NCIt definition : An orally bioavailable inhibitor of the nuclear enzyme poly(ADP-ribose) polymerase
(PARP), with potential chemo/radiosensitizing and antineoplastic activities. Upon
administration, saruparib selectively targets and binds to PARP and prevents PARP-mediated
DNA repair of single-strand DNA breaks via the base-excision repair pathway. This
enhances the accumulation of DNA strand breaks and promotes genomic instability and
eventually leads to apoptosis. This may enhance the cytotoxicity of DNA-damaging agents.
PARP catalyzes post-translational ADP-ribosylation of nuclear proteins that signal
and recruit other proteins to repair damaged DNA and is activated by single-strand
DNA breaks. The PARP-mediated repair pathway is dysregulated in a variety of cancer
cell types.;