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

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 Lu. While Lu-CHX-A''-DTPA-NCS could be obtained in high yields at equimolar ratios of lutetium to CHX-A''-DTPA-NCS, >95% yield of Lu-NOTA-NCS could be achieved at 1:2M ratio of lutetium to NOTA-NCS. Trace metals reduced the yields of Lu-NOTA-NCS significantly as compared to Lu-CHX-A''-DTPA-NCS. In vitro stability of Lu-CHX-A''-DTPA-NCS was also superior to 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 Lu radiopharmaceuticals.