Saruparib (AZD5305) is a potent, selective, orally active PARP1 inhibitor (IC50=3 nM) and PARP1-DNA trapper.
AZD5305 is highly selective for PARP1 over other PARP family members (PARP2 IC50=1.4 uM), with good secondary pharmacology and physicochemical properties and excellent pharmacokinetics in preclinical species.
AZD5305 reduced effects on human bone marrow progenitor cells in vitro, showed excellent in vivo efficacy in a BRCA mutant HBCx-17 PDX model.
