Preclinical evaluation of Tc-99m labeled gefitinib as a potential scintigraphic probe for the detection of tumors expressing epidermal growth factor receptors

摘要

In the present study, we successfully radiolabeled gefitinib with Tc-99m by direct labeling method. The radio-ligand had radiolabeling efficiency of > 95.0% and in vitro stability of >80.0% at 24 h. The radiotracer cleared from blood bi-exponentially. Animal organ biodistribution data indicated hepatorenal excretion of the radiotracer. Scintigraphy carried out in tumor bearing mice (induced by EGFR expressing EAT cell lines) demonstrated that the radiotracer accumulated in the tumor site with T/NT ratio of 33 +/- 0.2 at 1 h. (C) 2015 Elsevier Ltd. All rights reserved.