Literature DB >> 33891195

Human biodistribution and dosimetry of [11C]-UCB-J, a PET radiotracer for imaging synaptic density.

Koen Van Laere1,2, Michel Koole3, Christopher Cawthorne1, Paul Maguire4, Joel Mercier4, David Sciberras4, Kim Serdons2, Guy Bormans5, Jan de Hoon6.   

Abstract

RATIONALE: [11C]-UCB-J is an emerging tool for the noninvasive measurement of synaptic vesicle density in vivo. Here, we report human biodistribution and dosimetry estimates derived from sequential whole-body PET using two versions of the OLINDA dosimetry program.
METHODS: Sequential whole-body PET scans were performed in 3 healthy subjects for 2 h after injection of 254 ± 77 MBq [11C]-UCB-J. Volumes of interest were drawn over relevant source organs to generate time-activity curves and calculate time-integrated activity coefficients, with effective dose coefficients calculated using OLINDA 2.1 and compared to values derived from OLINDA 1.1 and those recently reported in the literature.
RESULTS: [11C]-UCB-J administration was safe and showed mixed renal and hepatobiliary clearance, with largest organ absorbed dose coefficients for the urinary bladder wall and small intestine (21.7 and 23.5 μGy/MBq, respectively). The average (±SD) effective dose coefficient was 5.4 ± 0.7 and 5.1 ± 0.8 μSv/MBq for OLINDA versions 1.1 and 2.1 respectively. Doses were lower than previously reported in the literature using either software version.
CONCLUSIONS: A single IV administration of 370 MBq [11C]-UCB-J corresponds to an effective dose of less than 2.0 mSv, enabling multiple PET examinations to be carried out in the same subject. TRIAL REGISTRATION: EudraCT number: 2016-001190-32. Registered 16 March 2016, no URL available for phase 1 trials.

Entities:  

Keywords:  Human biodistribution; OLINDA; Radiation dosimetry; Synaptic density; [11C]-UCB-J

Year:  2021        PMID: 33891195     DOI: 10.1186/s40658-021-00384-5

Source DB:  PubMed          Journal:  EJNMMI Phys        ISSN: 2197-7364


  30 in total

1.  Quantifying SV2A density and drug occupancy in the human brain using [11C]UCB-J PET imaging and subcortical white matter as reference tissue.

Authors:  Michel Koole; June van Aalst; Martijn Devrome; Nathalie Mertens; Kim Serdons; Brigitte Lacroix; Joel Mercier; David Sciberras; Paul Maguire; Koen Van Laere
Journal:  Eur J Nucl Med Mol Imaging       Date:  2018-08-18       Impact factor: 9.236

2.  RADAR Dose Estimate Report: A Compendium of Radiopharmaceutical Dose Estimates Based on OLINDA/EXM Version 2.0.

Authors:  Michael G Stabin; Jeffry A Siegel
Journal:  J Nucl Med       Date:  2017-09-08       Impact factor: 10.057

Review 3.  Discovery and development of SV2A PET tracers: Potential for imaging synaptic density and clinical applications.

Authors:  Joel Mercier; Laurent Provins; Anne Valade
Journal:  Drug Discov Today Technol       Date:  2017-12-01

4.  Kinetic evaluation and test-retest reproducibility of [11C]UCB-J, a novel radioligand for positron emission tomography imaging of synaptic vesicle glycoprotein 2A in humans.

Authors:  Sjoerd J Finnema; Nabeel B Nabulsi; Joël Mercier; Shu-Fei Lin; Ming-Kai Chen; David Matuskey; Jean-Dominique Gallezot; Shannan Henry; Jonas Hannestad; Yiyun Huang; Richard E Carson
Journal:  J Cereb Blood Flow Metab       Date:  2017-08-09       Impact factor: 6.200

Review 5.  PET imaging of synaptic density: A new tool for investigation of neuropsychiatric diseases.

Authors:  Zhengxin Cai; Songye Li; David Matuskey; Nabeel Nabulsi; Yiyun Huang
Journal:  Neurosci Lett       Date:  2018-07-31       Impact factor: 3.046

6.  Differential expression of synaptic vesicle protein 2 (SV2) isoforms.

Authors:  S M Bajjalieh; G D Frantz; J M Weimann; S K McConnell; R H Scheller
Journal:  J Neurosci       Date:  1994-09       Impact factor: 6.167

7.  SV2, a brain synaptic vesicle protein homologous to bacterial transporters.

Authors:  S M Bajjalieh; K Peterson; R Shinghal; R H Scheller
Journal:  Science       Date:  1992-08-28       Impact factor: 47.728

8.  The synaptic vesicle protein SV2A is the binding site for the antiepileptic drug levetiracetam.

Authors:  Berkley A Lynch; Nathalie Lambeng; Karl Nocka; Patricia Kensel-Hammes; Sandra M Bajjalieh; Alain Matagne; Bruno Fuks
Journal:  Proc Natl Acad Sci U S A       Date:  2004-06-21       Impact factor: 11.205

9.  Levetiracetam reverses synaptic deficits produced by overexpression of SV2A.

Authors:  Amy Nowack; Erik B Malarkey; Jia Yao; Adam Bleckert; Jessica Hill; Sandra M Bajjalieh
Journal:  PLoS One       Date:  2011-12-29       Impact factor: 3.240

10.  Human adult and adolescent biodistribution and dosimetry of the synaptic vesicle glycoprotein 2A radioligand 11C-UCB-J.

Authors:  Jason Bini; Daniel Holden; Kathryn Fontaine; Tim Mulnix; Yihuan Lu; David Matuskey; Jim Ropchan; Nabeel Nabulsi; Yiyun Huang; Richard E Carson
Journal:  EJNMMI Res       Date:  2020-07-14       Impact factor: 3.138

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