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Additional file 1. Supplemental data.

The Ag-mediated electrophilic [18F]fluorination of an arylboronic ester is reported. This new radiochemical transformation uses [ 18F]selectfluor bis(triflate) in acetone. The process gave 6-[ 18F]fluoro-l-DOPA with a RCY of 19 ± 12% and a specific activity of 2.6 ± 0.3 GBq μmol-1. © 2013 The Royal Society of Chemistry.

OP03 Selective extraction of medically-related radionuclides from proton-irradiated thorium targets, V. Radchenko, J.W. Engle, C. Roy, J. Griswold, M.F. Nortier, E.R. Birnbaum, M. Brugh, S. Mirzadeh, K. D. John, M.E. Fassbender, OP04 Comparison of [68Ga]FSC(succ-RGD)3 and [68Ga]NODAGA-RGD for PET imaging of αvβ3 integrin expression, Chuangyan Zhai, Gerben M. Franssen, Milos Petrik, Peter Laverman, Clemens Decristoforo, OP05 A new NPY-Y1R targeting peptide for breast cancer PET imaging, Ait-Mohand Samia, Dumulon-Perreault Véronique, Guérin Brigitte, OP06 The influence of multivalency on CCK 2 receptor targeting, D. Summer, A. Kroess, C. Rangger, H. Haas, P. Laverman, F. Gerben, E. von Guggenberg, C.Decristoforo, OP07 SPECT Imaging of αvβ3 Expression by [99mTc(N)PNP43]- Bifunctional Chimeric RGD Peptide not Cross-Reacting with αvβ5, Cristina Bolzati, Nicola Salvarese, Fiorenzo Refosco, Laura Meléndez-Alafort, Debora Carpanese, Antonio Rosato, Michele Saviano, Annarita Del Gatto, Daniela Comegna, Laura Zaccaro, OP09 New dienophiles for the inverse-electron-demand Diels-Alder reaction and for pretargeted PET imaging, Emilie Billaud, Muneer Ahamed, Frederik Cleeren, Elnaz Shahbazali, Tim Noël, Volker Hessel, Alfons Verbruggen and Guy Bormans, OP10 New complexing agent for Al18F-labelling of heat-sensitive biomolecules: Synthesis and preclinical evaluation of Al18F-RESCA1-HAS, Cleeren F, Lecina J, Koole M, Verbruggen A and Bormans G, OP11 A novel versatile precursor efficient for F-18 radiolabelling via click-chemistry, B. Lugatoa, S. Stucchia, E.A. Turollaa, L. Giulianoa, S.Toddea, P. Ferraboschib, OP12 A general applicable method to quantify unidentified UV impurities in radiopharmaceuticals, R.P. Klok, M.P.J. Mooijer, N.H. Hendrikse, A.D. Windhorst, OP13 Development of [18F]Fluoro-C-glycosides to radiolabel peptides, Collet C., Petry N., Chrétien F., Karcher G., Pellegrini-Moïse N., Lamandé-Langle S., OP14 A Microfluidic Approach for the 68Ga-labeling of PSMAHBED-CC and NODAGA-RGD, Sarah Pfaff, Cecile Philippe, Markus Mitterhauser, Marcus Hacker, Wolfgang Wadsak, OP16 Surprising reactivity of astatine in the nucleophilic substitution of aryliodonium salts: application to the radiolabeling of antibodies, François Guérard, Yong-Sok Lee, Sébastien Gouard, Kwamena Baidoo, Cyrille Alliot, Michel Chérel, Martin W. Brechbiel, Jean-François Gestin, OP17 64Cu-NOTA-pertuzumab F(ab')2 fragments, a second-generation probe for PET imaging of the response of HER2-positive breast cancer to trastuzumab (Herceptin), Lam K, Chan C, Reilly RM, OP18 Development of radiohalogenated analogues of a avb6-specific peptide for high LET particle emitter targeted radionuclide therapy of cancer, Salomé Paillas, John Marshall, Jean-Pierre Pouget, Jane Sosabowski, OP19 Ligand Specific Efficiency (LSE) as a guide in tracer optimization, Emmanuelle Briard, Yves P. Auberson, John Reilly, Mark Healy, David Sykes, OP23 The radiosynthesis of an 18F-labeled triglyceride, developed to visualize and quantify brown adipose tissue activity, Andreas Paulus, Wouter van Marken Lichtenbelt,Felix Mottaghy, Matthias Bauwens, OP24 Influence of the fluorescent dye on the tumor targeting properties of dual-labeled HBED-CC based PSMA inhibitors, Baranski, Ann-Christin, Schäfer, Martin, Bauder-Wüst, Ulrike, Haberkorn, Uwe, Eder, Matthias, Kopka, Klaus, OP25 [18F]MEL050 as a melanin PET tracer : fully automated radiosynthesis and evaluation for the detection of pigmented melanoma in mice pulmonary metastases, Chaussard M, Hosten B, Vignal N, Tsoupko-Sitnikov V, Hernio N, Hontonnou F, Merlet P, Poyet JL, Sarda-Mantel L, Rizzo-Padoin N, OP26 Design and Preclinical Evaluation of Novel Radiofluorinated PSMA Targeting Ligands Based on PSMA-617, J. Cardinale, M. Schäfer, M. Benešová, U. Bauder-Wüst, O. Seibert, F. Giesel, U. Haberkorn, M. Eder, K. Kopka, OP27 A novel radiolabeled peptide for PET imaging of prostate cancer: 64Cu-DOTHA2-PEG-RM26, Mansour Nematallah, Paquette Michel, Ait-Mohand Samia, Dumulon-Perreault Véronique, Lecomte Roger, Guérin Brigitte, OP29 Biodistribution of [18F]Amylovis®, a new radiotracer PET imaging of β-amyloid plaques, Fernandez-Maza L, Rivera-Marrero S, Prats Capote A, Parrado-Gallego A, Fernandez-Gomez I, Balcerzyk M, Sablon-Carrazana M, Perera-Pintado A, Merceron-Martinez D, Acosta-Medina E, Rodriguez-Tanty C, OP30 Synthesis and preclinical evaluation of [11C]-BA1 PET tracer for the imaging of CSF-1R, Bala Attili, Muneer Ahamed, Guy Bormans, OP31 In vivo imaging of the MCHR1 in the ventricular system via [18F]FE@SNAP, C. Philippe, M. Zeilinger, T. Scherer, C. Fürnsinn, M. Dumanic, W. Wadsak, M. Hacker, M. Mitterhauser, OP32 Synthesis of the first carbon-11 labelled P2Y12 receptor antagonist for imaging the anti-inflammatory phenotype of activated microglia, B. Janssen, D.J. Vugts, G.T. Molenaar, U. Funke, P.S. Kruijer, F. Dollé, G. Bormans, A.A. Lammertsma, A.D. Windhorst, OP33 Radiosynthesis of a selective HDAC6 inhibitor [11C]KB631 and in vitro and ex vivo evaluation, Koen Vermeulen, Muneer Ahamed, Michael Schnekenburger, Mathy Froeyen, Dag Erlend Olberg, Marc Diederich, Guy Bormansa, OP34 Improving metabolic stability of fluorine-18 labelled verapamil analogues, Raaphorst RM, Luurtsema G, Lammertsma AA, Elsinga PH, Windhorst AD, OP36 Development of a novel PET tracer for the activin receptor-like kinase 5, Lonneke Rotteveel, Uta Funke, Peter ten Dijke, Harm Jan Bogaard, Adriaan A. Lammertsma, Albert D. Windhorst, OP37 SPECT imaging and biodistribution studies of 111In-EGF-Au-PEG nanoparticles in vivo, Lei Song, Sarah Able, Nadia Falzone, Veerle Kersemans, Katherine Vallis, OP38 Melanoma targeting with [99mTc(N)(PNP3)]-labeled NAPamide derivatives: preliminary pharmacological studies, Davide Carta, Nicola Salvarese, Wiebke Sihver, Feng Gao, Hans Jürgen Pietzsch, Barbara Biondi, Paolo Ruzza, Fiorenzo Refosco, Cristina Bolzati, OP39 [68Ga]NODAGA-RGD: cGMP synthesis and data from a phase I clinical study, Roland Haubner, Armin Finkensted, Armin Stegmair, Christine Rangger, Clemens Decristoforo, Heinz Zoller, Irene J. Virgolin, OP44 Implementation of a GMP-grade radiopharmacy facility in Maastricht, Ivo Pooters, Maartje Lotz, Roel Wierts, Felix Mottaghy, Matthias Bauwens, OP45 Setting up a GMP production of a new radiopharmaceutical, Forsback, Sarita, Bergman Jörgen, Kivelä Riikka, OP48 In vitro and in vivo evaluation of 68-gallium labeled Fe3O4-DPD nanoparticles as potential PET/MRI imaging agents, M. Karageorgou, M. Radović, C. Tsoukalas, B. Antic, M. Gazouli, M. Paravatou-Petsotas, S. Xanthopouls, M. Calamiotou, D. Stamopoulos, S. Vranješ-Durić, P. Bouziotis, OP49 Fast PET imaging of inflammation using 68Ga-citrate with Fe-containing salts of hydroxy acids, A. S. Lunev, A. A. Larenkov, K.A. Petrosova, O. E. Klementyeva, G. E. Kodina, PP01 Installation and validation of 11C-methionine synthesis, Kvernenes, O.H., Adamsen, T.C.H., PP02 Fully automated synthesis of 68Ga-labelled peptides using the IBA Synthera® and Synthera® Extension modules, René Martin, Sebastian Weidlich, Anna-Maria Zerges, Cristiana Gameiro, Neva Lazarova, Marco Müllera, PP03 GMP compliant production of 15O-labeled water using IBA 18 MeV proton cyclotron, Gert Luurtsema, Michèl de Vries, Michel Ghyoot, Gina van der Woude, Rolf Zijlma, Rudi Dierckx, Hendrikus H. Boersma, Philip H. Elsinga, PP04 In vitro Nuclear Imaging Potential of New Subphthalocyanine and Zinc Phthalocyanine, Fatma Yurt Lambrecht, Ozge Er, Mine Ince, Cıgır Biray Avci, Cumhur Gunduz, Fatma Aslihan Sarı, PP05 Synthesis, Photodynamic Therapy Efficacy and Nuclear Imaging Potential of Zinc Phthalocyanines, Kasim Ocakoglu, Ozge Er, Onur Alp Ersoz, Fatma Yurt Lambrecht, Mine Ince, Cagla Kayabasi, Cumhur Gunduz, PP06 Radio-U(H)PLC – the Search on the Optimal Flow Cell for the γ-Detector, Torsten Kniess, Sebastian Meister, Steffen Fischer, Jörg Steinbach, PP07 Radiolabeling, characterization & biodistribution study of cysteine and its derivatives with Tc99m, Rabia Ashfaq, Saeed Iqbal, Atiq-ur-Rehman, Irfan ullah Khan, PP08 Radiolabelling of poly (lactic-co.glycolic acid) (PLGA) nanoparticles with 99mTC, R Iglesias-Jerez, Cayero-Otero, L. Martín-Banderas, A. Perera-Pintado, I. Borrego-Dorado, PP09 Development of [18F]PD-410 as a non-peptidic PET radiotracer for gastrin releasing peptide receptors, Ines Farinha-Antunes, Chantal Kwizera, Enza Lacivita, Ermelinda Lucente, Mauro Niso, Paola De Giorgio, Roberto Perrone, Nicola A. Colabufo, Philip H. Elsinga, Marcello Leopoldo, PP10 An improved nucleophilic synthesis of 2-(3,4-dimethoxyphenyl)-6-(2-[18F]fluoroethoxy) benzothiazole ([18F]FEDMBT), potential diagnostic agent for breast cancer imaging by PET, V.V. Vaulina, O.S. Fedorova, V.V. Orlovskaja, ?�.L. Chen, G.Y. Li, F.C. Meng, R.S. Liu, H.E. Wang, R.N. Krasikova, PP11 Internal radiation dose assessment of radiopharmaceuticals prepared with accelerator-produced 99mTc, Laura Meléndez-Alafort, Mohamed Abozeid, Guillermina Ferro-Flores, Anna Negri, Michele Bello, Nikolay Uzunov, Martha Paiusco, Juan Esposito, Antonio Rosato, PP12 A specialized five-compartmental model software for pharmacokinetic parameters calculation, Laura Meléndez-Alafort, Cristina Bolzati, Guillermina Ferro-Flores, Nicola Salvarese, Debora Carpanese, Mohamed Abozeid, Antonio Rosato, Nikolay Uzunov, PP13 Molecular imaging of the pharmacokinetic behavior of low molecular weight 18F-labeled PEtOx in comparison to 89Zr-labeled PEtOx, Palmieri L, Verbrugghen T, Glassner M, Hoogenboom R, Staelens S, Wyffels L, PP14 Towards nucleophilic synthesis of the α-[18F]fluoropropyl-L-dihydroxyphenylalanine, V. V. Orlovskaja, O. F. Kuznetsova, O. S. Fedorova, V. I. Maleev, Yu. N. Belokon, A. Geolchanyan, A. S. Saghyan, L. Mu, R. Schibli, S. M. Ametamey, R. N. Krasikova, PP15 A convenient one-pot synthesis of [18F]clofarabine, Revunov, Evgeny, Malmquist, Jonas, Johnström, Peter, Van Valkenburgh, Juno, Steele, Dalton, Halldin, Christer, Schou, Magnus, PP16 BODIPY-estradiol conjugates as multi-modality tumor imaging agents, Samira Osati,Michel Paquette,Simon Beaudoin,Hasrat Ali,Brigitte Guerin, Jeffrey V. Leyton, Johan E. van Lier, PP17 Easy and high yielding synthesis of 68Ga-labelled HBED-PSMA and DOTA-PSMA by using a Modular-Lab Eazy automatic synthesizer, Di Iorio V, Iori M, Donati C, Lanzetta V, Capponi PC, Rubagotti S, Dreger T, Kunkel F, Asti M, PP18 Synthesis and evaluation of fusarinine C-based octadentate bifunctional chelators for zirconium-89 labelling, Chuangyan Zhai, Christine Rangger, Dominik Summer, Hubertus Haas, Clemens Decristoforo, PP19 Fully automated production of [18F]NaF using a re-configuring FDG synthesis module., Suphansa Kijprayoon, Ananya Ruangma, Suthatip Ngokpol, Samart Tuamputsha, PP20 Extension of the Carbon-11 Small Labeling Agents Toolbox and Conjugate Addition, Ulrike Filp, Anna Pees, Carlotta Taddei, Aleksandra Pekošak, Antony D. Gee, Alex J. Poot, Albert D. Windhorst, PP21 In vitro studies on BBB penetration of pramipexole encapsulated theranostic liposomes for the therapy of Parkinson’s disease, Mine Silindir Gunay, A. Yekta Ozer, Suna Erdogan, Ipek Baysal, Denis Guilloteau, Sylvie Chalon, PP22 Factors affecting tumor uptake of 99mTc-HYNIC-VEGF165, Filippo Galli, Marco Artico, Samanta Taurone, Enrica Bianchi, Bruce D. Weintraub, Mariusz Skudlinski, Alberto Signore, PP23 Rhenium-188: a suitable radioisotope for targeted radiotherapy, Nicolas Lepareur, Nicolas Noiret, François Hindré, Franck Lacœuille, Eric Benoist, Etienne Garin, PP24 Preparation of a broad palette of 68Ga radiopharmaceuticals for clinical applications, Trejo-Ballado F, Zamora-Romo E, Manrique-Arias JC, Gama-Romero HM, Contreras-Castañon G, Tecuapetla-Chantes RG, Avila-Rodriguez MA, PP25 68Ga-peptide preparation with the use of two 68Ge/68Ga-generators, H. Kvaternik, D. Hausberger, C. Zink, B. Rumpf, R. M. Aigner, PP26 Assay of HEPES in 68Ga-peptides by HPLC, H. Kvaternik, D. Hausberger, B. Rumpf, R. M. Aigner, PP27 Preparation, in vitro and in vivo evaluation of a 99mTc(I)-Diethyl Ester (S,S)-Ethylenediamine- N,N´-DI-2-(3-Cyclohexyl) Propionic acid as a target-specific radiopharmaceutical, Drina Janković, Mladen Lakić, Aleksandar Savić, Slavica Ristić, Nadežda Nikolić, Aleksandar Vukadinović, Tibor J. Sabo, Sanja Vranješ-Đurić, PP28 90Y-labeled magnetite nanoparticles for possible application in cancer therapy, S. Vranješ-Đurić, M. Radović, D. Janković, N. Nikolić, G. F. Goya, P. Calatayud, V. Spasojević, B. Antić, PP29 Simplified automation of the GMP production of 68Ga-labelled peptides, David Goblet, Cristiana Gameiro, Neva Lazarova, PP30 Combining commercial production of multi-products in a GMP environment with Clinical & R&D activities, Cristiana Gameiro, Ian Oxley, Antero Abrunhosa, Vasko Kramer, Maria Vosjan, Arnold Spaans, PP31 99mTc(CO)3-labeling and Comparative In-Vivo Evaluation of Two Clicked cRGDfK Peptide Derivatives, Kusum Vats, Drishty Satpati, Haladhar D Sarma, Sharmila Banerjee, PP32 Application of AnaLig resin for 99mTc separation from molybdenum excess, Wojdowska W., Pawlak D.W., Parus L. J., Garnuszek P., Mikołajczak R., PP33 Constraints for selection of suitable precursor for one-step automated synthesis of [18F]FECNT, the dopamine transporter ligand, Pijarowska-Kruszyna J, Jaron A, Kachniarz A, Malkowski B, Garnuszek P, Mikolajczak R, PP34 Gamma scintigraphy studies with 99mTc- amoxicillin sodium in bacterially infected and sterile inflamed rats, Derya Ilem-Ozdemir, Oya Caglayan-Orumlu, Makbule Asikoglu, PP35 Preparation of 99mTc- Amoxicillin Sodium Lyophilized Kit, Derya Ilem-Ozdemir, Oya Caglayan-Orumlu, Makbule Asikoglu, PP36 Outfits of Tracerlan FXC-PRO for 11C-Labeling, Arponen Eveliina, Helin Semi, Saarinen Timo, Vauhkala Simo, Kokkomäki Esa, Lehikoinen Pertti, PP37 Microfluidic synthesis of ω-[18F]fluoro-1-alkynes, Mariarosaria De Simone, Giancarlo Pascali, Ludovica Carzoli, Mauro Quaglierini, Mauro Telleschi, Piero A. Salvadori, PP38 Automated 18F-flumazenil production using chemically resistant disposable cassettes, Phoebe Lam, Martina Aistleitner, Reinhard Eichinger, Christoph Artner, PP39 The effect of the eluent solutions (TBAHCO3, Kryptand K2.2.2) on the radiochemical yields of 18F-Fluoromethylcholine, Surendra Nakka, Hemantha Kumara MC, Al-Qahtani Mohammed, PP40 [68Ga]Radiolabeling of short peptide that has a PET imaging potentials, Al-Qahtani, Mohammed, Al-Malki, Yousif, PP41 Is validation of radiochemical purity analysis in a public hospital in a developing country possible?, N Mambilima, SM Rubow, PP42 Improved automated radiosynthesis of [18F]FEPPA, N. Berroterán-Infante, M. Hacker, M. Mitterhauser, W. Wadsak, PP43 Synthesis and initial evaluation of Al18F-RESCA1-TATE for somatostatin receptor imaging with PET, Uta Funke, Frederik Cleeren, Joan Lecina, Rodrigo Gallardo, Alfons M. Verbruggen, Guy Bormans, PP44 Radiolabeling and SPECT/CT imaging of different polymer-decorated zein nanoparticles for oral administration, Rocío Ramos-Membrive, Ana Brotons, Gemma Quincoces, Laura Inchaurraga, Inés Luis de Redín, Verónica Morán, Berta García-García, Juan Manuel Irache, Iván Peñuelas, PP45 An analysis of the quality of 68Ga-DOTANOC radiolabelling over a 3 year period, Trabelsi, M., Cooper M.S., PP46 In vivo biodistribution of adult human mesenchymal stem cells I (MSCS-ah) labeled with 99MTC-HMPAO administered via intravenous and intra-articular in animal model. Preliminary results, Alejandra Abella, Teodomiro Fuente, Antonio Jesús Montellano, Teresa Martínez, Ruben Rabadan, Luis Meseguer-Olmo, PP47 Synthesis of [18F]F-exendin-4 with high specific activity, Lehtiniemi P, Yim C, Mikkola K, Nuutila P, Solin O, PP48 Experimental radionuclide therapy with 177Lu-labelled cyclic minigastrin and human dosimetry estimations, von Guggenberg E, Rangger C, Mair C, Balogh L, Pöstényi Z, Pawlak D, Mikołajczak R, PP49 Synthesis of radiopharmaceuticals for cell radiolabelling using anion exchange column, Socan A, Kolenc Peitl P, Krošelj M, Rangger C, Decristoforo C, PP50 [68Ga]peptide production on commercial synthesiser mAIO, Collet C., Remy S., Didier R,Vergote T.,Karcher G., Véran N., PP51 Dry kit formulation for efficient radiolabeling of 68Ga-PSMA, D. Pawlak, M. Maurin, P. Garnuszek, U. Karczmarczyk, R. Mikołajczak, PP52 Development of an experimental method using Cs-131 to evaluate radiobiological effects of internalized Auger-electron emitters, Pil Fredericia, Gregory Severin, Torsten Groesser, Ulli Köster, Mikael Jensen, PP53 Preclinical comparative evaluation of NOTA/NODAGA/DOTA CYCLO-RGD peptides labelled with Ga-68, R. Leonte, F. D. Puicea, A. Raicu, E. A. Min, R. Serban, G. Manda, D. Niculae, PP54 Synthesizer- and Kit-based preparation of prostate cancer imaging agent 68Ga-RM2, Marion Zerna, Hanno Schieferstein, Andre Müller, Mathias Berndt, PP55 Synthesis of pancreatic beta cell-specific [18F]fluoro-exendin-4 via strain-promoted aza-dibenzocyclooctyne/azide cycloaddition, Cheng-Bin Yim, Kirsi Mikkola, Pirjo Nuutila, Olof Solin, PP56 Automated systems for radiopharmacy, D. Seifert, J. Ráliš, O. Lebeda, PP57 Simple, suitable for everyday routine use quality control method to assess radionuclidic purity of cyclotron-produced 99mTc, Svetlana V. Selivanova, Helena Senta, Éric Lavallée, Lyne Caouette, Éric Turcotte, Roger Lecomte, PP58 Effective dose estimation using Monte Carlo simulation for patients undergoing radioiodine therapy, Marina Zdraveska Kochovska, Emilija Janjevik Ivanovska, Vesna Spasic Jokic, PP59 Chemical analysis of the rituximab radioimmunoconjugates in lyophilized formulations intended for oncological applications, Darinka Gjorgieva Ackova, Katarina Smilkov, Petre Makreski, Trajče Stafilov, Emilija Janevik-Ivanovska, PP61 The need and benefits of established radiopharmacy in developing African countries, Aschalew Alemu, Joel Munene Muchira, David Mwanza Wanjeh, Emilija Janevik-Ivanovska, PP62 University Master Program of Radiopharmacy – step forward for Good Radiopharmacy Education, Emilija Janevik-Ivanovska, Zoran Zdravev, Uday Bhonsle, Osso Júnior João Alberto, Adriano Duatti, Bistra Angelovska, Zdenka Stojanovska, Zorica Arsova Sarafinovska, Darko Bosnakovski, Darinka Gorgieva-Ackova, Katarina Smilkov, Elena Drakalska, Meera Venkatesh, Rubin Gulaboski, PP63 Synthesis and preclinical validations of a novel 18F-labelled RGD peptide prepared by ligation of a 2-cyanobenzothiazole with 1,2-aminothiol to image angiogenesis., Didier J. Colin, James A. H. Inkster, Stéphane Germain, Yann Seimbille

Contains fulltext : 171117.pdf (Publisher’s version ) (Open Access) Overexpression of the epidermal growth factor receptor (EGFR) is linked to an adverse outcome in various solid tumors. Cetuximab is an EGFR inhibitor, which in combination with radiotherapy improves locoregional control and survival in a subgroup of patients with head and neck squamous cell carcinomas (HNSCCs). The aim of this study was to develop and characterize an EGFR-directed PET tracer, (64) Cu-cetuximab-F(ab')2 , to determine the systemic accessibility of EGFR. Mice with HNSCC xenografts, UT-SCC-8 (n = 6) or UT-SCC-45 (n = 6), were imaged 24 h post injection with (64) Cu-NODAGA-cetuximab-F(ab')2 using PET/CT. One mouse for each tumor model was co-injected with excess unlabeled cetuximab 3 days before radiotracer injection to determine non-EGFR-mediated uptake. Ex vivo biodistribution of the tracer was determined and tumors were analyzed by autoradiography and immunohistochemistry. The SUVmax of UT-SCC-8 tumors was higher than that of UT-SCC-45: 1.5 +/- 1.0 and 0.8 +/- 0.2 (p < 0.05), respectively. SUVmax after in vivo blocking of EGFR with cetuximab was 0.4. Immunohistochemistry showed that UT-SCC-8 had a significantly higher EGFR expression than UT-SCC-45: 0.50 +/- 0.19 versus 0.12 +/- 0.08 (p < 0.005), respectively. Autoradiography indicated that (64) Cu-cetuximab-F(ab')2 uptake correlated with EGFR expression in both tumors: r = 0.86 +/- 0.06 (UT-SCC-8) and 0.90 +/- 0.06 (UT-SCC-45). (64) Cu-cetuxmab-F(ab')2 is a promising PET tracer to determine expression of EGFR in vivo. Clinically, this tracer has the potential to be used to determine cetuximab targeting of tumors and possibly to non-invasively monitor the response to EGFR-inhibitor treatment. Copyright (c) 2015 John Wiley & Sons, Ltd.

Introduction High starting radioactivity is usually advantageous for producing radiopharmaceuticals with high specific radioactivity. However, the [11C]CH4 yields from N2-H2 gas target fall short from theoretical amounts, as calculated from the cross section for the well-known 14N(p,α)11C nuclear reaction1. The beneficial effect of increased target chamber temperature on [11C]CH4 yields has recently been brought forward by us2 and others3. In addition to the temperature effect, our attention has also been on the hydrogen content factor. This study intends to examine the N2-H2 target performance in a substantially larger target chamber and at higher temperatures than our setup before and compare the results to the existing data. Materials and Methods Aluminium bodied custom design target chamber is used in fixed 17 MeV proton beam irradiations. Target chamber is equipped with heating elements and cooling circuit for temperature control. In addition to the target chamber body temperature, the target gas loading pressure and irradiation current can be varied. The irradiation product is collected into an ad-sorbent trap that was immersed in a liquid argon cooling bath within a dose calibrator. Results and Conclusion Pursued data will show [11C]CH4 saturation yields (Ysat [GBq/µA]) at different irradiation and target parameters.

The PET radionuclide 61Cu is accessible through several nuclear reactions. Besides the common production route via 61Ni(p,n)61Cu the 64Zn(p,α)61Cu reaction offers some advantages. Especially the comparatively cheap enriched 64Zn makes this process economical. For fast product purification and recycling of target material an ion exchanger cascade was developed. In addition a separation technique with a copper selective resin was tested. 61Cu with specific activities up to 1000 GBq/µmol was produced with these methods.

Ziel: Die Herstellung von 61Cu hoher spezifischer Aktivität erfordert besonders aufwändige Maßnahmen, um Metallkontaminationen sowohl durch Cu-Isotope als auch durch andere Metalle zu minimieren. Dementsprechend müssen die herkömmlichen Methoden ververfeinert werden, um 61Cu sowohl in hoher Qualität als auch effektiv herstellen zu können. Vergleichswerte über spezifische Aktivitäten von 61Cu sind in der Literatur selten zu finden. McCarthy et al. [1] berichten zu spez. Aktivitäten von 61Cu im Bereich von 47 bis 190 GBq/µmol; erzeugt durch 61Ni(p,n)61Cu und 60Ni(d,n)61Cu-Reaktion. Eine Alternative dazu stellt die 64Zn(p,α)61Cu-Reaktion dar [2]. Das hierfür genutzte Targetmaterial 64Zn (99,3% Isotopenanreicherung) ist im Vergleich zu angereichertem 61Ni weitaus weniger kostenintensiv. Methoden: Für die Bestrahlung am Zyklotron wird ein massiver Targetträger aus Gold verwendet, auf dem ca. 100 mg angereichertes 64Zn (99,3% Isotopenanreicherung) abgeschieden sind. Die radiochemische Trennung erfolgt über Ionenaustauschtechniken nach Literaturangaben [3-8]. Die angewandte Methode nutzt eine Ionenaustauscherkaskade, die aus zwei Kationenaustauscher-Säulen und einer Anionenaustauscher-Säule besteht. Dabei sorgt der doppelte Kationenaustauscherschritt für die effektive Abtrennung von Galliumisotopen (66/67/68Ga) und die Anionenaustauscher-Säule für die Trennung des 61Cu vom Zn-Targetmaterial. Der Gesamtprozess zur Gewinnung des gereinigten 61Cu dauert eine Stunde. Die Methode umfasst die Wiedergewinnung des eingesetzten 64Zn, welches danach zur erneuten Verwendung zur Verfügung steht. Das optimierte Verfahren nutzt kleinere Ionenaustauschersäulen als bisher und ausschließlich wässrige Salzsäure; Details vgl. Thieme et al. [2]. Die Ermittlung der spezifischen Aktivität erfolgt über TETA-Titrationen und ICP-MS-Analysen. Es wurden Bestrahlungen an zwei verschiedenen Zyklotronen durchgeführt: am Cyclone 18/9 (IBA, Belgien) des Instituts für Radiopharmazie, Dresden-Rossendorf und am CC 18/9 (Efremov Institut, St. Petersburg, Russland) des Turku PET Centre in Turku, Finnland. Ergebnisse: Die Bestrahlungen mit dem Cyclone 18/9 wurden mit 12 µA und 16 MeV durchgeführt. Dies führte innerhalb von 30 Minuten zu Ausbeuten von ca. 300 MBq 61Cu (EOB). Am CC 18/9 wurde mit 30 µA, 13 MeV, 30 Minuten gearbeitet. Dabei wurden ebenfalls 330-400 MBq 61Cu (EOB) erzeugt, bei einer Bestrahlungszeit von 3 Stunden bis zu 1150 MBq61Cu (EOB). Am CC 18/9 wurde eine extrem hohe spezifische Aktivität des 61Cu von über 1000 GBq/µmol erreicht. Demgegenüber fielen die spezifischen Aktivitäten am Cyclone 18/9 deutlich ab, es konnte nur eine spezifische Aktivität von ca. 2 GBq/µmol erzielt werden. Wahrscheinlich tritt in diesem Fall eine Kontamination mit stabilem Kupfer schon während der Bestrahlung auf. Möglicherweise geht diese von der Targethalterung am Zyklotron aus, da sie nicht wie beim CC 18/9 komplett aus Aluminium, sondern größtenteils aus Messing besteht. Bisherige Versuche zum Schutz des Targetträgers und des Targetmaterials vor derartigen Kontaminationen bzw. der Versuch, Kontaminationen während des Trennprozesses zu verhindern, blieben erfolglos. Schlussfolgerungen: Die Ergebnisse zeigen, dass es prinzipiell möglich ist, 61Cu mit hoher spezifischer Aktivität mit Hilfe der 64Zn(p,α)61Cu-Reaktion herzustellen. Die genutzte radiochemische Trennmethode bietet sich hervorragend für eine routinemäßige Herstellung von 61Cu an. Referenzen: [1] McCarthy, D. W.; Bass, L. A.; Cutler, P. D.; Shefer, R. E.; Klinkowstein, R. E.; Herrero, P.; Lewis, J. S.; Cutler, C. S.; Anderson, C. J.; Welch, M. J. (1999) Nucl. Med. Biol. 26, 351-358 [2] Thieme, S.; Walther, M.; Pietzsch, H.-J.; Steinbach, J. in: Technetium and other radiometals in chemistry and medicine (Mazzi, U.; Eckelman, W. C.; Volkert, W. A. eds.), pp 475-478, SGE Editoriali, Padova, Italy [3] Kraus, K. A.; Moore, G. E. (1953) J. Am. Chem. Soc. 75, 1460-1462 [4] O'Brien, H. A. (1969) Int. J. Appl. Radiat. Isot. 20, 121-124 [5] Neirinckx, R. D. (1977) Int. J. Appl. Radiat. Isot. 28, 802-804 [6] Jamriska, D. J.; Taylor, W. A.; Ott, M. A.; Heaton, R. C.; Phillips, D. R.; Fowler, M. M. (1995) J. Radioanal. Nucl. Chem. Art. 195, 263-270 [7] Smith, S. V.; Waters, D. J.; Di Bartolo, N. (1996) Radiochim. Acta 75, 65-68 [8] Rowshanfarzad, P.; Sabet, M.; Jalilian, A. R.; Kamalidehghan, M. (2006) Appl. Radiat. Isot. 64, 1563-1573

Objectives: Optimized production and separation parameters, use of only ultra-pure reagents with ppt-levels of metal traces are necessary for the production of high specific activities (SA) 61Cu. From previous studies regarding production of 61Cu there is little data on SA published. McCarthy et al. [1] measured SA ranging from 47 to 190 GBq/µmol for 61Cu produced via 61Ni(p,n)61Cu and 60Ni(d,n)61Cu reaction. An alternative method for production is the use of the 64Zn(p,α)61Cu reaction [2]. The use of 99% enriched 64Zn is considerably cheaper than use of enriched 61Ni. Methods: A target setup was developed using approximately 100 mg enriched 64Zn electroplated on a massive gold disk for proton irradiation. The radiochemical separation technique included recycling of the target material and was based on ion exchange methods described in the literature [3-8]. It consisted of a system of cation and anion exchange columns. This ion exchanger cascade included a twofold cation exchange step developed for effective removal of gallium by-products (66/67/68Ga) and one anion exchange step to separate 61Cu from the target material. This separation procedure took one hour. After the recycling procedure for the target material a new electrodeposition of the 64Zn could be carried out. The method used small ion exchange columns, aqueous hydrochloric acid solutions and is described in detail by Thieme et al. [2]. The SA was evaluated by TETA binding assay with radio TLC. Two different cyclotrons were used for the irradiations: a Cyclone 18/9 (IBA, Belgium) at the Insitute of Radiopharmacy in Dresden-Rossendorf with a home-made solid target holder and a CC 18/9 (Efremov Institute, St. Petersburg, Russia) at Turku PET Centre in Turku also with a home-made solid target holder. Results: With the Cyclone 18/9 the irradiations were performed with 12 µA of 16 MeV protons on target for 30 min and yielded about 300 MBq 61Cu at EOB. The CC 18/9 irradiations with 30 µA of 13 MeV protons on target for 30 min yielded 330-400 MBq 61Cu, and with 3 hours 1150 MBq 61Cu, respectively. SA of 500 GBq/µmol were achieved with the CC 18/9 which is equipped with a solid target holder completely made of aluminum preventing contamination of the target disk with non-radioactive copper. Compared to the low specific activities, less than 1 GBq/µmol was achieved at the Cyclone 18/9. This low SA is most likely caused by contamination with non-radioactive copper from the currently used solid target holder containing brass/copper parts. Conclusions: These results show the possibility to produce high SA 61Cu (SA up to 500 GBq/µmol) via the 64Zn(p,α)61Cu reaction at low proton energies. Together with the used radiochemical separation method it is possible to produce high quality 61Cu routinely.

Excitation functions were measured using the stacked foil irradiation technique from threshold energies to 28 MeV for He-3- and to 21 MeV for alpha-particle induced nuclear reactions on natural antimony leading to the formation of I-121,I-123,I-124 radioisotopes. The measured excitation functions were compared with the contradicting results of the earlier investigations found in the literature and with the curves predicted by the ALICE-IPPE and EMPIRE-II codes. Integral yields were also calculated and compared with the experimental thick target yields reported in the literature. (C) 2009 Elsevier Ltd. All rights reserved.

S-([18F]fluoromethyl)-(+)-McN5652 ([18F](+)-FMe-McN5652) has recently been synthesized as a new potential radiotracer for positron emission tomography (PET) imaging of the 5-HT transporter. It is an analog of [11C](+)-McN5652, which has been used in clinical PET studies for 5-HT transporter imaging. This article describes the comparison of these two radiotracers in pigs with respect to their in vivo binding characteristics. PET images revealed that the highest accumulation of both radiotracers was found in the ventral midbrain, thalamus, olfactory lobe, and pons which is consistent with the known density of 5-HT transporters. The specific binding was determined by subtracting the values of the inactive (-) enantiomers or of the occipital cortex from those obtained with [11C](+)-McN5652 or [18F](+)-FMe-McN5652 in the time period between 75 and 115 min after radiotracer injection. The specific binding of the 18F-labeled derivative was about 40 % higher than that of the 11C-labeled derivative. A strong inhibition of the specific binding was observed for both radiotracers after pre-treatment with the selective 5-HT uptake inhibitor citalopram. [18F](+)-FMe-McN5652 showed faster kinetics than [11C](+)-McN5652. It reached the binding equilibrium during a study length of 120 min, which was not the case for [11C](+)-McN5652. It is concluded that [18F](+)-FMe-McN5652 is suitable for 5-HT transporter imaging with PET.

The [18F]fluoromethyl analog of (+)-McN5652 ([18F]FMe-NcN) for imaging serotonin transporter (SERT) with positron emission tomography (PET) has recently been synthesized. We describe here the biological evaluation of [18F]FMe-NcN in rats. Biodistribution studies of [18F]FMe-McN in rat brain ex vivo after an intravenous injection showed a high accumulation of radioactivity in the regions rich in SERT, such as raphe nuclei, hypothalamus, thalamus, substantia nigra, locus coeruleus, and amygdala. Region-to-cerebellum ratios reached a muximum value of 9 in raphe nuclei within 3.5 h after administration. The specificity and selctivity of [18F]FMe-McN binding to SERT was studied by preinjecting blocking doses of serotonin, norepinephrine, and dopamine transporter inhibitors. Fluoxetine, a specific inhibitor for SERT, decreased the specific binding of [18F]FMe-McN in raphe nuclei by 91 plus minus 4 %; in other regions rich in SERT, similar results were obtained GBR12909 and nisoxetine, selective inhibitors for dopamine transporter (DAT) and norepinephrine transporter (NET), respectively, showed no significant effects on the uptake of [18F]FMe-McN. Our studies show that [18F]FMe-McN has a clear potential as a tracer for studies with PET or SERT function in humans.

Hypoxia is a characteristic feature of malignant tumors that should be evaluated before the start of therapy. (18)F-labeled fluoroerythronitroimidazole (FETNIM) is a possible candidate for imaging tumor hypoxia with PET. Quantitative analysis of [(18)F]FETNIM uptake in vivo is necessary before proceeding to assays predicting hypoxia.Eight patients with untreated head and neck squamous cell carcinoma were enrolled in the study. All patients underwent dynamic PET imaging with [(18)F]FETNIM, coupled with measurements of blood flow with [(15)O]H(2)O and blood volume with [(15)O]CO. The metabolically active tumor volume was determined from [(18)F]FDG PET performed on a separate day. [(18)F]FETNIM uptake in the tumor was correlated with that in neck muscles and arterial plasma and compared with the findings of other PET studies.Blood flow in tumor was 5- to 30-fold greater than in muscle, in contrast to blood volume, which did not significantly differ in the 2 tissues. With [(18)F]FETNIM PET, muscle activity remained invariably less than plasma activity, whereas activity in whole tumors was always greater than that in muscle. In 4 instances, the maximum tumor uptake of [(18)F]FETNIM was 1.2-2.0 times higher than plasma activity in the late dynamic phase. A kinetic model developed for calculation of distribution volume of reversibly trapping tracers was successfully applied in the [(18)F]FETNIM studies. Tumor distribution volume correlated strongly with the standardized uptake value of [(18)F]FETNIM between 60 and 120 min and with blood flow but not with the standardized uptake value of [(18)F]FDG. The relationship between [(18)F]FETNIM uptake and the blood flow of the tumor was less obvious on a pixel-by-pixel level.Uptake of [(18)F]FETNIM in head and neck cancer is highly variable and seems to be governed by blood flow at least in the early phase of tissue accumulation. Maximum tumor-to-muscle tracer uptake ratios180 min were in the range of 1-4, comparing favorably with those reported previously for [(18)F]fluoromisonidazole. Assessment of the distribution volume of [(18)F]FETNIM after the initial blood-flow phase is feasible for subsequent evaluation of hypoxia-specific retention.