Evaluation of 99mTc-glucarate as a breast cancer imaging agent in a xenograft animal model

TECNECIO

NEOPLASMA

MEDICINA NUCLEAR

BIBLIOGRAFIA NACIONAL QUIMICA

2011

Introduction: The use of [99mTc]glucarate has been reported as an infarct-avid agent with the potential for very early detection of myocardial infarction. [99mTc]Glucarate has also been postulated as an agent for non-invasive detection of tumors. The aim of our study was to develop a Glucarate kit and evaluate [99mTc]glucarate as a potential cancer imaging agent in female SCID mice bearing humanMDA-MB-435 breast tumors. Methods: Glucarate in a kit formulation was labeled with 99mTc and evaluated for radiolabelling efficiency and radiochemical purity. The Glucarate kit stability was assessed by monthly quality controls. The pharmacokinetics of [99mTc]glucarate were determined in female SCID mice bearing MDA-MB-435 human breast carcinoma tumors at 0.5, 1, 2, 4 and 24 h. Nuclear imaging studies were performed with a microsingle photon emission tomography (SPECT)/computed tomography (CT) system at 2 h post injection, while magnetic resonance imaging (MRI) was employed for tumor morphology analysis and metastatic deposit localization. Results: The Glucarate kits exhibited a stable shelf life of 6 months. [99mTc]Glucarate was obtained with radiochemical purity greater than 95%. Biodistribution studies demonstrated moderate tumor uptake coupled with high renal clearance. Tumor-to-muscle ratios were 4.85 and 5.14 at 1 and 4 h post injection. MRI analysis showed tumors with dense cellular growth and moderate central necrosis. [99mTc]Glucarate uptake in the primary MDA-MB-435 shoulder tumors and metastatic lesions were clearly visualized with micro-SPECT/CT imaging. Conclusions: Selective tumor uptake and rapid clearance from nontarget organs makes [99mTc]glucarate a potential agent for breast cancer imaging that awaits validation in a clinical trial.

Nuclear Medicine and Biology v. 38, no. 2, 2011. -- p. 255-260

Elsevier

2011

 

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doi:10.1016/j.nucmedbio.2010.08.002