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  • Title: Human biodistribution and radiation dosimetry of 11C-(R)-PK11195, the prototypic PET ligand to image inflammation.
    Author: Hirvonen J, Roivainen A, Virta J, Helin S, Någren K, Rinne JO.
    Journal: Eur J Nucl Med Mol Imaging; 2010 Mar; 37(3):606-12. PubMed ID: 19862517.
    Abstract:
    PURPOSE: The positron emission tomography (PET) radiotracer (11)C-(R)-PK11195 allows the in vivo imaging in humans of the translocator protein 18 kDa (TSPO), previously called peripheral benzodiazepine receptor (PBR), a marker of inflammation. Despite its widespread use, the radiation burden associated with (11)C-(R)-PK11195 in humans is not known. To examine this, we performed dynamic whole-body imaging with PET and (11)C-(R)-PK11195 in healthy humans. METHODS: Five healthy male volunteers were scanned with PET and (11)C-(R)-PK11195, using a dynamic whole-body imaging protocol. An organ-specific method was used to measure accumulated radioactivity in source organs, and residence times were calculated as areas under the curve of time-activity curves expressed as percentage of injected radioactivity. Residence times were used as input for OLINDA/EXM 1.0 software to model the equivalent organ doses and the effective dose for the 70-kg man. RESULTS: After intravenous injection of (11)C-(R)-PK11195, radioactivity accumulated in organs rich in TSPO as well as routes of excretion: the hepatobiliary system and the urine. The mean effective dose was 4.8 microSv/MBq according to International Commission on Radiological Protection (ICRP) Publication 60 and 5.1 microSv/MBq according to ICRP Publication 103, and the highest equivalent organ doses were observed in the kidneys (14.0 microSv/MBq), spleen (12.5 microSv/MBq) and small intestine (12.2 microSv/MBq). CONCLUSION: Imaging of TSPO with PET using (11)C-(R)-PK11195 is associated with modest radiation exposure, similar in magnitude to most other (11)C-labelled PET tracers, suggesting feasibility of (11)C-(R)-PK11195 imaging in clinical human studies involving multiple scans in the same subjects per year.
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