Synthesis and evaluation of ⁶⁴Cu-radiolabeled NOTA-cetuximab (⁶⁴Cu-NOTA-C225) for immuno-PET imaging of EGFR expression.

ABSTRACT:

Objective

Epidermal growth factor receptor (EGFR) is overexpressed in a wide variety of solid tumors, serving as a well-characterized target for cancer imaging or therapy. In this study, we aimed to design and synthesize a radiotracer, ⁶⁴Cu-NOTA-C225, targeting EGFR for tumor positron emission tomography (PET) imaging.

Methods

Cetuximab (C225) was conjugated to a bifunctional chelator, p-isothiocyanatobenzyl-1,4,7-triazacyclononane-1,4,7-triacetic acid (NOTA), and further radiolabeled with copper-64 for PET imaging. ⁶⁴Cu-NOTA-IgG and Cy5.5-C225 were also synthesized as control probes. A431 and A549 mouse models were established for micro-PET and/or near-infrared fluorescence (NIRF) imaging.

Results

⁶⁴Cu-NOTA-C225 exhibited stability

SUBMITTER: Xu X 

PROVIDER: S-EPMC6513748 | biostudies-literature | 2019 Apr

REPOSITORIES: biostudies-literature