Development of KSQ-4279 as a first-in-class USP1 inhibitor for the treatment of BRCA-deficient cancers

Background: Drugs targeting poly (ADP-ribose) polymerase (PARP) have provided significant clinical benefit for cancer patients with tumors harboring mutations in BRCA1/2 or other homologous recombination deficiencies (HRD). Despite their success, not all patients respond to PARP inhibitors, and those that do benefit often develop resistance.