Pharmacokinetics and Biodistribution of Tc-99m N-MPO in Healthy Human Volunteers

作者：Gao, Shi; Zhao, Guoqing; Wen, Qiang; Bai, Lin; Chen, Bin; Ji, Tiefeng; Ji, Bin; Ma, Qingjie^*

来源：Clinical Nuclear Medicine, 2014, 39(1): E14-E19.

• Tc-99m N-MPO
• myocardial perfusion imaging
• biodistribution
• pharmacokinetics
• radiation dosimetry

Purpose: Tc-99m N-MPO ([Tc-99m N(MPO)(PNP5)](+): HMPO = 2-mercaptopyridine N-oxide, and PNP5 = N-ethoxyethyl-N,N-bis[2-(bis(3-methoxypropyl)phosphino) ethyl] amine) is a new Tc-99m radiotracer useful for myocardial perfusion imaging. This study was designed to determine its pharmacokinetics and biodistribution in healthy volunteers.
Patients and Methods: Ten healthy volunteers were involved in this study. Each subject was administered approximately 925 MBq of Tc-99m N-MPO under rest or stress conditions (n = 5 per group). Whole-body planar images were obtained at 10, 30, 60, 240, and 1440 minutes after injection. Organ uptake was quantified by region-of-interest analysis. The blood clearance and urine excretion kinetics were determined by collecting blood and urine samples at different time points.
Results: Tc-99m N-MPO showed significant accumulation in myocardium with prolonged retention. At rest, its percentage of injected dose (% ID) uptake in the heart, lungs, and liver at 10 minutes after injection was 2.47% (0.64%), 1.84% (0.64%), and 20.88% (5.23%), respectively. The liver uptake decreased to 6.79% ID (1.60% ID) at 60 minutes after injection and 4.50% ID (1.86% ID) at 240 minutes after injection. Under stress conditions, the heart uptake was slightly increased (2.57% ID [0.21% ID]). The rapid liver clearance led to favorable heart-to-liver ratios, reaching values of 0.27% ID (0.07% ID) under rest condition and 0.28% ID (0.05% ID) under stress condition at 60 minutes after injection.
Conclusions: Tc-99m N-MPO demonstrates a highly favorable biodistribution in humans. The high heart uptake and the fast liver washout of Tc-99m N-MPO will allow SPECT images of the left ventricle to be acquired as early as 10 minutes after injection.

• 出版日期2014-1
• 单位吉林大学