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Applied radiation and isotopes : including data, instrumentation and methods for use in agriculture, industry and medicine

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


PMID 25702887

Abstract

In the present study, we successfully radiolabeled gefitinib with (99m)Tc by direct labeling method. The radio-ligand had radiolabeling efficiency of >95.0% and in vitro stability of >80.0% at 24h. The radiotracer cleared from blood bi-exponentially. Animal organ biodistribution data indicated hepato-renal 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 3.3±0.2 at 1h.

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