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Published on: February 3, 2015
Targeted radionuclide therapy for lung cancer with iodine-131-labeled peptide in a nude-mouse model
Zhenzhu Chen1, Hongyi Gao, Man Li
1aDepartment of Pathology, Zhujiang Hospital bDepartment of Nuclear Medicine, Nanfang Hospital, Southern Medical University, Guangzhou, People's Republic of China.
Abstract:
Integrin α3β1 has been shown to be a novel candidate target for the imaging and specific therapy of non-small-cell lung cancer. We have previously reported on a peptide containing a novel motif of NGXG that specifically binds to the integrin α3 receptor on lung cancer cells using a one-bead one-peptide combinatorial library. In this study, we developed the peptide cNGEGQQc-based therapeutic agent labeling with radionuclide iodine-131 (I) and evaluated its characteristics including stability, biodistribution, antitumor activity, and safety. The results showed that I-cNGEGQQc was stable in serum. Furthermore, the biodistribution of I-cNGEGQQc was determined in normal mice and rabbits. In-vivo biodistribution studies showed that radiolabeled peptide in the kidney was significantly higher than that in other organs. Nude mice bearing lung cancer cell xenografts (H1975 and L78) were used as an in-vivo model for tumor-inhibition efficacy studies with I-cNGEGQQc. The tumor growth decreased significantly in mice receiving I-labeled peptide compared with the controls and the effect of I-labeled peptide can be blocked by unlabeled cNGEGQQc. Safety studies showed that I-cNGEGQQc was relatively safe for animals without significant toxicity. Our data suggest that I-cNGEGQQc has potential as a targeted radiotherapeutic agent for non-small-cell lung cancer.
Insights
A novel peptide, I-cNGEGQQc, targets integrin α3β1 receptors on non-small-cell lung cancer cells. This radiolabeled peptide demonstrated significant tumor inhibition and safety in preclinical studies, showing potential for targeted lung cancer therapy.
Area of Science:
- Oncology
- Radiochemistry
- Molecular Imaging
Background:
- Integrin α3β1 is a promising target for non-small-cell lung cancer (NSCLC) imaging and therapy.
- A previously identified peptide motif (NGXG) specifically binds to the integrin α3 receptor on lung cancer cells.
Purpose of the Study:
- To develop and evaluate a novel therapeutic agent, cNGEGQQc, labeled with iodine-131 (¹³¹I).
- To assess the stability, biodistribution, antitumor activity, and safety of ¹³¹I-cNGEGQQc for NSCLC treatment.
Main Methods:
- Peptide synthesis and radiolabeling with ¹³¹I.
- In vitro stability assessment in serum.
- In vivo biodistribution studies in normal mice and rabbits.
- Tumor inhibition efficacy studies in nude mice bearing NSCLC xenografts.
- Blocking studies with unlabeled cNGEGQQc.
- Preclinical safety evaluation.
Main Results:
- ¹³¹I-cNGEGQQc exhibited stability in serum.
- Biodistribution studies showed highest uptake in the kidneys.
- Significant inhibition of lung cancer xenograft growth was observed with ¹³¹I-cNGEGQQc.
- The antitumor effect was confirmed to be receptor-mediated via blocking studies.
- The agent demonstrated a favorable safety profile with no significant toxicity.
Conclusions:
- ¹³¹I-cNGEGQQc is a stable and effective targeted radiotherapeutic agent candidate for NSCLC.
- The peptide's ability to inhibit tumor growth and its safety profile support its potential clinical application.
