pegylated TOP1 inhibitor PEEL-224

A pegylated camptothecin derivative, with potential antineoplastic activity. Upon administration of pegylated TOP1 inhibitor PEEL-224, camptothecin reaches the tumor cells and selectively stabilizes covalent topoisomerase I-DNA complexes, which results in single-stranded and double-stranded DNA breaks, the inhibition of DNA replication, and the induction of apoptosis. Pegylation allows for increases in half-life and the exposure time for tumor cells, while decreasing both blood plasma concentrations and exposure to off-target organs. This may increase efficacy and reduce systemic toxicities.