In vitro in vivo studies in Balb-c and nude mice of a new sup(177)Lu-bombesin analog developed for prostate tumor diagnosis and treatment

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2009

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INTERNATIONAL NUCLEAR ATLANTIC CONFERENCE; MEETING ON NUCLEAR APPLICATIONS, 9th; MEETING ON REACTOR PHYSICS AND THERMAL HYDRAULICS, 16th; MEETING ON NUCLEAR INDUSTRY, 1st
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In this work we describe the radiolabeling with 177Lu and some properties of the novel bombesin analog BBNp6 – DOTA-X-BBN(6-14), where X is a spacer of six aminoacids. Bombesin (BBN) is an analog of human gastrin releasing peptide (GRP) isolated from the skin of the frog Bombina bombina in 1970. Development of radiolabeled BBN derivatives as agents for diagnostic imaging and systemic radiotherapy has increased considerable because of the observation that GRP receptors (GRPr) are over-expressed in a variety of human tumor cells, such as prostate tumor cells. 177Lu-labeled peptides are attractive due to the excellent radiophysical properties and commercial availability of the radiometal. BBNp6 was labeled with high yield after reacting with 92.5 MBq of 177LuCl3 at 90 °C for 30 minutes and this mixture kept stable for more than 96 hours at 4 ºC and 1 hour in human plasma. In vivo studies showed a multicompartimental distribution model with fast blood clearance, mainly performed by renal pathway. In addition, 177Lu-BBNp6 showed high affinity for PC-3 tumor xenografts, but not for pancreas and intestine (GRP positive tissues), suggesting its specificity and usefulness for prostate tumor treatment. Moreover, scintigraphic images showed that this derivative can also be a tool in this tumor diagnosis. So, BBNp6 is a promising radiopharmaceutical for prostate tumor imaging and treatment.

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PUJATTI, PRISCILLA B.; SANTOS, JOSEFINA S.; COUTO, RENATA M.; SUZUKI, MIRIAM F.; MENGATTI, JAIR; ARAUJO, ELAINE B. de. In vitro in vivo studies in Balb-c and nude mice of a new sup(177)Lu-bombesin analog developed for prostate tumor diagnosis and treatment. In: INTERNATIONAL NUCLEAR ATLANTIC CONFERENCE; MEETING ON NUCLEAR APPLICATIONS, 9th; MEETING ON REACTOR PHYSICS AND THERMAL HYDRAULICS, 16th; MEETING ON NUCLEAR INDUSTRY, 1st, September 27 - October 2, 2009, Rio de Janeiro, RJ. Proceedings... Disponível em: http://repositorio.ipen.br/handle/123456789/13219. Acesso em: 20 Mar 2026.
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