BARC/PUB/2017/0125

 
 

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

 
     
 
Author(s)

Pandey, U.; Gamre, N.; Lohar, S. P.; Dash, A.
(RPhD)

Source

Applied Radiation and Isotopes, 2017. Vol. 127: pp. 1-6

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 177Lu. While 177Lu-CHX-A’’-DTPA-NCS could be obtained in high yields at equimolar ratios of lutetium to CHX-A’’-DTPA-NCS,>95% yield of 177Lu-NOTA-NCS could be achieved at 1:2 M ratio of lutetium to NOTA-NCS. Trace metals reduced the yields of 177Lu-NOTA-NCS significantly as compared to 177Lu-CHX-A’’-DTPA-NCS. In vitro stability of 177Lu-CHX-A’’-DTPA-NCS was also superior to 177Lu-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 177Lu radiopharmaceuticals.

 
 
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