Title: The next step in increasing the efficacy of PRRT: Preclinical studies in vicvo and in vitro with 213Bi-[DOTA0,Tyr3]-octreotate
Authors: CHAN Ho SzeKONIJNENBERG M.w.DE BLOIS ErikKOELEWIJN S.j.ANDERSON TamaraNYSUS MoniqueBREEMAN W.a.p.ATCHER RobertMORGENSTERN AlfredBRUCHERTSEIFER FrankNORENBERG JeffreyDE JONG Marion
Citation: EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING vol. 42 no. S1 p. S203 ; OP489
Publisher: SPRINGER
Publication Year: 2015
JRC N°: JRC96963
ISSN: 1619-7070
URI: http://publications.jrc.ec.europa.eu/repository/handle/JRC96963
DOI: 10.1007/s00259-015-3198-z
Type: Articles in periodicals and books
Abstract: Peptide Receptor RadioTherapy shows a reasonable objective response rate of 30-35% with the use of 177Lu-[DOTA0,Tyr3]-octreotate (177Lu-DOTATATE). Alpha-particle emitters can augment the therapeutic efficacy of PRRT and make it exceptional, especially in small tumours and metastasis cell clusters. In preclinical studies with alpha-emitter labeled peptides high specific activity is required, because of the high-affinity, but low-capacity of tumour cell receptors. The stability of -radiopeptides should be maintained until receptor mediated uptake, both in vivo as in vitro , to minimize off-targeting effects. Also the radio-peptide should have rapid uptake ,high retention in tumour tissue and high clearance capacity from normal tissue. In this study we optimized the application of 213Bi-[DOTA0,Tyr3]-octreotate (213Bi-DOTATATE) for TAT in vitro and in vivo. We investigated in various somatostatin receptor-positive tumour models in mice the therapeutic efficacy of 213Bi-DOTATATE. The labelling procedure for 213Bi-DOTATATE was chemically optimized for preclinical applications.
JRC Directorate:Nuclear Safety and Security

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