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Nuklearmedizin 2021; 60(05): 375-380
DOI: 10.1055/a-1486-3683
Original Article

Human Absorbed Dose Evaluation of [177Lu]Lu-IBA as a Bone Palliative Candidate

Bewertung der vom Menschen absorbierten Dosis von [177Lu] Lu-IBA als Kandidat für ein Knochenpalliativmittel
Hassan Ranjbar
1   Nuclear Science and Technology Research Institute, Tehran, Iran (the Islamic Republic of)
,
Zahra Pourhabib
2   Payame Noor University, Tehran, Iran (the Islamic Republic of)
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Abstract

The role of lutetium-177 among bone-seeking radionuclides in targeted therapy is noteworthy. The clinical pharmacokinetics of ibandronate (IBA) indicates that this bisphonate has powerful bone mineral affinity. The aim of this study was to evaluate of [177Lu]Lu-IBA efficacy as a new compound.

The [177Lu]Lu-IBA was prepared by radiolabeling of IBA ligand to 177LuCl3 that was obtained by thermal neutron irradiation of enriched Lu2O3 sample. Produced [177Lu]Lu-IBA with high radiochemical purity was administered intravenously to mice. Biodistribution data were collected at 1, 4, 24, 48 h and 7 d post injections. With calculating accumulated activities in each organ and extrapolating mouse’s organs to human’s organs by the RADAR method and using OLINDA/EXM software the injected dose in various human organs was achieved.

[177Lu]Lu-IBA was produced with radiochemical purity nearly 96 %. Its biodistribution data showed the high uptake and durability in the skeletal tissues without significant uptake in other major organs.

The results showed that [177Lu]Lu-IBA has considerably good properties as a bone-seeking radiopharmaceutical and therefore can be a candidate for bone pain palliative therapy in skeletal metastases; however, further biological studies are still needed.

Zusammenfassung

Die Rolle von Lutetium-177 unter den knochensuchenden Radionukliden in der zielgerichteten Therapie ist bemerkenswert. Die klinische Pharmakokinetik von Ibandronat (IBA) deutet darauf hin, dass dieses Bisphosphonat eine starke Affinität zu Knochenmineral besitzt. Das Ziel dieser Studie war es, die Wirksamkeit von [177Lu] Lu-IBA als neue Verbindung zu untersuchen.

[177Lu] Lu-IBA wurde durch Radiomarkierung des IBA-Liganden an 177LuCl3 hergestellt, das durch thermische Neutronenbestrahlung einer angereicherten Lu2O3-Probe gewonnen wurde. Hergestelltes [177Lu] Lu-IBA mit hoher radiochemischer Reinheit wurde Mäusen intravenös verabreicht. Biodistributionsdaten wurden 1, 4, 24, 48 Stunden und 7 Tage nach der Injektion gesammelt. Durch die Berechnung der akkumulierten Aktivitäten in jedem Organ und die Extrapolation der Mäuseorgane auf die Organe des Menschen mittels der RADAR-Methode und unter Verwendung der OLINDA/EXM-Software wurde die injizierte Dosis in verschiedenen menschlichen Organen ermittelt.

[177Lu] Lu-IBA wurde mit einer radiochemischen Reinheit von fast 96 % hergestellt. Seine Biodistributionsdaten zeigten die hohe Aufnahme und Haltbarkeit im Skelettgewebe ohne signifikante Aufnahme in andere wichtige Organe.

Die Ergebnisse zeigten, dass [177Lu] Lu-IBA als knochensuchendes Radiopharmazeutikum beträchtlich gute Eigenschaften aufweist und daher ein Kandidat für eine palliative Knochenschmerztherapie bei Skelettmetastasen sein kann. Weitere biologische Studien sind jedoch noch erforderlich.

Keywords

177Lu-IBA - bone metastases - internal dosimetry - RADAR - OLINDA/EXM - nitrogen containing bisphosphonates

Schlüsselwörter

177 Lu-IBA - Knochenmetastasen - interne Dosimetrie - RADAR - OLINDA/EXM - stickstoffhaltige Bisphosphonate


Publication History

Received: 25 January 2021

Accepted: 18 April 2021

Article published online:
08 June 2021

© 2021. Thieme. All rights reserved.

Georg Thieme Verlag KG
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