Radiosynthesis, radiochemical, and biological characterization of 177 Lu-labeled diethylenetriamine penta-acetic acid.

Diethylenetriamine penta-acetic acid (DTPA), when complexed with a gamma (gamma)-emitter radioisotope like Tc-99m, is used for renal function diagnosis and many other diagnostic applications. The main aim of this study was to develop a novel and versatile single-step methodology for the synthesis of a new Lu-177-labeled radiopharmaceutical with high radiochemical yield, which can be used for diagnostic purposes and therapeutic purposes also. The single and well-defined Lu-177-DTPA complex was radiochemically characterized by paper chromatography, thin-layer chromatography, high-performance liquid chromatography, and electrophoresis techniques. Dependence of the labeling yield of Lu-177-DTPA complex on different factors was studied in detail. Biological evaluation was also performed in a normal rabbit by developing images under a gamma camera at various time intervals. More than 99% labeling yield was obtained by reacting DTPA with Lu-177 at specific conditions (pH 7.0, 15 minutes reaction time at 100 degrees C). Lu-177-DTPA complex showed high stability both at room temperature and in vitro. Biodistribution studies in normal mice indicated the fractional renal uptake of intravenously administered Lu-177-DTPA complex, which reached in the kidneys within 2-3 minutes. Scintigraphy showed rapid clearance from the body. Based on these results, we propose that Lu-177-DTPA complex might be used as an ideal candidate for functional evaluation of kidneys and the urinary tract, especially when needed to be transported to long-range consumer sites, because of its suitable half-life.