Preliminary biological evaluation of novel (99m)Tc-Cys-annexin A5 as a apoptosis imaging agent.

A novel annexin A5 derivative (cys-annexin A5) with a single cysteine residue at its C-terminal has been developed and successfully labeled in high labeling yield with (99m)Tc by a ligand exchange reaction. Like the 1st generation (99m)Tc-HYNIC-annexin A5, the novel (99m)Tc-cys-annexin A5 derivative shows in normal mice mainly renal and, to a lesser extent, hepatobiliary excretion. In rat models of hepatic apoptosis there was 283% increase in hepatic uptake of (99m)Tc-cys-annexin A5 as compared to normal mice. The results indicate that the novel (99m)Tc-cys-annexin A5 is a potential apoptosis imaging agent.