Drug intelligence / Profile preview

Pegloprastide

Development stage
Phase 2
Lead developer
Avelas Biosciences
Modality
Light/Condition-Responsive Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Peptides, Recombinant Proteins and Enzymes
Administration
Intravenous
01

Overview

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].

Other names
fluorescent protease-activated peptide AVB-620fluorescent probe - Avelas Biosciencesactivated cell penetrating peptide - Avelas Biosciencesfluorescent peptide conjugate-Avelas Biosciences
02

Targets

MMP12 (Macrophage Metalloelastase)

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