title: Biodistribution of 99mTc-sunitinib as a potential radiotracer for tumor hypoxia imaging.
abstract: 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.
authors.affiliation: Radioactive Isotopes and Generator Department, Hot Labs Center, Atomic Energy Authority, PO Box 13759, Cairo, Egypt.
authors.forename: T M
authors.initials: TM
authors.lastname: Sakr
authors.forename: D M
authors.initials: DM
authors.lastname: El-Safoury
authors.forename: Gehanne A S
authors.initials: GA
authors.lastname: Awad
authors.forename: M A
authors.initials: MA
authors.lastname: Motaleb
mesh_terms: D000818:Animals; D015687:Cell Hypoxia; D007211:Indoles / Q000138:chemical synthesis / Q000737:chemistry / Q000493:pharmacokinetics*; D007553:Isotope Labeling; D051379:Mice; D009374:Neoplasms, Experimental / Q000000981:diagnostic imaging*; D015609:Organotechnetium Compounds / Q000138:chemical synthesis / Q000493:pharmacokinetics*; D011758:Pyrroles / Q000737:chemistry; D019275:Radiopharmaceuticals / Q000138:chemical synthesis / Q000493:pharmacokinetics*; D000077210:Sunitinib; D015899:Tomography, Emission-Computed, Single-Photon
chemical_list: D007211:Indoles; D015609:Organotechnetium Compounds; D011758:Pyrroles; D019275:Radiopharmaceuticals; C000589728:technetium 99m N-(2-(diethylamino)ethyl)-5-((5-fluoro-2-oxo-2,3-dihydro-1H-indol-3-ylidene)methyl)-2,4-dimethyl-1H-pyrrole-3-carboxamide; D000077210:Sunitinib
keywords: SPECT; Tumor; hypoxia; imaging; sunitinib; technetium-99 m