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HH102007 is a highly selective and potent small molecule inhibitor and DNA trapper of poly (ADP-ribose) polymerase 1 (PARP1) developed by Haihe Biopharma. It is designed to selectively target PARP1 over PARP2 to minimize the hematological toxicities, such as myelosuppression, commonly associated with non-selective first-generation PARP inhibitors. In preclinical studies, HH102007 demonstrated superior selectivity for PARP1 compared to other next-generation inhibitors like AZD5305 and AZD9574. It showed robust anti-tumor efficacy and induced tumor regression in BRCA-mutated breast cancer models (such as MDA-MB-436 xenografts) both as a monotherapy and in synergistic combination with carboplatin, while maintaining a favorable hematological safety profile in animal models.
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