Synthesis and preclinical investigation of Tc-p-SCN-Bzl-DTPA-cetuximab for targeting EGFR using head and neck squamous cell carcinoma (HNSCC) xenografts.

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ID: 20034
2019
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Abstract
To assess the preclinical potential of technetium-99m labelled conjugated para-isothiocyanato-benzyl diethylene triamine penta-acetic acid cetuximab (Tc-p-SCN-Bzl-DTPA cetuximab) for imaging EGFR in HNSCC mice and rabbits xenografts. Cetuximab, a chimeric monoclonal antibody targeting EGFR, was conjugated with p-SCN-Bzl-DTPA followed by labelling with Tc. The labelled conjugate was evaluated for in vitro stability in cysteine at 37 °C. The Tc-p-SCN-Bzl-DTPA cetuximab was also investigated for immunoreactivity, internationalization kinetics, dose escalation (up to 300 µg) and biodistribution in HNSCC mice xenograft. The suitability of labelled moiety as a specific EGFR radio-tracer was assessed in HNSCC rabbit xenograft. Tc-p-SCN-Bzl-DTPA cetuximab exhibited more than 98% radiochemical purity at room temperature. In excess cysteine, it showed a stable behaviour at 37 °C up to 4 h p.l. The labelled conjugate was internalized in vitro in FaDu tumor cells up to 19.55%. Significantly higher uptake in tumor (at 10 µg; 34.75 ± 0.38% ID/g: pi) was seen in HNSCC mice xenograft with dose escalation assay from 1 to 300 µg/mouse. Blocking of EGFR with excess cetuximab consequently decreased the uptake of tumor up to 6.80 ± 1.25%. SPECT images of rabbit xenograft confirmed increase in tumor to background ratio after 4 h pi and validated its potential in preclinical trial as a specific FaDu tumor tracer. Our in vitro and in vivo preclinical findings indicate that the Tc-p-SCN-Bzl-DTPA cetuximab prepared at optimal dose of cetuximab could become a useful tool for EGFR imaging in HNSCC using SPECT.
Reference Key
shah2019synthesismolecular Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors Shah, Syed Qaiser;Gul-E-Raana, ;
Journal molecular biology reports
Year 2019
DOI
10.1007/s11033-019-04616-x
URL
Keywords Keywords not found

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