A systematic study on the utility of CHX-A’’-DTPA-NCS and NOTA-NCS as bifunctional chelators for 177Lu radiopharmaceuticals

Abstract This paper describes the evaluation of [(R)-2-Amino-3-(4-isothiocyanatophenyl)propyl]-trans-(S,S)-cyclohexane-1,2-diamine-pentaacetic acid (CHX-A’’-DTPA-NCS) and 2-S-(4-isothiocyanatobenzyl)−1,4,7-triazacyclononane-1,4,7-triacetic acid (NOTA-NCS) as bifunctional chelators for 177 Lu. While 177 Lu-CHX-A’’-DTPA-NCS could be obtained in high yields at equimolar ratios of lutetium to CHX-A’’-DTPA-NCS, >95% yield of 177 Lu-NOTA-NCS could be achieved at 1:2 M ratio of lutetium to NOTA-NCS. Trace metals reduced the yields of 177 Lu-NOTA-NCS significantly as compared to 177 Lu-CHX-A’’-DTPA-NCS. In vitro stability of 177 Lu-CHX-A’’-DTPA-NCS was also superior to 177 Lu-NOTA-NCS. It could be concluded from this study that among the two chelators evaluated, CHX-A’’-DTPA-NCS is more appropriate for preparation of 177 Lu radiopharmaceuticals.