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89Zr-ss-pertuzumab is an investigational radiopharmaceutical imaging agent developed for the detection and quantification of human epidermal growth factor receptor 2 (HER2) expression in cancer patients. It consists of the humanized monoclonal antibody pertuzumab labeled with the positron-emitting radioisotope zirconium-89 (89Zr). Unlike standard conjugation methods that result in heterogeneous mixtures, this agent utilize a site-specific (ss) conjugation technique—often chemoenzymatic glycan remodeling—to ensure a uniform product with preserved binding affinity and optimized pharmacokinetics. Pertuzumab specifically targets the extracellular dimerization domain (Domain II) of HER2, preventing the receptor from pairing with other HER family members (such as HER3). This diagnostic tracer is primarily used in positron emission tomography (PET) imaging to assess HER2 status non-invasively, identify metastatic lesions, and evaluate the heterogeneity of HER2 expression to guide therapy in patients with breast and other HER2-positive cancers.
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