Biodistribution of 99mTc‐sunitinib as a potential radiotracer for tumor hypoxia imaging. (22nd May 2013)

• Record Type: Journal Article
• Authors: Sakr, T. M.; El‐Safoury, D. M.; Awad, Gehanne A. S.; Motaleb, M. A.
• Is Part Of: Journal of labelled compounds & radiopharmaceuticals. Volume 56:Number 8(2013)
• Page Start: 392
• Page End: 395
• Publication Date: 2013-05-22
• Subjects: Tracers (Chemistry) -- Periodicals; Radiopharmaceuticals -- Periodicals; 615.8424
• DOI: 10.1002/jlcr.3060
• Languages: English
• ISSNs: 0362-4803

Abstract

<abstract abstract-type="main"> <title> <x xml:space="preserve">Abstract</x> </title> <p>Tyrosine kinases are groups of enzymes, which are over‐expressed in solid tumor cells, representing good targets for different drugs such as sunitinib (<italic>N</italic>‐[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 ^99mTc‐sunitinib radiotracer and to study its tumor binding specificity as a novel selective radiopharmaceutical for tumor hypoxia imaging. The <italic>in vivo</italic> biodistribution of ^99mTc‐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 ^99mTc‐sunitinib is ready to go through the clinical trials as a potential selective radiotracer able to image tumor hypoxia.</p> </abstract>