Introduction: Auger electron based radioimmunotherapy (RIT) using 111In-DOTA-trastuzumab (111In-DOTA-antiHer2) feasibility was studied in vitro on a HER2/neu positive cell line, SkBr3. Methods: 111In-DOTA-antiHer2 was prepared according to the optimized conditions followed by quality control tests including radiochemical purity; immunoreactivity). SkBr3 as a HER2/neu positive cell line was used...

introduction: auger electron based radioimmunotherapy (rit) using 111in-dota-trastuzumab (111in-dota-antiher2) feasibility was studied in vitro on a her2/neu positive cell line, skbr3. methods:111in-dota-antiher2 was prepared according to the optimized conditions followed by quality control tests including radiochemical purity; immunoreactivity). skbr3 as a her2/neu positive cell line was used ...

Introduction: Auger electron based radioimmunotherapy (RIT) using 111In-DOTA-trastuzumab (111In-DOTA-antiHer2) feasibility was studied in vitro on a HER2/neu positive cell line, SkBr3. Methods:111In-DOTA-antiHer2 was prepared according to the optimized conditions followed by quality control tests including radioch...

BACKGROUND Our objective was to compare 111In- or 64Cu-DOTA-trastuzumab Fab fragments for imaging small or large s.c. tumor xenografts in athymic mice that display a wide range of human epidermal growth factor receptor-2 (HER2) expression using microSPECT/CT or microPET/CT. METHODS Trastuzumab Fab were labeled with 111In or 64Cu by conjugation to 1,4,7,10-tetraazacyclododecane N, N', N'', N''...

Imaging of expression of human epidermal growth factor receptor type 2 (HER2) in breast carcinomas may help to select patients eligible for trastuzumab therapy. The Affibody molecule Z(HER2:342) is a small (7-kDa) non-immunoglobulin affinity protein, which binds to HER2 with a picomolar affinity. Previously, a benzyl-DTPA conjugate of Z(HER2:342) was labeled with 111In and demonstrated good tar...

Overexpression of human epidermal growth factor receptor 3 (HER3) is involved in resistance to several therapies for malignant tumours. Currently, several anti-HER3 monoclonal antibodies are under clinical development. We introduce an alternative approach to HER3-targeted therapy based on engineered scaffold proteins, i.e. affibody molecules. We designed a small construct (22.5 kDa, denoted 3A3...

Scintigraphic imaging of metastatic melanoma lesions requires highly tumor-specific radiolabeled compounds. Because both melanotic and amelanotic melanomas overexpress receptors for -melanocyte–stimulating hormone ( -MSH; receptor name: melanocortin type 1 receptor, or MC1R), radiolabeled -MSH analogs are potential candidates for melanoma diagnosis. The aim of this study was to develop a melano...

In comparison to somatostatin receptor scintigraphy, gastrin receptor scintigraphy using 111In-DTPA-minigastrin (MG0) showed added value in diagnosing neuroendocrine tumors. We investigated whether the 68Ga-labeled gastrin analogue DOTA-MG0 is suited for positron emission tomography (PET), which could improve image quality. Targeting of cholecystokinin-2 (CCK2)/gastrin receptor-positive tumor c...

A majority of melanotic and amelanotic melanomas overexpress melanocortin type 1 receptors (MC1Rs) for α-melanocyte-stimulating hormone. Radiolabeled linear or cyclic analogs of α-MSH have a great potential as diagnostic or therapeutic tools for the management of malignant melanoma. Compounds such as [111In]DOTA-NAP-amide exhibit high affinity for the MC1R in vitro, good tumor uptake in vivo, b...

The thesis is focused on site-specific labeling of affinity molecules for different applications where two types of binding proteins, Affibody molecules and antibodies, have been used. For the purpose of improving the properties of Affibody molecules for in vivo imaging, novel bifunctional chelators for radiolabeling using the radionuclide 111In were evaluated. In a first study, two chelators d...