title: Preclinical evaluation of (99m)Tc labeled gefitinib as a potential scintigraphic probe for the detection of tumors expressing epidermal growth factor receptors.
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.
authors.affiliation: Department of Nuclear Medicine, Postgraduate Institute of Medical & Research, Chandigarh, India.
authors.forename: Pardeep
authors.initials: P
authors.lastname: Kumar
authors.affiliation: Department of Nuclear Medicine, Postgraduate Institute of Medical & Research, Chandigarh, India. Electronic address: drbsingh5144@yahoo.com.
authors.forename: Baljinder
authors.initials: B
authors.lastname: Singh
authors.affiliation: Department of Nuclear Medicine, Postgraduate Institute of Medical & Research, Chandigarh, India.
authors.forename: Anchal
authors.initials: A
authors.lastname: Ghai
authors.affiliation: Division of Cyclotron & Radiopharmaceutical Sciences, Institute of Nuclear Medicine and Allied Sciences, Delhi, India.
authors.forename: Krishna
authors.initials: K
authors.lastname: Chuttani
authors.affiliation: Center for Nuclear Medicine, UIEAST, Panjab University, Chandigarh, India.
authors.forename: Devinder
authors.initials: D
authors.lastname: Dhawan
authors.affiliation: Department of Nuclear Medicine, Postgraduate Institute of Medical & Research, Chandigarh, India.
authors.forename: Bhagwant R
authors.initials: BR
authors.lastname: Mittal
authors.affiliation: Division of Cyclotron & Radiopharmaceutical Sciences, Institute of Nuclear Medicine and Allied Sciences, Delhi, India.
authors.forename: Anil K
authors.initials: AK
authors.lastname: Mishra
mesh_terms: D000818:Animals; D002286:Carcinoma, Ehrlich Tumor / Q000000981:diagnostic imaging* / Q000378:metabolism*; D045744:Cell Line, Tumor; D003287:Contrast Media / Q000493:pharmacokinetics; D066246:ErbB Receptors / Q000037:antagonists & inhibitors* / Q000378:metabolism*; D000077156:Gefitinib; D006801:Humans; D007553:Isotope Labeling / Q000379:methods; D008657:Metabolic Clearance Rate; D051379:Mice; D008807:Mice, Inbred BALB C; D015336:Molecular Probe Techniques; D015335:Molecular Probes; D011799:Quinazolines / Q000493:pharmacokinetics*; D011817:Rabbits; D011877:Radionuclide Imaging; D015203:Reproducibility of Results; D012680:Sensitivity and Specificity; D013667:Technetium / Q000493:pharmacokinetics*; D014018:Tissue Distribution
chemical_list: D003287:Contrast Media; D015335:Molecular Probes; D011799:Quinazolines; D013667:Technetium; C512478:EGFR protein, human; D066246:ErbB Receptors; D000077156:Gefitinib
keywords: (99m)Tc; Epidermal growth factor receptor; Gefitinib; Molecular imaging