Articles

Synthesis, radiosynthesis, in vitro and first in vivo evaluation of a new matrix metalloproteinase inhibitor based on γ-fluorinated α-sulfonylaminohydroxamic acid

To study MMP activity in vivo in disease, several radiolabeled MMP inhibitors functioning as radiotracers have been evaluated by means of SPECT and PET. Unfortunately, most of them suffer from metabolic instab...

Authors: Verena Hugenberg, Malte Behrends, Stefan Wagner, Sven Hermann, Michael Schäfers, Hartmuth C. Kolb, Katrin Szardenings, Joseph C. Walsh, Luis F. Gomez, Klaus Kopka and Günter Haufe

A random walk approach to estimate the confinement of α-particle emitters in nanoparticles for targeted radionuclide therapy

Targeted radionuclide therapy is a highly efficient but still underused treatment modality for various types of cancers that uses so far mainly readily available β-emitting radionuclides. By using α-particle e...

Authors: Uwe Holzwarth, Isaac Ojea Jimenez and Luigi Calzolai

Comparison of fully-automated radiosyntheses of [¹¹C]erlotinib for preclinical and clinical use starting from in target produced [¹¹C]CO₂ or [¹¹C]CH₄

[¹¹C]erlotinib has been proposed as a PET tracer to visualize the mutational status of the epidermal growth factor receptor (EGFR) in cancer patients. For clinical use, a stable, reproducible and high-yielding ra...

Authors: Cécile Philippe, Severin Mairinger, Verena Pichler, Johann Stanek, Lukas Nics, Markus Mitterhauser, Marcus Hacker, Thomas Wanek, Oliver Langer and Wolfgang Wadsak

19th European Symposium on Radiopharmacy and Radiopharmaceuticals (ESRR’18)

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Preparation and preclinical evaluation of a ⁶⁸Ga-labelled c(RGDfK) conjugate comprising the bifunctional chelator NODIA-Me

We recently developed a chelating platform based on the macrocycle 1,4,7-triazacyclononane with up to three, five-membered azaheterocyclic arms for the development of ⁶⁸Ga- and ⁶⁴Cu-based radiopharmaceuticals. He...

Authors: Tilman Läppchen, Jason P. Holland, Yvonne Kiefer and Mark D. Bartholomä

A new two-strip TLC method for the quality control of technetium-99m mercaptoacetyl-triglycine (^99mTc-MAG3)

^99mTc-mercaptoacetyl-triglycine (^99mTc-MAG3) has been used for dynamic renal imaging since about 30 years. Free pertechnetate (^99mTcO₄), colloidal ^99mTc ((^99mTcO₂)_n), ^99mTc-tartrate (precursor), precomplexes (^99m

Authors: Marietta Straub, Michel Leresche, Claude Pilloud, Fabien Devynck, Nicolas Stritt and Rolf Hesselmann

Synthesis of an Al¹⁸F radiofluorinated GLU-UREA-LYS(AHX)-HBED-CC PSMA ligand in an automated synthesis platform

Overexpression of prostatic membrane antigen (PSMA) is associated with the progression and prognosis of prostate cancer. There are numerous studies using this peptide with the ⁶⁸Ga radionuclide. Previous methods ...

Authors: Javier Giglio, Maia Zeni, Eduardo Savio and Henry Engler

Production of novel diagnostic radionuclides in small medical cyclotrons

The global network of cyclotrons has expanded rapidly over the last decade. The bulk of its industrial potential is composed of small medical cyclotrons with a proton energy below 20 MeV for radionuclides prod...

Authors: Mateusz Adam Synowiecki, Lars Rutger Perk and J. Frank W. Nijsen

Metabolite profiling with HPLC-ICP-MS as a tool for in vivo characterization of imaging probes

Current analytical methods for characterizing pharmacokinetic and metabolic properties of positron emission tomography (PET) and single photon emission computed tomography (SPECT) probes are limited. Alternati...

Authors: Eszter Boros, Omar R. Pinkhasov and Peter Caravan

Radiosynthesis and evaluation of an ¹⁸F–labeled silicon containing exendin-4 peptide as a PET probe for imaging insulinoma

Analogues of exendin-4 have been radiolabeled for imaging the glucagon-like peptide type 1 receptors (GLP-1R) which are overexpressed in insulinoma. The aim of this research was to synthesize an ¹⁸F–labeled silic...

Authors: Lukas O. Dialer, Andreas Jodal, Roger Schibli, Simon M. Ametamey and Martin Béhé

Convergent synthesis of ¹³N-labelled Peptidic structures using aqueous [¹³N]NH₃

Nitrogen-13 has a 10-min half-life which places time constraints on the complexity of viable synthetic methods for its incorporation into PET imaging agents. In exploring ways to overcome this limitation, we h...

Authors: Julia E. Blower, Samuel F. Cousin and Antony D. Gee

Generation of fluorescently labeled tracers – which features influence the translational potential?

Given the increasing exploration of fluorescent tracers in the field of nuclear medicine, a need has risen for practical development guidelines that can help improve the translation aspects of fluorescent trac...

Authors: Fijs W. B. van Leeuwen, Bart Cornelissen, Federico Caobelli, Laura Evangelista, Latifa Rbah-Vidal, Silvana Del Vecchio, Catarina Xavier, Jacques Barbet and Marion de Jong

Production and separation of ⁴³Sc for radiopharmaceutical purposes

The favorable decay properties of ⁴³Sc and ⁴⁴Sc for PET make them promising candidates for future applications in nuclear medicine. An advantage ⁴³Sc (T_1/2 = 3.89 h, Eβ⁺ _av = 476 keV [8...

Authors: Katharina A. Domnanich, Robert Eichler, Cristina Müller, Sara Jordi, Vera Yakusheva, Saverio Braccini, Martin Behe, Roger Schibli, Andreas Türler and Nicholas P. van der Meulen

Improving the stability of ¹¹C–labeled L-methionine with ascorbate

Carbon-11 labeled L-methionine (¹¹C–MET) is a popular tracer used in the clinic for imaging brain tumors with positron emission tomography. However, the stability of ¹¹C–MET in its final formulation is not well d...

Authors: Michael Woods, Leo Leung, Kari Frantzen, Jennifer G. Garrick, Zhengxing Zhang, Chengcheng Zhang, Wade English, Don Wilson, François Bénard and Kuo-Shyan Lin

Position statement on radiopharmaceutical production for clinical trials

The EU regulation 536/2014 aims to facilitate the experimental use of diagnostic radiopharmaceuticals in particular for GMP requirements and needs to be applied in EU countries. As definitely clarified by this...

Authors: G. Bormans, A. Buck, A. Chiti, M. Cooper, J. Croasdale, M. Desruet, V. Kumar, Y. Liu, I. Penuelas, C. Rossetti, R. Schiavo, S. W. Schwarz and A. D. Windhorst

Comparing the use of radiolabeled SSTR agonists and an SSTR antagonist in breast cancer: does the model choice influence the outcome?

Authors: Simone U. Dalm and Marion de Jong

An efficient preparation of labelling precursor of [¹¹C]L-deprenyl-D₂ and automated radiosynthesis

The synthesis of [¹¹C]L-deprenyl-D₂ for imaging of astrocytosis with positron emission tomography (PET) in neurodegenerative diseases has been previously reported. [¹¹C]L-deprenyl-D₂ radiosynthesis requires a pre...

Authors: Kevin Zirbesegger, Pablo Buccino, Ingrid Kreimerman, Henry Engler, Williams Porcal and Eduardo Savio

Sulfur - fluorine bond in PET radiochemistry

The importance of the sulfur-fluorine bond is starting to increase in modern medicinal chemistry literature. This is due to a better understanding of the stability and reactivity of this moiety depending on th...

Authors: Giancarlo Pascali, Lidia Matesic, Bo Zhang, Andrew T. King, Andrea J. Robinson, Alison T. Ung and Benjamin H. Fraser

Guidance on validation and qualification of processes and operations involving radiopharmaceuticals

Validation and qualification activities are nowadays an integral part of the day by day routine work in a radiopharmacy. This document is meant as an Appendix of Part B of the EANM “Guidelines on Good Radiopha...

Authors: S. Todde, P. Kolenc Peitl, P. Elsinga, J. Koziorowski, V. Ferrari, E. M. Ocak, O. Hjelstuen, M. Patt, T. L. Mindt and M. Behe

Pretargeting for imaging and therapy in oncological nuclear medicine

Oncological pretargeting has been implemented and tested in several different ways in preclinical models and clinical trials over more than 30 years. Despite highly promising results, pretargeting has not achi...

Authors: Clément Bailly, Caroline Bodet-Milin, Caroline Rousseau, Alain Faivre-Chauvet, Françoise Kraeber-Bodéré and Jacques Barbet

An updated radiosynthesis of [¹⁸F]AV1451 for tau PET imaging

[¹⁸F]AV1451 is a commonly used radiotracer for imaging tau deposits in Alzheimer’s disease (AD) and related non-AD tauopathies. Existing radiosyntheses of [¹⁸F]AV1451 require complex purifications to provide dose...

Authors: Andrew V. Mossine, Allen F. Brooks, Bradford D. Henderson, Brian G. Hockley, Kirk A. Frey and Peter J. H. Scott

⁴⁷Sc as useful β^–-emitter for the radiotheragnostic paradigm: a comparative study of feasible production routes

Radiotheragnostics makes use of the same molecular targeting vectors, labeled either with a diagnostic or therapeutic radionuclide, ideally of the same chemical element. The matched pair of scandium radionucli...

Authors: Katharina A. Domnanich, Cristina Müller, Martina Benešová, Rugard Dressler, Stephanie Haller, Ulli Köster, Bernard Ponsard, Roger Schibli, Andreas Türler and Nicholas P. van der Meulen

Evaluation of agonist and antagonist radioligands for somatostatin receptor imaging of breast cancer using positron emission tomography

The somatostatin receptor subtype 2 (sstr2) is expressed on a majority of luminal breast cancers, however SPECT and scintigraphy imaging with agonistic sstr2 probes has been sub-optimal. High affinity antagoni...

Authors: Iulia Dude, Zhengxing Zhang, Julie Rousseau, Navjit Hundal-Jabal, Nadine Colpo, Helen Merkens, Kuo-Shyan Lin and François Bénard

Synthesis, gallium labelling and characterization of P04087, a functionalized phosphatidylserine-binding peptide

Radiolabeled phosphatidylserine (PS)-binding peptides represent an innovative strategy for molecular imaging of apoptosis and thrombus. The hexapeptide PGDLSR was described as a selective and high affinity lig...

Authors: Rana Ben Azzouna, Alexandre Guez, Khadija Benali, Faisal Al-Shoukr, Walter Gonzalez, Philippe Karoyan, François Rouzet and Dominique Le Guludec

[⁶⁴Cu]NOTA-pentixather enables high resolution PET imaging of CXCR4 expression in a preclinical lymphoma model

The chemokine receptor 4 (CXCR4) is an important molecular target for both visualization and therapy of tumors. The aim of the present study was the synthesis and preclinical evaluation of a ⁶⁴Cu-labeled, CXCR4-t...

Authors: Andreas Poschenrieder, Margret Schottelius, Theresa Osl, Markus Schwaiger and Hans-Jürgen Wester

Nomenclature for radiopharmaceuticals, consultation of your opinion!

Authors: Philip H. Elsinga

Preclinical validations of [¹⁸F]FPyPEGCBT-c(RGDfK): a ¹⁸F-labelled RGD peptide prepared by ligation of 2-cyanobenzothiazole and 1,2-aminothiol to image angiogenesis

α_Vβ₃, α_Vβ₅ and α₅β₁ integrins are known to be involved in carcinogenesis and are overexpressed in many types of tumours compared to healthy tissues; thereby they have been selected as promising therapeutic target...

Authors: Didier J. Colin, James A. H. Inkster, Stéphane Germain and Yann Seimbille

Automation of the Radiosynthesis of Six Different ¹⁸F-labeled radiotracers on the AllinOne

Fast implementation of positron emission tomography (PET) into clinical and preclinical studies highly demands automated synthesis for the preparation of PET radiopharmaceuticals in a safe and reproducible man...

Authors: Shihong Li, Alexander Schmitz, Hsiaoju Lee and Robert H. Mach

Bone targeting compounds for radiotherapy and imaging: *Me(III)-DOTA conjugates of bisphosphonic acid, pamidronic acid and zoledronic acid

Bisphosphonates have a high adsorption on calcified tissues and are commonly used in the treatment of bone disorder diseases. Conjugates of bisphosphonates with macrocyclic chelators open new possibilities in ...

Authors: M. Meckel, R. Bergmann, M. Miederer and F. Roesch

Strategies to facilitate the discovery of novel CNS PET ligands

Positron Emission Tomography (PET), as a non-invasive translatable imaging technology, can be incorporated into various stages of the CNS drug discovery process to provide valuable information for key preclini...

Authors: Lei Zhang and Anabella Villalobos

Are we “preparing” radiopharmaceuticals?

Authors: Clemens Decristoforo and Marianne Patt

18th European Symposium on Radiopharmacy and Radiopharmaceuticals

OP03 Selective extraction of medically-related radionuclides from proton-irradiated thorium targets

Authors: 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, Chuangyan Zhai, Gerben M. Franssen, Milos Petrik, Peter Laverman, Clemens Decristoforo, Ait-Mohand Samia…

New protein deposition tracers in the pipeline

Traditional nuclear medicine ligands were designed to target cellular receptors or transporters with a binding pocket and a defined structure–activity relationship. More recently, tracers have been developed t...

Authors: Aleksandar Jovalekic, Norman Koglin, Andre Mueller and Andrew W. Stephens

Optimizing labelling conditions of ²¹³Bi-DOTATATE for preclinical applications of peptide receptor targeted alpha therapy

²¹³Bismuth (²¹³Bi, T_1/2 = 45.6 min) is one of the most frequently used α-emitters in cancer research. High specific activity radioligands are required for peptide receptor radionuclide...

Authors: Ho Sze Chan, Erik de Blois, Mark W. Konijnenberg, Alfred Morgenstern, Frank Bruchertseifer, Jeffrey P. Norenberg, Fred J. Verzijlbergen, Marion de Jong and Wouter A. P. Breeman

⁴⁴Sc for labeling of DOTA- and NODAGA-functionalized peptides: preclinical in vitro and in vivo investigations

Recently, ⁴⁴Sc (T_1/2 = 3.97 h, Eβ⁺ _av = 632 keV, I = 94.3 %) has emerged as an attractive radiometal candidate for PET imaging using DOTA-functionalized biomolecules. The aim of this st...

Authors: Katharina A. Domnanich, Cristina Müller, Renata Farkas, Raffaella M. Schmid, Bernard Ponsard, Roger Schibli, Andreas Türler and Nicholas P. van der Meulen

Improved GMP-compliant multi-dose production and quality control of 6-[¹⁸F]fluoro-L-DOPA

6-[¹⁸F]Fluoro-L-3,4-dihydroxyphenylalanine (FDOPA) is a frequently used radiopharmaceutical for detecting neuroendocrine and brain tumors and for the differential diagnosis of Parkinson’s disease. To meet the dem...

Authors: G. Luurtsema, H. H. Boersma, M. Schepers, A. M. T. de Vries, B. Maas, R. Zijlma, E. F. J. de Vries and P. H. Elsinga

Improved radiolabeling of DOTATOC with trivalent radiometals for clinical application by addition of ethanol

Typically, metal-based radiopharmaceuticals are synthesized in aqueous solutions with no or low ethanol content. Labeling yields are defined by temperature, period of labeling, amount of precursor, pH etc. As ...

Authors: Elisabeth Eppard, Marylaine Pèrez-Malo and Frank Rösch

Alpha-PET with terbium-149: evidence and perspectives for radiotheragnostics

¹⁴⁹Tb represents a powerful alternative to currently used α-emitters: the relatively short half-life (T_1/2 = 4.1 h), low α-energy (3.97 MeV, I_α = 16.7 %), absence of α-emitting daughters ...

Authors: Cristina Müller, Christiaan Vermeulen, Ulli Köster, Karl Johnston, Andreas Türler, Roger Schibli and Nicholas P. van der Meulen

Striatal phosphodiesterase 10A availability is altered secondary to chronic changes in dopamine neurotransmission

Phosphodiesterase 10A (PDE10A) is an important regulator of nigrostriatal dopamine (DA) neurotransmission. However, little is known on the effect of alterations in DA neurotransmission on PDE10A availability. ...

Authors: Maarten Ooms, Sofie Celen, Ronald De Hoogt, Ilse Lenaerts, Johnny Liebregts, Greet Vanhoof, Xavier Langlois, Andrey Postnov, Michel Koole, Alfons Verbruggen, Koen Van Laere and Guy Bormans

DATATOC: a novel conjugate for kit-type ⁶⁸Ga labelling of TOC at ambient temperature

The widespread acceptance and application of ⁶⁸Ga-PET depends on our ability to develop radiopharmaceuticals that can be prepared in a convenient and suitable manner. A kit-type labelling protocol provides such c...

Authors: Johanna Seemann, Bradley Waldron, David Parker and Frank Roesch

Position paper on requirements for toxicological studies in the specific case of radiopharmaceuticals

This is a position paper of the Radiopharmacy Committee of the EANM (European Association of Nuclear Medicine) addressing toxicology studies for application of new diagnostic and therapeutic radiopharmaceutica...

Authors: J. Koziorowski, M. Behe, C. Decristoforo, J. Ballinger, P. Elsinga, V. Ferrari, P. Kolenc Peitl, S. Todde and T. L. Mindt

Editorial - EJNMMI radiopharmacy and chemistry

Authors: Philip H. Elsinga