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PEG-talazoparib (PLX376) is a long-acting prodrug of talazoparib, a potent poly(ADP-ribose) polymerase (PARP) inhibitor. It is designed for intravenous administration, potentially every two weeks, to maintain therapeutic levels of talazoparib within its known therapeutic window. The drug is being developed by ProLynx for oncology indications. Its mechanism of action involves the active component, talazoparib, which inhibits PARP enzymes, particularly PARP1 and PARP2. This inhibition leads to the trapping of PARP on damaged DNA, interfering with DNA repair processes and ultimately causing cell death, especially in cancer cells with homologous recombination deficiencies, such as those with BRCA1/2 mutations.
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