177lu-dota-peg-parpi

**177Lu-DOTA-PEG-PARPi** is an experimental radiopharmaceutical designed as a theranostic agent for targeting poly(ADP-ribose) polymerase 1 (PARP-1) in tumors, particularly those with high PARP-1 expression such as pancreatic cancer. The compound consists of a PARP inhibitor (PARPi) moiety conjugated via a polyethylene glycol (PEG) linker to a DOTA chelator, which coordinates with the radioactive isotope lutetium-177 (^177Lu^). This structure enables targeted delivery of beta radiation to PARP-1-expressing tumor cells, exploiting PARP-1’s role in DNA repair and inducing cytotoxicity by causing localized DNA damage. Preclinical studies show high binding affinity for PARP-1, effective tumor uptake, stability in vitro, and moderate tumor growth inhibition in a pancreatic cancer xenograft model, with a favorable biodistribution that supports further development as a targeted radiotherapeutic for cancers with PARP-1 upregulation[3].