[123I]CC1

[123I]CC1 is an experimental PARP-targeting radiopharmaceutical designed for targeted radionuclide therapy (TRT). It consists of a small molecule PARP inhibitor, CC1, radiolabeled with the Auger electron-emitting isotope iodine-123. The agent specifically targets and binds to PARP1, PARP2, and PARP3 enzymes. Its therapeutic efficacy is driven by 'PARP trapping,' a mechanism where the drug stabilizes the PARP-DNA complex, thereby increasing the residence time of the radionuclide on the chromatin. This proximity allows the short-range, high-linear energy transfer (LET) Auger electrons to induce localized, lethal DNA double-strand breaks. Preclinical research has demonstrated potent antitumor activity and DNA damage induction in models of pancreatic cancer, glioblastoma, and breast cancer. The compound is synthesized using a copper-mediated iododeboronation reaction.

Other names

Iodine-123 labeled CC1Iodine123 labeled CC1Iodine 123 labeled CC1