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European Journal of Nuclear Medicine and Molecular Imaging

Published in:

01-03-2010 | Original Article

Human biodistribution and radiation dosimetry of ¹¹C-(R)-PK11195, the prototypic PET ligand to image inflammation

Authors: Jussi Hirvonen, Anne Roivainen, Jere Virta, Semi Helin, Kjell Någren, Juha O. Rinne

Published in: European Journal of Nuclear Medicine and Molecular Imaging | Issue 3/2010

Abstract

Purpose

The positron emission tomography (PET) radiotracer ¹¹C-(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 ¹¹C-(R)-PK11195 in humans is not known. To examine this, we performed dynamic whole-body imaging with PET and ¹¹C-(R)-PK11195 in healthy humans.

Methods

Five healthy male volunteers were scanned with PET and ¹¹C-(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 ¹¹C-(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 µSv/MBq according to International Commission on Radiological Protection (ICRP) Publication 60 and 5.1 µSv/MBq according to ICRP Publication 103, and the highest equivalent organ doses were observed in the kidneys (14.0 µSv/MBq), spleen (12.5 µSv/MBq) and small intestine (12.2 µSv/MBq).

Conclusion

Imaging of TSPO with PET using ¹¹C-(R)-PK11195 is associated with modest radiation exposure, similar in magnitude to most other ¹¹C-labelled PET tracers, suggesting feasibility of ¹¹C-(R)-PK11195 imaging in clinical human studies involving multiple scans in the same subjects per year.

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Title: Human biodistribution and radiation dosimetry of 11C-(R)-PK11195, the prototypic PET ligand to image inflammation
Authors: Jussi Hirvonen
Anne Roivainen
Jere Virta
Semi Helin
Kjell Någren
Juha O. Rinne
Publication date: 01-03-2010
Publisher: Springer-Verlag
Published in: European Journal of Nuclear Medicine and Molecular Imaging / Issue 3/2010
Print ISSN: 1619-7070
Electronic ISSN: 1619-7089
DOI: https://doi.org/10.1007/s00259-009-1298-3

At a glance: The STEP trials

Springer Medicine

Human biodistribution and radiation dosimetry of ¹¹C-(R)-PK11195, the prototypic PET ligand to image inflammation

Abstract

Purpose

Methods

Results

Conclusion

At a glance: The STEP trials

Springer Medicine

Abstract

Purpose

Methods

Results

Conclusion

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