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Pegloprastide is an investigational intravenous imaging agent developed for real-time intraoperative cancer detection, particularly during breast cancer surgery. It is designed to deliver a fluorescent marker specifically to cancer cells, enabling surgeons to identify positive margins in real time and potentially reduce the need for repeat surgeries. Pegloprastide utilizes activatable cell-penetrating peptides conjugated with two fluorophores (Cy5 and Cy7), allowing ratiometric fluorescence imaging that improves accuracy by compensating for common artifacts such as variable drug concentration or camera distance. Its mechanism of action involves targeting matrix metalloproteinases (MMPs) that are overexpressed in tumor tissue; upon activation by MMPs, the probe emits a fluorescent signal detectable during surgery. Clinical studies have shown that pegloprastide can significantly improve intraoperative margin assessment without serious drug-related adverse events[1][4][5][6][7][8].
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