[Phase I clinical trial of a new myocardial imaging agent, 99mTc-PPN1011]

A new myocardial imaging agent, 99mTc-1,2-bis[bis(2-ethoxyethyl) phosphino]ethane (99mTc-PPN1011) was administered to healthy male volunteers to evaluate its safety and kinetics. No significant drug-related events were observed. After intravenous injection, blood clearance was rapid. Prompt heart uptake (1.8% of the injected dose after 5 minutes) was followed by relatively slow wash-out (1.0% remained after 3 hours). Liver and lung uptake was observed but the clearance was more rapid than in the heart. 4.7-24.0% of the injected 99mTc-PPN1011 was excreted into urine until 4 hours after injection. 99mTc-PPN1011 also seemed to be excreted through hepato-biliary system. Excellent and low-background myocardial images were obtained using either SPECT or planar imaging. We conclude that 99mTc-PPN1011 could be useful for myocardial perfusion imaging.