WE011

WE011 is an orally bioavailable small molecule inhibitor of poly (ADP-ribose) polymerase (PARP), specifically targeting the PARP1 and PARP2 isoforms. Developed by Shanghai Baolong Pharmaceutical, it is currently in clinical development for the treatment of advanced solid tumors, including breast and ovarian cancers. The drug's mechanism of action involves the inhibition of PARP enzymes, which are critical for the repair of single-strand DNA breaks via the base excision repair pathway. In cells with homologous recombination deficiencies (HRD), such as those harboring BRCA1 or BRCA2 mutations, the inhibition of PARP leads to the conversion of single-strand breaks into double-strand breaks during DNA replication. These double-strand breaks cannot be accurately repaired in HRD-deficient cells, resulting in genomic instability and apoptosis, a therapeutic strategy known as synthetic lethality.