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89Zr-DFO*-trastuzumab is a next-generation positron emission tomography (PET) imaging agent designed to visualize and quantify human epidermal growth factor receptor 2 (HER2) expression in patients with solid tumors, such as breast and gastric cancer. It consists of the anti-HER2 monoclonal antibody trastuzumab conjugated with the positron-emitting radioisotope Zirconium-89 via the improved chelator DFO* (extended desferrioxamine). Preclinical research has demonstrated that DFO* provides superior complexation stability compared to the traditional DFO chelator, which significantly reduces the release of free radiometal and subsequent non-specific uptake in the bone, liver, and spleen. This improved stability results in a higher tumor-to-background ratio, potentially allowing for more accurate non-invasive assessment of HER2 heterogeneity across metastatic sites and helping to identify patients who are likely to benefit from HER2-targeted therapies.
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