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.
CHAN Ho Sze;
KONIJNENBERG M.W.;
DE BLOIS Erik;
KOELEWIJN S.J.;
ANDERSON Tamara;
NYSUS Monique;
BREEMAN W.A.P.;
ATCHER Robert;
MORGENSTERN Alfred;
BRUCHERTSEIFER Frank;
NORENBERG Jeffrey;
DE JONG Marion;
2015-11-06
SPRINGER
JRC96963
1619-7070,
https://publications.jrc.ec.europa.eu/repository/handle/JRC96963,
10.1007/s00259-015-3198-z,
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