Biodistribution and Radiation Dosimetry of 18 F-FTC-146 in Humans.

Autor:	Hjørnevik T; Department of Radiology, Stanford University, Stanford, California.; Department of Diagnostic Physics, Oslo University Hospital, Oslo, Norway.; The Norwegian Medical Cyclotron Centre, Oslo, Norway., Cipriano PW; Department of Radiology, Stanford University, Stanford, California., Shen B; Department of Radiology, Stanford University, Stanford, California., Park JH; Department of Radiology, Stanford University, Stanford, California., Gulaka P; Department of Radiology, Stanford University, Stanford, California., Holley D; Department of Radiology, Stanford University, Stanford, California., Gandhi H; Department of Radiology, Stanford University, Stanford, California., Yoon D; Department of Radiology, Stanford University, Stanford, California., Mittra ES; Department of Radiology, Stanford University, Stanford, California., Zaharchuk G; Department of Radiology, Stanford University, Stanford, California., Gambhir SS; Department of Radiology, Stanford University, Stanford, California., McCurdy CR; Department of Medicinal Chemistry, University of Florida, Gainesville, Florida; and.; UF Translational Drug Development Core, University of Florida, Gainesville, Florida., Chin FT; Department of Radiology, Stanford University, Stanford, California chinf@stanford.edu biswal@stanford.edu., Biswal S; Department of Radiology, Stanford University, Stanford, California chinf@stanford.edu biswal@stanford.edu.
Jazyk:	angličtina
Zdroj:	Journal of nuclear medicine : official publication, Society of Nuclear Medicine [J Nucl Med] 2017 Dec; Vol. 58 (12), pp. 2004-2009. Date of Electronic Publication: 2017 Jun 01.
DOI:	10.2967/jnumed.117.192641
Abstrakt:	The purpose of this study was to assess safety, biodistribution, and radiation dosimetry in humans for the highly selective σ-1 receptor PET agent 18 F-6-(3-fluoropropyl)-3-(2-(azepan-1-yl)ethyl)benzo[ d ]thiazol-2(3H)-one ( 18 F-FTC-146). Methods: Ten healthy volunteers (5 women, 5 men; age ± SD, 34.3 ± 6.5 y) were recruited, and written informed consent was obtained from all participants. Series of whole-body PET/MRI examinations were acquired for up to 3 h after injection (357.2 ± 48.8 MBq). Blood samples were collected, and standard vital signs (heart rate, pulse oximetry, and body temperature) were monitored at regular intervals. Regions of interest were delineated, time-activity curves were calculated, and organ uptake and dosimetry were estimated. Results: All subjects tolerated the PET/MRI examination well, and no adverse reactions to 18 F-FTC-146 were reported. High accumulation of 18 F-FTC-146 was observed in σ-1 receptor-dense organs such as the pancreas and spleen, moderate uptake in the brain and myocardium, and low uptake in bone and muscle. High uptake was also observed in the kidneys and bladder, indicating renal tracer clearance. The effective dose of 18 F-FTC-146 was 0.0259 ± 0.0034 mSv/MBq (range, 0.0215-0.0301 mSv/MBq). Conclusion: First-in-human studies with clinical-grade 18 F-FTC-146 were successful. Injection of 18 F-FTC-146 is safe, and absorbed doses are acceptable. The potential of 18 F-FTC-146 as an imaging agent for a variety of neuroinflammatory diseases is currently under investigation. (© 2017 by the Society of Nuclear Medicine and Molecular Imaging.)
Databáze:	MEDLINE
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