Articles

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