EB-ss-CPT

EB-ss-CPT is a theranostic agent consisting of an Evans Blue (EB) derivative conjugated to the cytotoxic agent camptothecin (CPT) via a redox-responsive disulfide (ss) linker. The Evans Blue moiety allows the molecule to bind non-covalently to endogenous serum albumin, which significantly extends its circulatory half-life and enhances accumulation in tumor tissues through the enhanced permeability and retention (EPR) effect and albumin-mediated uptake. Once internalized into the tumor microenvironment, the disulfide linker is cleaved by high intracellular concentrations of glutathione (GSH), releasing active camptothecin. Camptothecin subsequently inhibits DNA topoisomerase I, leading to DNA damage and apoptosis. When labeled with positron-emitting isotopes such as Gallium-68 (68Ga) or Copper-64 (64Cu), the compound serves as a PET imaging tracer for the staging and detection of primary and metastatic tumors, including colorectal cancer.

Other names

Evans Blue-disulfide-camptothecin