-LHRH.
- In vivo biodistribution studies in mice were performed using 131I-LHRH to assess clearance and organ accumulation patterns.
Main Results:
- High expression of LHRH-R was detected in tumor tissues: 82.61% in HCC, 95% in breast cancer, 70% in prostate cancer, 85% in lung cancer, and 80% in endometrial cancer, compared to lower rates in normal tissues.
- The 99mTc-LHRH labeling method yielded high radiochemical purity (93.9-96.4%) and stability, with a simple and rapid preparation process.
- In vitro studies confirmed that 99mTc-LHRH exhibits saturable receptor binding with high affinity, demonstrating biological activity.
- In vivo studies showed rapid clearance from the blood and accumulation in the liver and kidneys, with gradual decrease over time.
Conclusions:
- GnRH receptors are present in hepatocellular, lung, breast, prostate, and endometrial cancers.
- 99mTc-LHRH can be prepared efficiently with high purity and stability, retaining significant receptor binding ability and biological activity.
- 99mTc-LHRH demonstrates promising characteristics for clinical application as a GnRH receptor imaging agent.
