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The preparation and preliminary biological evaluation of a metronidazole-BFCA (bifunctional chelating agent) conjugate labeled with  177 Lu is reported. Metronidazole, a well known hypoxia marker has been suitably derivatized and coupled with a polyazamacrocyclic BFCA, namely, para-aminobenzyl-1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid ( p -amino-benzyl-DOTA).  177 Lu, which is presently being considered as one of the pivotal radionuclides for targeted therapy was produced in adequate specific activity (∼185 TBq/g) and high radionuclidic purity (99.99%) by irradiating enriched (60.6%  176 Lu) Lu 2 O 3  target at a moderate thermal neutron flux of 3×10 13  n/cm 2 /s. The metronidazole-BFCA conjugate was radiolabeled with  177 Lu in high radiochemical purity (97%). Preliminary biodistribution studies carried out in Swiss mice bearing fibrosarcoma tumors revealed good tumor uptake (1.30% ID/g at 30 min post-injection) with rapid renal clearance (94.48% ID at 30 min post-injection) and significant tumor to blood (28.00 at 3 h post-injection) and tumor to muscle (14.00 at 3 h post-injection) ratios.

Preparation and preliminary biological evaluation of a 177 Lu labeled nitroimidazole derivative for possible use in targeted tumor therapy