کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1875793 | 1532098 | 2015 | 5 صفحه PDF | دانلود رایگان |
• Gefitinib – an epidermal growth factor receptor inhibitor was successfully radiolabeled with 99mTc and the resultant radiolabel 99mTc-gefitinib had high radiolabeling efficiency and in vitro stability.
• The radiotracer cleared from blood bi-exponentially.
• Animal organ biodistribution data demonstrated hepato-renal excretion of the radiotracer.
• Gamma camera imaging in tumor bearing mice demonstrated that the radiotracer accumulated in the tumor site with high target to non target ratio.
• The diagnostic efficacy of 99mTc-gefitinib needs clinical validation in tumors expressing high EGFR density.
In the present study, we successfully radiolabeled gefitinib with 99mTc 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 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 1 h.
Journal: Applied Radiation and Isotopes - Volume 99, May 2015, Pages 41–45