Pharmacokinetics and radiation dosimetry of ^(99m)Tc-3PRGD_2 in healthy individuals:A pilot study  

作　　者：CHENG Guanghui GAO Shi JI Tiefeng MA Qingjie JIA Bing CHEN Zuowei WANG Qing 

机构地区：[1]China-Japan Union Hospital,Jilin University [2]Medical Isotopes Research Center,Peking University [3]Department of Nuclear Medicine,People's Hospital of Shenzhen

出　　处：《Nuclear Science and Techniques》2012年第6期349-354,共6页核技术（英文）

基　　金：Supported by the National Natural Science Foundation of China(NSFC) projects(no.81271606);the Research Fund of Science and Technology Department of Jilin Province(no.201015185 and no.201201041);the Research Fund of Shenzhen Sci-tech Department of Guangdong Province(no.201102154)

摘　　要：99mTc-3PRGD2 is a new SPECT radiotracer for several tumor imaging with high uptake where integrinαvβ3 is highly expressed.This pilot study was to assess the safety,biodistribution and radiation dosimetry of 9,mTc-3PRGD2 in healthy volunteers.The 10 healthy male volunteers were injected with 99mTc-3PRGD2（786.7±55.8 MBq,19.1-24.2 mCi）.Baseline measurements of vital signs,laboratory safety tests and 12-lead electrocardiogram were recorded before and after injection.Blood and urine samples were collected and radiation counts were obtained at various time points.Whole-body scans and ROIs of identified organs were used for visual analysis and estimating the radiation dosimetry.No adverse reactions were found during the study.99mTc-3PRGD2 exhibited a rapid clearance from the blood with less than 45%of the initial dosage at 10 min after injection and gradual increasing radioactivity in urine with（52.9±6）%of original dose at 1440 min.The whole-body imaging showed high radioactive accumulation in bladder.And the highest 99mTc-3PRGD2 uptake was found in the kidneys(3.50×10-2 mSv/MBq).The 99mTc-3PRGD2 exhibited good pharmacokinetic properties and little radiation burden.This study showed that 99mTc-3PRGD2 would be a safe and attractive SPECT agent in clinic applications.99mTc-3PRGD_2 is a new SPECT radiotracer for several tumor imaging with high uptake where integrinα_vβ_3 is highly expressed.This pilot study was to assess the safety,biodistribution and radiation dosimetry of 9,mTc-3PRGD2 in healthy volunteers.The 10 healthy male volunteers were injected with ^（99m）Tc-3PRGD_2（786.7±55.8 MBq,19.1-24.2 mCi）.Baseline measurements of vital signs,laboratory safety tests and 12-lead electrocardiogram were recorded before and after injection.Blood and urine samples were collected and radiation counts were obtained at various time points.Whole-body scans and ROIs of identified organs were used for visual analysis and estimating the radiation dosimetry.No adverse reactions were found during the study.^（99m）Tc-3PRGD_2 exhibited a rapid clearance from the blood with less than 45%of the initial dosage at 10 min after injection and gradual increasing radioactivity in urine with（52.9±6）%of original dose at 1440 min.The whole-body imaging showed high radioactive accumulation in bladder.And the highest ^（99m）Tc-3PRGD_2 uptake was found in the kidneys（3.50×10^（-2） mSv/MBq）.The ^（99m）Tc-3PRGD_2 exhibited good pharmacokinetic properties and little radiation burden.This study showed that ^（99m）Tc-3PRGD_2 would be a safe and attractive SPECT agent in clinic applications.

关 键 词：安全试验 健康人 药代动力学 辐射剂量 高放射性 SPECT 可视化分析 投资回报率 

分 类 号：R73-3[医药卫生—肿瘤]