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HSK40495 is a potent, highly selective, next-generation small molecule inhibitor of poly(ADP-ribose) polymerase 1 (PARP1) developed by Haisco Pharmaceutical. It exhibits greater than 5000-fold selectivity for PARP1 over PARP2, which is designed to minimize the hematological toxicities (such as myelosuppression) commonly associated with first-generation, non-selective PARP inhibitors like talazoparib. In preclinical studies, HSK40495 has demonstrated robust anti-proliferative activity in homologous recombination repair-deficient (HRD) and BRCA-mutated cancer models, including breast and colorectal cancers, while showing improved hematopoietic safety in bone marrow progenitor cells. It is being developed for the treatment of HRD-positive cancers.
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