Nuclear Science and Techniques

《核技术》(英文版) ISSN 1001-8042 CN 31-1559/TL     2019 Impact factor 1.556

Nuclear Science and Techniques ›› 2012, Vol. 23 ›› Issue (6): 349-354 doi: 10.13538/j.1001-8042/nst.23.349-354


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

CHENG Guanghui; GAO Shi; JI Tiefeng; MA Qingjie; JIA Bing; CHEN Zuowei; WANG Qing;   

  1. China-Japan Union Hospital,Jilin University; Medical Isotopes Research Center,Peking University; Department of Nuclear Medicine,People's Hospital of Shenzhen;
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CHENG Guanghui, GAO Shi, JI Tiefeng, MA Qingjie, JIA Bing, CHEN Zuowei, WANG Qing, . Pharmacokinetics and radiation dosimetry of ~(99m)Tc-3PRGD_2 in healthy individuals:A pilot study.Nuclear Science and Techniques, 2012, 23(6): 349-354     doi: 10.13538/j.1001-8042/nst.23.349-354


~(99m)Tc-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.

Key words: 99mTc-3PRGD2, Integrin αvβ3, Pharmacokinetic, Dosimetry