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Updated: Sep 23, 2026
Pretargeted Radioimmunotherapy Based on the Inverse Electron Demand Diels-Alder Reaction
Published on: January 29, 2019
Radioimmuno targetting (99m)technetium labeled anti-epidermal growth factor receptor monoclonal antibodies in
A Meenakshi1, V Ganesh, R Suresh Kumar
1Department of Biochemical Oncology, Cancer Institute (WIA), Regional Center for Cancer Research and Treatment of Government of India, Adyar, Chennai, India. meenakshi_a3@rediffmail.com
Aim:
Monoclonal antibodies (MAb) directed at the extra cellular domain (ECD) of epidermal growth factor receptor (EGFR) offer a promising strategy for diagnosis and therapy of cancers that over-express EGFR. Radiolabelled MAbs against cell surface antigens have improved in vivo tumor diagnosis and treatment. EGFR over-expression has been reported in a wide range of carcinomas especially of the head and neck, breast, etc., and is associated with poor prognosis and resistance to therapy. CIBCNSH3 is a murine MAb generated to the ECD of EGFR in our laboratory and has been extensively characterized and has proven antitumor activity. The tumor targeting potential of (99m)Tc labelled CIBCNSH3 in an experimental tumor model is discussed in this paper.
Methods:
A431, an epidermoid carcinoma cell line with overexpression of EGFR, SUDHLH, a lymphoma cell line was used to induce xenografts in inbred adult female BALB/C mice and used for the study. A reduction mediated method of (99m)Tc labelling was adopted to label the MAb. Scintiscan pictures were taken at different time intervals after i.v. administration of the (99m)Tc labelled MAb using a gamma camera and results were correlated with those of biodistribution studies.
Results:
Immunoscan pictures taken at different time periods showed high uptake of the radioimmunoconjugate by the tumor providing clear tumor images and no uptake in control animals with lymphoma xenografts. Results of scan pictures correlated well with the biodistribution studies.
Conclusion:
The radioimmunoconjugate (99m)Tc-CIBCNSH3 appears to be a promising tool in identifying any early recurrence and micro-metastasis of lesions that overexpress EGFR.
Insights
This study shows that the radioimmunoconjugate (99m)Tc-CIBCNSH3 effectively targets tumors overexpressing the epidermal growth factor receptor (EGFR). This imaging agent holds promise for detecting early cancer recurrence and micrometastases.
Area of Science:
- Oncology
- Nuclear Medicine
- Immunology
Background:
- Epidermal Growth Factor Receptor (EGFR) overexpression is linked to poor prognosis in various cancers.
- Monoclonal antibodies (MAbs) targeting EGFR offer diagnostic and therapeutic potential.
- Radiolabeled MAbs enhance in vivo tumor imaging and treatment.
Purpose of the Study:
- To evaluate the tumor targeting capability of a novel radioimmunoconjugate, (99m)Tc-CIBCNSH3, in an experimental cancer model.
- To assess the utility of (99m)Tc-CIBCNSH3 for imaging EGFR-overexpressing tumors.
Main Methods:
- The study utilized A431 epidermoid carcinoma xenografts in BALB/C mice.
- (99m)Tc labeling of the CIBCNSH3 MAb was performed using a reduction-mediated method.
- In vivo imaging was conducted using a gamma camera, with results correlated to biodistribution studies.
Main Results:
- Immunoscintigraphy revealed high uptake of (99m)Tc-CIBCNSH3 in EGFR-overexpressing tumors, yielding clear images.
- No significant uptake was observed in control lymphoma xenografts.
- Scan results demonstrated strong correlation with biodistribution data.
Conclusions:
- The radioimmunoconjugate (99m)Tc-CIBCNSH3 shows significant promise as an imaging agent.
- It can potentially aid in the early detection of EGFR-overexpressing cancer recurrence and micrometastases.
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