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.
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)
