Venadaparib (IDX-1197) is a potent, selective PARP inhibitor with IC50 of 1.4 nM and 1.0 nM for PARP1 and PARP2, respectively.
IDX-1197 does not inhibits PARP5A (Tankyrase-1, IC50>10 uM), which belongs to the PARP family.
IDX-1197 significantly inhibited PARP1-mediated PAR expression in DNA damage-induced Hela cells.
IDX-1197 exhibits potent tumor growth inhibition in germline BRCA1-mutated ovarian cancer PDX model.
IDX-1197 shows improved antitumor activity against breast cancer PDX models, which included both germline BRCA-mutated and non-germline BRCA-mutated models, compared with olaparib and/or niraparib.
1. Myongjae Lee, et al. Abstract A106: Development of IDX-1197, a novel, selective, and highly potent PARP inhibitor. American Association for Cancer Research, 2018.
