Astatine-211 for targeted alpha therapy – current status and future perspectives

Focused Pre-Symposium organized by the COST action NOAR

Thursday, April 18 from 16:00-18:00

Welcome & Introduction by the ESRR local organizers – Antero Abrunhosa

The current status of astatine research, production & clinical trials at brief – Emma Aneheim, COST-NOAR Vice Chair

Scientific presentation 1: “Preparation and evaluation of stabilized 211At-labelled aryl compounds” – Romain Fouinneteau, France
Scientific presentation 2: “Defining a time-yield correlation of two different radiolabelling strategies using Astatine-211 recovered in chloroform after dry distillation” – Ellinor Hansson, Sweden
Scientific presentation 3: “Astatinations via Germanyl Precursors – A new convient labeling method” – Mattias Herth, Denmark
Future perspectives of astatine-211 use within TAT; introducing the World Astatine Community – Jean-François Gestin, COST-NOAR Chair

Scientific Programme – ESRR’24

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Thursday, April 18, 2024

19:30 – 20:30Opening Ceremony & Welcome meeting
Chairpersons: Antero Abrunhosa, Filippo Lodi

AI in chemistry, with focus on data-driven reaction prediciton
Teodoro Laino, Zurich, CH

Friday, April 19, 2024

Sci Session 1Imaging tracers
Chairpersons: Jessica Bridoux, Filipe Elvas
08:30 – 09:15Back-to-basics I: Novel agents and future prespectives
on theranostics
Filipe Elvas, Antwerp, BE
09:15 – 09:27Oral Sessions:
OP01 Improved PET imaging of NETs with [61Cu]-NOTA-TATE: a straightforward comparison with [61Cu]-/[68Ga]-DOTA-TATE
Alexandra  Fonseca, PT
09:27 – 09:39
OP02 Development of SPECT agent [99mTc]Tc-BQ0413 for PSMA visualization: preclinical evaluation and preliminary results of Phase I clinical study 
Anna Orlova, SE
09:39 – 09:51
OP03 Folate-targeted polymeric micelles for image-guided drug delivery of an anticancer gold complex
Joana Santos, PT
09:51-10:03OP04 Development and characterization of 99mTc-scFvD2B as a potential theranostic pair for 177Lu-scFvD2B
Laura  Melendez Alafort , IT
10:05 – 10:35Coffee Break
Sci Session 2Auger and other therapeutic emitters
Chairpersons: Peter Laverman, Samantha Terry
10:35 – 11:20Auger electron therapy
Samantha Terry, London, UK
11:20 – 11:32Oral Sessions:
OP05 111In- and 161Tb-Radioconjugates Carrying PSMA and Triphenylphosphonium Derivatives for Auger Therapy of Prostate Cancer
António Paulo, PT
11:32 – 11:44OP06 Sulfur Symphony: Capturing the Exotic Mercury-197m/g Auger Emitters with Macrocyclic S-Rich Chelators
Marianna Tosato, Italy
11:44 – 11:56OP07 Synthesis and preclinical evaluation of BOLD-100 radiolabeled with ruthenium-97/103
Thomas Mindt, AT
11:56 – 12:08OP08 Nanobioconjugates of 109Pd/109mAg in-vivo generators for targeted Auger electron therapy
Aleksander Bilewicz, PL
12:08 – 12:20

OP09 Synthesis, 68Ga-radiolabelling and in vitro evaluation of a PET/PDT agent for prostate cancer theranostics
Laurène Wagner, UK
12:20 – 13:45Lunch
Sci Session 3New oncological radiotracers
Chairpersons: Sanne van Lith, Ines Farinha Antunes
13:45 – 14:30Improving radioimmunotherapy with immuno/chemotherapy/EBRT
– a winning combination?
Sanne van Lith, Nijmegen, NL
14:30 – 14:42Oral Sessions:
OP10 Structure-based design, optimization and development of [18F]SK60: A Novel PET radioligand for the imaging of mutated Isocitrate Dehydrogenase 
Sarandeep Kaur, DE
14:42 – 14:54OP11 Molecular Imaging of HER2 Expression in Breast Cancer Using DARPin [123I]I-(HE)3-G3. From mice to Phase I.
Vladimir Tolmachev, SE
14:54 – 15:06OP12 Fully automated production of [18F]FB-labeled single-domain antibodies: the immune-checkpoint TIGIT for PET imaging
Herlinde Dierick, BE
15:06 – 15:18OP13 A novel Al18F-labeled radiotracer for in vivo imaging of CXCR4 using positron emission tomography
Muriel Aline Spahn, BE
15:18 – 15:30
OP14 Radioiodinated closo-dicarbadodecaborane(12)-based cyclooxygenase-2/5-lipoxygenase inhibitors
Jonas Schädlich, DE
15:30 – 16:00Coffee Break
Sci Session 4Chairpersons: Martin Behe, Thomas Mindt
16:00 – 16:45Debate: Small molecules vs peptides vs antibodies vs antibody
fragments as vector molecule for theranostic radiopharmaceuticals
Moderator: Frederik Cleeren, Leuven, BE
16:45 – 17:15Poster pitches (order of presentation)

PP34 89Zr-DFO-Atezolizumab for PD-L1 Imaging of Glioblastoma: Clinical Experience
Anna Kastelik-Hryniewiecka

PP43 211At-labeling of trans-cyclooctenes and cis-cyclooctenes with astatine-211 using electrophilic and nucleophilic reactions
Maarten Vanermen

PP46 Manufacturing of investigational medicinal products under GMP conditions using the example of a radiopharmaceutical kit PSMA-T4 for technetium-99m labelling
Anna  Drapsa

PP47 Radionuclidic purity of Ga-68 eluted from Ge-68/Ga-68 generators by Thin Layer Chromatography
Joao Alberto Osso Junior

PP53 Preliminary evaluation of a novel Temozolomide-based molecule  radiolabeled with 99mTc as a theranostic agent against glioblastoma Penelope Bouziotis

PP54 PSMA-targeted Radioconjugates Bearing a DNA Intercalator for Enhanced Auger Therapy of Prostate cancer 
Catarina Dorisa  Silva

PP55 Therapeutic Efficacy of 177Lu-DMSA-SPIONs in a Mouse CT26 and 4T1 Xenograft Model
Dragana Stanković

PP57 Automated production of [68Ga]Ga-deferoxamine on two different synthesis modules for bacterial infection imaging
Martin Kraihammer

PP61 Development of [18F]AlF-RESCA-FSH as a diagnostic probe for ovarian cancer
Maria Kominia

PP63 Using Epin boronic esters as substrates improves the copper-mediated [18F]-fluorination of arenes
Annemarie  Doze
17:15 – 18:00Poster viewing + refreshments

Saturday, April 20, 2024

Sci Session 5Radiochemistry
Chairpersons: Matthias Herth, Verena Pichler
08:30 – 09:15Back-to-basics II: Computational methods in radiopharmaceutical
Verena Pichler, Vienna, AT
09:15 – 09:27Oral Sessions:
OP15 Synthesis, stability determination and radiolabeling of new diazabenzene-based azamacrocycles with barium-131, actinium-225, lanthanum-133, and lead-212
Magdalena Blei, DE
09:27 – 09:39OP16 Evaluation of sydnones-based click chemistry for the labeling with heavy radiohalogens
Ludovic Le Saux, FR
09:39 – 09:51
OP17 From Theory to Clinical Application: Understanding Ac-225 radiochemistry through [225Ac]Ac-DOTA-TATE
Eline  Hooijman, NL
09:51 – 10:05

OP18 Radiolabelling of various macrocyclic ligands using 155Tb/156Tb radioisotopes
Mátyás Fodor, HU
10:05 – 10:35Coffee Break
Sci Session 6New neurological tracers
Chairpersons: Philip Elsinga, Bienke Janssen
10:35 – 11:20Pretargeting strategies, where are we?
Matthias Herth, Copenhagen, DN
11:20 – 11:32Oral Sessions:
OP19 11C-carboxylations using Grignard reactions for the preparation of [carbonyl 11C]WAY-100635 and [1-11C]Sodium Acetate
Vanessa Tomé, PT
11:32 – 11:44OP20 Preclinical evaluation of [11C]HSP990 as novel Hsp90 PET brain probe for in vivo visualization of Hsp90 in healthy aging and neurodegeneration
Romy Cools, BE
11:44 – 11:56OP21 Radiolabeling of M13 bacteriophages for in vivo imaging
Johanna Trommer, DE

11:56 – 12:08
OP22 Synthesis, in vitro and in vivo evaluation of novel radioligands for α-synuclein PET 
Albert D. Windhorst, NL
12:08 – 13:00Workshop: EATRIS EU Tracer Factory
Nadja van Camp
Bert Windhorst
13:00 – 14:00Lunch
Sci Session 7New infection and inflammation tracers
Chairpersons: Aljaz Socan, Jan Rijn Zeevaart
14:00 – 14:42Tracking cells with radiopharmaceuticals: strategies and applications
Aljaž Sočan, Ljubljana, SL
14:42 -14:54

14:54 – 15:06

15:06 – 15:18

15:18 – 15:30
Oral Sessions:
OP23 Repurposing a pharmaceutical development for infection theranostics
Clemens Decristoforo, AT

OP24 Synthesis and preclinical evaluation of novel 18F-vancomycin-based tracers for the detection of bacterial infections using positron emission tomography
Gerbren B. Spoelstra, NL

OP25 Artificial biomimetic Siderophores as PET radiopharmaceuticals: Radiolabelling and evaluation for PET imaging of invasive aspergillosis 
Milos  Petrik, CZ

OP26 [68Ga]Ga-TEoS-DAZA as PET tracer for liver function determination and diagnosis of liver-bile-related diseases
Julia Greiser, DE
15:30 – 16:00Coffee Break
Sci Session 8Chairpersons: Petra Kolenc, Clemens Decristoforo
16:00 – 17:00Round table GMP and Legislation (Annex 1 and 3)

Problems arising from revised Annex 1 for preparation of radiopharmaceuticals
Thijs Kroon, Amsterdam, NL
A pharmacist’s view on practical problems with Annex 1 for PET
Hendrikus Boersma, Groningen, NL
Practical problems with Annex 1 for kit-based Radiopharmaceuticals and how a revision of Annex 3 help with the issues
Neil Hartman, Swansea, UK

Outcome from an ITF EMA meeting of PRISMAP (quality requirements for new radionuclides in clinical trials)
Oliver Kiss, Dresden, DE
Questions from PRISMAP on Annex 3, will it be revised and what can we do?
Clemens Decristoforo, Innsbruck, AT
17:00 – 18:00Pharmacopoeia Corner
Thijs Kroon
Ellen Pel

Sunday, April 21, 2024

Sci Session 9From alpha to beta and back
Chairpersons: Janke Kleynhans, Klaus Kopka
08:30 – 09:15Back-to-basics III: Alpha emitters, from basic physics to labeling and measuring
Janke Kleynhans, Leuven, BE
09:15 – 09:27
Oral Sessions :
OP27 Tumor-targeted alpha therapy using terbium-149 in combination with somatostatin analogues
Cristina Müller, CH
09:27 – 09:39
OP28 Synergistic effects of a combination of trastuzumab-emtansine (T-DM1) and β- radiation (198AuNPs) for targeted HER2+ therapy
Agnieszka Majkowska-Pilip, PL

09:39 – 09:51
OP29 Assessment of cell damage produced by somatostatin analog radiopharmaceuticals labelled with 177Lu or 161Tb
Laura De Nardo, IT
09:51 – 10:05
OP30 Preclinical assessment of enhanced blood retention and tumor uptake PSMA-targeting 225Ac-labeled radioconjugates
Zbynek Novy, CZ
10:05 – 10:35Coffee Break
Sci Session 10Radionuclide production
Chairpersons: Nicholas van der Meulen, Tom Christian Adamsen
10:35 – 10:47
Oral Sessions:
OP31 Terbium-149 production and separation: the latest development update
Nicholas van der Meulen, CH
10:47 – 10:59OP32 155Gd-target enrichment for 155Tb production by low-energy cyclotrons
Francesca Barbaro, IT
10:59 – 11:11OP33 Development of a new technology for the 52Mn-radiopharmaceuticals cyclotron production
Giorgia Speltri, IT
11:11 – 11:23OP34 An alternative production route for the PET radionuclide 61Cu: exploring the 62Ni(p,2n)61Cu nuclear reaction
Santiago Brühlmann, DE
11:25 – 12:15Closing / Awards Ceremony
12:15 – 13:00Farewell Lunch