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~(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.
~ (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. 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 identified plants 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. whole body imaging showed high radioact (99m) Tc-3PRGD_2 exhibited good pharmacokinetic properties and little radiation (3.50 × 10 -2 mSv / MBq) burden.This study showed that ~ (99m) Tc-3PRGD_2 would be a safe and attractive SPECT agent in clinic applications.