Internal dose assessment of (-)-18F-flubatine, comparing animal model datasets of mice and piglets with first-in-human results

Journal of Nuclear Medicine

Volumn 55, Issue 11, 2014, Pages 1885-1892

  Sattler, Bernhard ^a   Kranz, Mathias ^a,b   Starke, Alexander ^c   Wilke, Stephan ^a   Donat, Cornelius K ^c   Deuther Conrad, Winnie ^c   Patt, Marianne ^a   Schildan, Andreas ^a   Patt, Jörg ^a   Smits, René ^d   Hoepping, Alexander ^d   Schoenknecht, Peter ^a   Steinbach, Jörg ^b   Brust, Peter ^c   Sabri, Osama ^a  

^a UNIVERSITY HOSPITAL LEIPZIG   (Germany)

^b INSTITUTE OF ION BEAM PHYSICS AND MATERIALS RESEARCH   (Germany)

^c Henriettenstiftung   (Germany)

^d ABX Advanced Biochemical Compounds   (Germany)

Author keywords

( ) 18F flubatine; A4 2; Nicotinic receptors; Positron emission tomography; Radiation dosimetry

Indexed keywords

FLUBATINE F 18; RADIOPHARMACEUTICAL AGENT; UNCLASSIFIED DRUG; BENZAMIDE DERIVATIVE; FLUORONORCHLOROEPIBATIDINE; FUSED HETEROCYCLIC RINGS; NICOTINIC RECEPTOR;

ABSENCE OF SIDE EFFECTS; ANIMAL TISSUE; ARTICLE; BLADDER; CD-1 MOUSE; COMPARATIVE STUDY; COMPUTER PROGRAM; CONTROLLED STUDY; DOSE RESPONSE; DOSIMETRY; FEMALE; GAMMA COUNTER; HUMAN; KIDNEY; LIVER; MALE; MASS; MOUSE; NONHUMAN; PET-CT SCANNER; PIGLET; POSITRON EMISSION TOMOGRAPHY; RADIATION DOSE; RADIATION DOSE DISTRIBUTION; RADIOACTIVITY; WHOLE BODY IMAGING; ANIMAL; CALIBRATION; CHEMISTRY; DIAGNOSTIC USE; FACTUAL DATABASE; MULTIMODAL IMAGING; PROCEDURES; RADIOMETRY; SCINTISCANNING; SWINE; TISSUE DISTRIBUTION;

ANIMALS; BENZAMIDES; BICYCLO COMPOUNDS, HETEROCYCLIC; CALIBRATION; DATABASES, FACTUAL; FEMALE; HUMANS; MALE; MICE; MULTIMODAL IMAGING; POSITRON-EMISSION TOMOGRAPHY; RADIATION DOSAGE; RADIOMETRY; RADIOPHARMACEUTICALS; RECEPTORS, NICOTINIC; SWINE; TISSUE DISTRIBUTION; URINARY BLADDER; WHOLE BODY IMAGING;

EID: 84910627078     PISSN: 01615505     EISSN: 2159662X     Source Type: Journal    
DOI: 10.2967/jnumed.114.137059     Document Type: Article

References (27)

1. Quik M, Wonnacott S. a6b2 and a4b2 nicotinic acetylcholine receptors as drug targets for Parkinson's disease. Pharmacol Rev. 2011;63:938-966.
2. Brasíc JR, Cascella N, Kumar A, et al. Positron emission tomography experience with 2-18F-fluoro-3-(2(S)-Azetidinylmethoxy)pyridine (2-18F-fa) in the living human brain of smokers with paranoid schizophrenia. Synapse. 2012; 66:352-368.
3. Wu J, Ishikawa M, Zhang J, Hashimoto K. Brain imaging of nicotinic receptors in Alzheimer's disease. Int J Alzheimers Dis. 2010;2010:548913.
4. Fischer S, Hiller A, Smits R, et al. Radiosynthesis of racemic and enantiomerically pure (2)-[18F]flubatine: a promising PET radiotracer for neuroimaging of a4b2 nicotinic acetylcholine receptors. Appl Radiat Isot. 2013;74: 128-136.
5. Brust P, Patt JT, Deuther-Conrad W, et al. In vivo measurement of nicotinic acetylcholine receptors with [18F]norchloro-fluoro-homoepibatidine. Synapse. 2008;62:205-218.
6. McParland BJ. Nuclear Medicine Radiation Dosimetry: Advanced Theoretical Principles. London, U.K.: Springer; 2010:456-460.
7. Deuther-Conrad W, Patt JT, Feuerbach D, Wegner F, Brust P, Steinbach J. Norchlorofluoro-homoepibatidine: specificity to neuronal nicotinic acetylcholine receptor subtypes in vitro. Farmaco. 2004;59:785-792.
8. Patt M, Schildan A, Habermann B, et al. Fully automated radiosynthesis of both enantiomers of [18F]flubatine under GMP conditions for human application. Appl Radiat Isot. 2013;80:7-11.
9. Lindstedt SL, Schaeffer PJ. Use of allometry in predicting anatomical and physiological parameters of mammals. Lab Anim. 2002;36:1-19.
10. Thomas SR, Stabin MG, Chen CT, Samaratunga RC. MIRD pamphlet no. 14 revised: a dynamic urinary bladder model for radiation dose calculations. Task Group of the MIRD Committee. J Nucl Med. 1999;40:102S-123S.
11. The 2007 recommendations of the International Commission of Radiological Protection: ICRP publication 103. Ann ICRP. 2007;37:1-332.
12. Stabin MG. Fundamentals of Nuclear Medicine Dosimetry. New York, NY: Springer; 2008:130-137.
13. Constantinescu CC, Sevrioukov E, Garcia A, Pan M-L, Mukherjee J. Evaluation of [18F]mefway biodistribution and dosimetry based on whole-body PET imaging of mice. Mol Imaging Biol. 2013;15:222-229.
14. Constantinescu CC, Garcia A, Mirbolooki MR, Pan M-L, Mukherjee J. Evaluation of [18F]Nifene biodistribution and dosimetry based on whole-body PET imaging of mice. Nucl Med Biol. 2013;40:289-294.
15. Parsey RV, Belanger MJ, Sullivan GM, et al. Biodistribution and radiation dosimetry of 11C-WAY100, 635 in humans. J Nucl Med. 2005;46:614-619.
16. Federal Office for Radiation Protection. Notice of the updated diagnostic reference values for nuclear medicine investigations. Federal Ministry of Justice, Federal Gazette (BAnz). B5, October 19, 2012:1-6.
17. Valentin DJ. Recalculated dose data for 19 frequently used radiopharmaceuticals from ICRP Publication 53. Ann ICRP. 1998;28:47-83.
18. Bottlaender M, Valette H, Roumenov D, et al. Biodistribution and radiation dosimetry of 18F-fluoro-A-85380 in healthy volunteers. J Nucl Med. 2003;44:596-601.
19. Zanotti-Fregonara P, Lammertsma A, Innis R. Suggested pathway to assess radiation safety of 18F-labeled PET tracers for first-in-human studies. Eur J Nucl Med Mol Imaging. 2013;40:1781-1783.
20. Doss M, Kolb HC, Zhang JJ, et al. Biodistribution and radiation dosimetry of the integrin marker 18F-RGD-K5 determined from whole-body PET/CT in monkeys and humans. J Nucl Med. 2012;53:787-795.
21. Maddahi J, Czernin J, Lazewatsky J, et al. Phase I, first-in-human study of BMS747158, a novel 18F-labeled tracer for myocardial perfusion PET: dosimetry, biodistribution, safety, and imaging characteristics after a single injection at rest. J Nucl Med. 2011;52:1490-1498.
22. Lazewatsky J, Azure M, Guaraldi M, et al. Dosimetry of BMS747158, a novel 18F labeled tracer for myocardial perfusion imaging, in nonhuman primates at rest [abstract]. J Nucl Med. 2008;49(suppl 1):15P.
23. Takano A, Gulyás B, Varrone A, et al. Biodistribution and radiation dosimetry of the 18 kDa translocator protein (TSPO) radioligand [18F]FEDAA1106: a human whole-body PET study. Eur J Nucl Med Mol Imaging. 2011;38:2058-2065.
24. Tolvanen T, Yli-Kerttula T, Ujula T, et al. Biodistribution and radiation dosimetry of [11C]choline: a comparison between rat and human data. Eur J Nucl Med Mol Imaging. 2010;37:874-883.
25. Tipre DN, Fujita M, Chin FT, et al. Whole-body biodistribution and radiation dosimetry estimates for the PET dopamine transporter probe 18F-FECNT in nonhuman primates. Nucl Med Commun. 2004;25:737-742.
26. Lu JQ, Ichise M, Liow JS, Ghose S, Vines D, Innis RB. Biodistribution and radiation dosimetry of the serotonin transporter ligand 11C-DASB determined from human whole-body PET. J Nucl Med. 2004;45:1555-1559.
27. Shimizu K, Takashima T, Yamane T, et al. Whole-body distribution and radiation dosimetry of [11C]telmisartan as a biomarker for hepatic organic anion transporting polypeptide (OATP) 1B3. Nucl Med Biol. 2012;39:847-853.