TY - JOUR
T1 - [177Lu]pertuzumab
T2 - Experimental therapy of HER-2-expressing xenografts
AU - Persson, Mikael
AU - Gedda, Lars
AU - Lundqvist, Hans
AU - Tolmachev, Vladimir
AU - Nordgren, Hans
AU - Malmström, Per Uno
AU - Carlsson, Jörgen
N1 - Copyright:
Copyright 2008 Elsevier B.V., All rights reserved.
PY - 2007/1/1
Y1 - 2007/1/1
N2 - Pertuzumab (Omnitarg) is a novel antibody against HER-2, domain II. HER-2 is a tyrosine kinase receptor that is overexpressed in several carcinomas, especially breast cancer. Pertuzumab, labeled with the low-energy β emitter 177Lu, might be a candidate for targeted radiotherapy of disseminated HER-2-positive micrometastases. The radiolabeled antibody [ 177Lu]pertuzumab showed favorable targeting properties in BALB/c (nu/nu) mice with HER-2-overexpressing xenografts. The absorbed dose in tumors was more than five times higher than the absorbed dose in blood and more than seven times the absorbed dose in any other normal organ. Experimental therapy showed that [177Lu]pertuzumab delayed tumor progression compared with controls (no treatment, P < 0.0001; nonlabeled pertuzumab antibody, P < 0.0001; and 177Lu-labeled irrelevant antibody, P < 0.01). No adverse side effects of the treatment could be detected. Thus, the experimental results support the planning of clinical studies applying [177Lu] pertuzumab for therapy.
AB - Pertuzumab (Omnitarg) is a novel antibody against HER-2, domain II. HER-2 is a tyrosine kinase receptor that is overexpressed in several carcinomas, especially breast cancer. Pertuzumab, labeled with the low-energy β emitter 177Lu, might be a candidate for targeted radiotherapy of disseminated HER-2-positive micrometastases. The radiolabeled antibody [ 177Lu]pertuzumab showed favorable targeting properties in BALB/c (nu/nu) mice with HER-2-overexpressing xenografts. The absorbed dose in tumors was more than five times higher than the absorbed dose in blood and more than seven times the absorbed dose in any other normal organ. Experimental therapy showed that [177Lu]pertuzumab delayed tumor progression compared with controls (no treatment, P < 0.0001; nonlabeled pertuzumab antibody, P < 0.0001; and 177Lu-labeled irrelevant antibody, P < 0.01). No adverse side effects of the treatment could be detected. Thus, the experimental results support the planning of clinical studies applying [177Lu] pertuzumab for therapy.
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U2 - 10.1158/0008-5472.CAN-06-2363
DO - 10.1158/0008-5472.CAN-06-2363
M3 - Article
C2 - 17210714
AN - SCOPUS:33846417642
VL - 67
SP - 326
EP - 331
JO - Journal of Cancer Research
JF - Journal of Cancer Research
SN - 0008-5472
IS - 1
ER -