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

Pardeep Kumar; Baljinder Singh; Anchal Ghai; Krishna Chuttani; Devinder Dhawan; Bhagwant R. Mittal; Anil K. Mishra

doi:10.1016/j.apradiso.2015.02.007

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

Pardeep Kumar, Baljinder Singh, Anchal Ghai, Krishna Chuttani, Devinder Dhawan, Bhagwant R. Mittal, Anil K. Mishra

Research output: Contribution to journal › Article › peer-review

4 Scopus citations

Abstract

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 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.

Original language	English (US)
Pages (from-to)	41-45
Number of pages	5
Journal	Applied Radiation and Isotopes
Volume	99
DOIs	https://doi.org/10.1016/j.apradiso.2015.02.007
State	Published - May 1 2015
Externally published	Yes

Keywords

Epidermal growth factor receptor
Gefitinib
Molecular imaging
Tc

ASJC Scopus subject areas

Radiation

Access to Document

10.1016/j.apradiso.2015.02.007

Cite this

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title = "Preclinical evaluation of 99mTc 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 99mTc 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.",

keywords = "Epidermal growth factor receptor, Gefitinib, Molecular imaging, Tc",

author = "Pardeep Kumar and Baljinder Singh and Anchal Ghai and Krishna Chuttani and Devinder Dhawan and Mittal, {Bhagwant R.} and Mishra, {Anil K.}",

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AU - Kumar, Pardeep

AU - Singh, Baljinder

AU - Ghai, Anchal

AU - Chuttani, Krishna

AU - Dhawan, Devinder

AU - Mittal, Bhagwant R.

AU - Mishra, Anil K.

PY - 2015/5/1

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AB - 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 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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