pre-clinical assessment of 177lu-labeled trastuzumab targeting her2 for treatment and management of cancer patients with disseminated intraperitoneal disease177年临床前评估lu-labeled曲妥珠单抗靶向治疗her2和癌症患者腹腔内传播疾病管理.pdf

Pharmaceuticals 2012, 5, 1-15; doi:10.3390/ph5010001 OPEN ACCESS Pharmaceuticals ISSN 1424-8247 /journal/pharmaceuticals Article Pre-Clinical Assessment of 177Lu-Labeled Trastuzumab Targeting HER2 for Treatment and Management of Cancer Patients with Disseminated Intraperitoneal Disease 1 1 1 2 Geoffrey L. Ray , Kwamena E. Baidoo , Lanea M. M. Keller , Paul S. Albert , Martin W. Brechbiel 1 and Diane E. Milenic 1,* 1 Radioimmune and Inorganic Chemistry Section, Radiation Oncology Branch, Center for Cancer Research, National Cancer Institute, National Institutes of Health, Bethesda, MD 20892, USA; E-Mails: x_ray82@ (G.L.R.); baidook@ (K.E.B.); lkeller8@ (L.M.M.K.); martinwb@ (M.W.B.) 2  Biostatistics and Bioinformatics Branch, Division of Epidemiology, Statistics Prevention, Eunice Kennedy Shriver National Institute of Child Health and Human Development, Bethesda, MD 20892, USA; E-Mail: albertp@ (P.S.A.) * Author to whom correspondence should be addressed; E-Mail: milenicd@; Tel.: +1-301-496-9086; Fax: +1-301-402-1923. Received: 4 November 2011; in revised form: 6 December 2011 / Accepted: 14 December 2011 / Published: 22 December 2011 Abstract: Studies from this laboratory have demonstrated the potential of targeting HER2 for therapeutic and imaging applications with medically relevant radionuclides. To expand the repertoire of trastuzumab as a radioimmunoconjugate (RIC) vector, use of 177Lu was investigated. The combination of a 6.7 d half-life, lower