peposertib

Peposertib is an orally bioavailable, potent, and selective small molecule inhibitor of DNA-dependent protein kinase (DNA-PK). It acts by blocking the non-homologous end joining (NHEJ) repair pathway for DNA double-strand breaks (DSBs), thereby preventing tumor cells from repairing damage caused by ionizing radiation or chemotherapeutic agents. This inhibition sensitizes cancer cells to chemo- and radiotherapy, enhancing cytotoxicity and promoting tumor cell death. Peposertib is being developed primarily as an antineoplastic agent in combination with other therapies for various solid tumors, including rectal cancer, pancreatic cancer, cholangiocarcinoma, gallbladder cancer, small cell lung cancer, and others. The drug has been investigated in multiple phase I/II clinical trials but has not received orphan drug status[1][2][4][5][6][7].

Other names

1637542-33-6