Fluzoparib (Fuzuloparib, SHR-3162) is a novel, potent and orally available inhibitor of PARP with IC50 of 1.46 nM (PARP1).
Fluzoparib (Fuzuloparib, SHR-3162) potently inhibited PARP1 enzyme activity and induced DNA double-strand breaks, G2/M arrest and apoptosis in homologous recombination repair (H)-deficient cells.
Fluzoparib (Fuzuloparib, SHR-3162) preferentially inhibited the proliferation of HR-deficient cells and sensitized both HR-deficient and HR-proficient cells to cytotoxic drugs.
Fluzoparib (Fuzuloparib, SHR-3162) demonstrates superior anti-tumor activity in HR-deficient xenografts models, elicited significantly improved anti-tumor responses without extra toxicity in combination with apatinib or with apatinib plus paclitaxel.
