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Cu-64 PCTA-trastuzumab (also referred to as [64Cu]-PCTA-trastuzumab) is an investigational radiolabeled immunoconjugate developed for positron emission tomography (PET) imaging of human epidermal growth factor receptor 2 (HER2) expression. The agent consists of the recombinant humanized monoclonal antibody trastuzumab (commercially known as Herceptin) conjugated to the novel bifunctional chelator 3,6,9,15-tetraazabicyclo[9.3.1]pentadeca-1(15),11,13-triene-3,6,9-triacetic acid (PCTA) and radiolabeled with copper-64 (Cu-64), a positron-emitting radioisotope. By targeting HER2, which is overexpressed in various cancers including breast and gastric malignancies, Cu-64 PCTA-trastuzumab enables non-invasive, high-contrast visualization of HER2-positive tumors. Preclinical studies in mouse models have demonstrated that the PCTA chelator allows for rapid and efficient radiolabeling under mild conditions, yielding superior tumor-to-background ratios and faster renal clearance compared to traditional DOTA-conjugated alternatives.
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