Imaging prostate cancer (PCa) with [99mTc(CO)3]finasteride dithiocarbamate

This investigation aimed to modify finasteride ( 1 ) to finasteride dithiocarbamate ( 2 ) for subsequent synthesis of the rhenium analogue ( 3 ) and [^99mTc]tricarbonyl complexes ( 4 ), to assess its prostate cancer (PCa) targeting potential in a rat model. To validate the identity of ( 4) , reference ( 3) has been synthesized by using fac‐[Net₄]₂[ReBr₃(CO)₃] precursor and characterized by ¹H‐NMR, ¹³C‐NMR, ESI‐MS, and elemental analysis. The analogue ( 4) was synthesized by using fac‐[^99mTc(H₂O)₃(CO)₃]⁺ precursor, and its structure was confirmed by comparative HPLC by using ( 3) as a reference. Further, the suitability of ( 4) as a PCa imaging agent was investigated in vitro and in vivo. At room temperature, ( 4) had ≥99% radiochemical purity and remained ≥84% stable in serum. In preclinical studies, biodistribution of ( 4) in histopathologically established rat model showed adequately high in vivo uptake in the prostate attracting the possibility of using it for noninvasive imaging of PCa.