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Saruparib is an orally bioavailable, potent, and selective inhibitor of poly(ADP-ribose) polymerase 1 (PARP1), with minimal effect on PARP2. It belongs to the class of PARP inhibitors and is being developed primarily for the treatment of various cancers characterized by homologous recombination repair deficiency, such as advanced solid tumors, metastatic castration-sensitive prostate cancer (mCSPC), and hormone receptor-positive/HER2-negative advanced breast cancer with BRCA1/BRCA2 or PALB2 mutations. By selectively inhibiting PARP1, saruparib impairs DNA repair in tumor cells, leading to synthetic lethality in cancers with defective homologous recombination repair mechanisms. This selectivity may offer a safer profile compared to nonselective PARPi and facilitate combination therapies with other DNA damage response inhibitors. Developed by: AstraZeneca
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