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Biodistribution of 99m Tc‐sunitinib as a potential radiotracer for tumor hypoxia imaging
Author(s) -
Sakr T. M.,
ElSafoury D. M.,
Awad Gehanne A. S.,
Motaleb M. A.
Publication year - 2013
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.3060
Subject(s) - biodistribution , sunitinib , chemistry , tumor hypoxia , in vivo , hypoxia (environmental) , pharmacology , cancer research , radiochemistry , in vitro , medicine , biochemistry , oxygen , cancer , biology , microbiology and biotechnology , organic chemistry , radiation therapy
Tyrosine kinases are groups of enzymes, which are over‐expressed in solid tumor cells, representing good targets for different drugs such as sunitinib ( N ‐[2‐(diethylamino)ethyl]‐5‐{[(3Z)‐5‐fluoro‐2‐oxo‐2,3‐dihydro‐1H‐indol‐3‐ylidene]methyl}‐2,4‐dimethyl‐1H‐pyrrole‐3‐carboxamide). The aim of this work was to design and synthesize 99m Tc‐sunitinib radiotracer and to study its tumor binding specificity as a novel selective radiopharmaceutical for tumor hypoxia imaging. The in vivo biodistribution of 99m Tc‐sunitinib in tumor bearing mice showed high target/non‐target (T/NT) ratio (T/NT ~ 3 at 60 min post injection). This preclinical high biological accumulation in tumor cells suggests that 99m Tc‐sunitinib is ready to go through the clinical trials as a potential selective radiotracer able to image tumor hypoxia.