The Influence of EDTMP-Concentration on the Biodistribution of Radio-Lanthanides and 225-Ac in Tumor-Bearing Mice

Beyer, G.J.; Offord, Robin E.; Künzi, G.; Aleksandrova, Yulia; Ravn, Ulla; Jahn, S.G.; Barker, James; Tengblad, O.; Lindroos, M.

doi:10.1016/s0969-8051(97)00011-5

Cited by 22 publications

(10 citation statements)

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“…Distinct values of the complex ligands (100-400 nmol) were added to the lutetium-containing vials. By varying pH (2)(3)(4)(5)(6)(7)(8)(9)(10)(11)(12) and temperature (50-100°C), the effect of these parameters was investigated based on ITLC results. For radio thin layer chromatography, a 5 lL sample of the final fraction was spotted on a chromatography Whatman No.…”

Section: Preparation and Quality Control Of 177 Lu-bpamdmentioning

confidence: 99%

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Preparation and biological assessment of 177Lu-BPAMD as a high potential agent for bone pain palliation therapy: comparison with 177Lu-EDTMP

Yousefnia

Zolghadri

Sadeghi

et al. 2015

J Radioanal Nucl Chem

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In this study, 177 Lu-(4-{[(bis(phosphonomethyl))-carbamoyl]methyl}-7,10-bis(carboxymethyl)-1,4,7,10-tetraazacyclododec-1-yl) acetic acid ( 177 Lu-BPAMD) was successfully prepared. The quality control, partition coefficient, hydroxyapatite binding assay and stability of the complex were determined. For better comparison, biodistribution patterns of 177 Lu-BPAMD and 177 Lu-EDTMP complexes were compared in same animal model. 177 Lu-BPAMD was prepared with high radiochemical purity ([93 %) and specific activity of 534 GBq/mmol at the optimal conditions. Comparative study between 177 Lu-BPAMD and 177 Lu-EDTMP indicated higher bone uptake and lesser accumulation in the other organs for 177 Lu-BPAMD. 177 Lu-BPAMD can be considered as a promising agent for bone pain palliation in the near future.

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Section: Preparation and Quality Control Of 177 Lu-bpamdmentioning

confidence: 99%

“…Unfortunately, EDTMP complexes have shown low in vivo stability and thus dissociate which result in liver accumulation and high toxicity [8,9]. In order to prevent complex dissociation, high amounts of EDTMP should be injected ([1.5 mg/kg body weight) [10].…”

Section: Introductionmentioning

confidence: 99%

Preparation and biological assessment of 177Lu-BPAMD as a high potential agent for bone pain palliation therapy: comparison with 177Lu-EDTMP

Yousefnia

Zolghadri

Sadeghi

et al. 2015

J Radioanal Nucl Chem

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“…The influence of varying ethylenediaminetetramethylenephosphonic acid (EDTMP) solution concentrations on the biodistribution of 225 Ac was determined in tumor-bearing mice [29]. Swiss nude mice were implanted with subcutaneous (s.c.) T380 human colon carcinoma and injected i.v.…”

Section: Biological Studies In Animal Modelsmentioning

confidence: 99%

Actinium-225 in Targeted Alpha-Particle Therapeutic Applications

Scheinberg

McDevitt²

2011

CRP

146

114

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Alpha particle-emitting isotopes are being investigated in radioimmunotherapeutic applications because of their unparalleled cytotoxicity when targeted to cancer and their relative lack of toxicity towards untargeted normal tissue. Actinium-225 has been developed into potent targeting drug constructs and is in clinical use against acute myelogenous leukemia. The key properties of the alpha particles generated by 225Ac are the following: i) limited range in tissue of a few cell diameters; ii) high linear energy transfer leading to dense radiation damage along each alpha track; iii) a 10 day half-life; and iv) four net alpha particles emitted per decay. Targeting 225Ac-drug constructs have potential in the treatment of cancer.

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“…Um eine Dissoziation der Komplexe im Blutplasma zu verhindern, wird gleichzeitig eine hohe Menge des nichtkomplexierten Chelators injiziert. Dies allerdings blockiert Bindungsstellen an der Metastasen-Knochenmatrix und führt folglich zu einer geringeren Aufnahme des aktiven Komplexes [2]. Hinzu kommt die getriggerte Produktion des 153 Sm.…”

Section: Diagnostikunclassified

68Ga- und 177Lu-markierte Bisphosphonate als Knochenmetastasen-Theranostika

Pfannkuchen

Meckel

Kubíček³

et al. 2015

Nuklearmediziner

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InstituteDie Institutsangaben sind am Ende des Beitrags gelistet Zusammenfassung ▼ Der erhöhte Metabolismus der Knochenmatrix kann zum einen mit der SPECT-und zum anderen mit der PET-Technik visualisiert werden. Als SPECT-Nuklid wird überwiegend 99 m Tc in Form von [ 99m Tc]Bisphosphonat-Komplexen verwendet. Die PET bietet im Gegensatz zur SPECT eine höhere lokale und temporale Auflösung. Mit dem 68 Ge/ 68 Ga-Generatorsystem existiert ein mittlerweile bewährtes PET-Pendant zum etablierten 99m Tc-Generator. Neuartige Bisphosphonate (BP) in Kombination mit makrozyklischen Chelatoren sind derzeit weltweit Gegenstand der Forschung. Zur Komplexierung von Ga(III) werden häufig DOTA und NOTA sowie deren Derivate verwendet. Speziell im Fall von DOTA-Derivaten bieten DOTA-BP die Möglichkeit, auch 177 Lu stabil zu koordinieren. Dies eröffnet vielversprechende Möglichkeiten für Theranostika: [ 68 Ga]NOTA-BP für die PET/ CT und -im Falle hoher SUV-Werte in den Knochenmetastasen -eine patientenindividuelle Therapie mit 177 Lu-Analoga. Die vorliegende Übersicht beschreibt den aktuellen Stand zur Diagnostik von Knochenmetastasen mit [ 68 Ga]NO2AP BP und [ 68 Ga]BPAMD und die erfolgreiche Anwendung von [ 177 Lu]BPAMD zur Therapie. Die neuen PET-Tracer werden mit [ 99m Tc]MDP und [ 18 F]Fluorid verglichen. Im Zusammenhang mit dem Potenzial von [ 68 Ga] HBED-PSMA zur Visualisierung von Knochenmetastasen werden erstmals Ergebnisse im direkten Vergleich mit [ 68 Ga]NO2AP BP vorgestellt. Im Hinblick auf die Therapie werden die vorliegenden ex-vivo-Daten mit 223 RA diskutiert. Abschließend wird ein Ausblick gegeben auf die laufenden Weiterentwicklungen hin zu neuen 68 Ga-bzw. 177 Lu-markierten Bisphosphonaten mit weiter verbesserten pharmakologischen Eigenschaften. Abstract ▼ Increased bone metabolism can be visualized by PET as well as SPECT. For SPECT, 99m Tc is predominately used as bisphosphonate complex. In contrast to SPECT, PET offers a higher spatial resolution and owing to the 68 Ge/ 68 Ga generator an analog to the established 99m Tc generator exists. Currently, the combination of novel bisphosphonates (BP) and macrocyclic chelators is studied worldwide. For complexation of Ga(III) DOTA, NOTA and their derivatives are often used. DOTA bisphosphonates are also able to coordinate 177 Lu, which offers the possibility of developing theranostics by using [ 68 Ga]NOTA-BP for PET/CT and 177 Lulabeled analogs for an individualized therapy. This overview describes the status quo of diagnosing bone metastases using [ 68 Ga]NO2AP BP and [ 68 Ga]BPAMD as well as the successful application of [ 177 Lu]BPAMD for therapy. The new PET tracers are compared to [ 99m Tc]MDP and [ 18 F] fluoride and results concerning the visualiza tion of bone metastases using [ 68 Ga]NO2AP BP are presented in comparison to [ 68 Ga]HBED-PSMA. In terms of therapy, available ex vivo data is compared to 223 RA .Finally, an outlook is provided on further developments providing new 68 Ga-and 177 Lu-labeled bisphosphonates offering improved pharmacological properties.

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The Influence of EDTMP-Concentration on the Biodistribution of Radio-Lanthanides and 225-Ac in Tumor-Bearing Mice

Cited by 22 publications

References 0 publications

Preparation and biological assessment of 177Lu-BPAMD as a high potential agent for bone pain palliation therapy: comparison with 177Lu-EDTMP

Preparation and biological assessment of 177Lu-BPAMD as a high potential agent for bone pain palliation therapy: comparison with 177Lu-EDTMP

Actinium-225 in Targeted Alpha-Particle Therapeutic Applications

68Ga- und 177Lu-markierte Bisphosphonate als Knochenmetastasen-Theranostika

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