Biodistribution of super(99m)Tc-sunitinib as a potential radiotracer for tumor hypoxia imaging

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- c a rboxamide). The aim of this work was to design and synthesize super(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 super(99m)Tc-sunitinib in tumor bearing mice showed high target/non-target (T/NT) ratio (T/NT~3 at 60min post injection). This preclinical high biological accumulation in tumor cells suggests that super(99m)Tc-sunitinib is ready to go through the clinical trials as a potential selective radiotracer able to image tumor hypoxia. super(99m)Tc-sunitinib is reported to be prepared with radiochemical yield of~90 plus or minus 2% and stability up to 8h. The preclinical in vivo biodistribution of super(99m)Tc-sunitinib in tumor bearing mice showed high target/non-target ratio (~3 at 60min post injection). This research article could introduce super(99m)Tc-sunitinib as a selective potential radiopharmaceutical for tumor hypoxia imaging.