||||||||||IDE161 / Ideaya Biosci IDE161, a potential first-in-class clinical candidate PARG inhibitor, selectively targets homologous-recombination-deficient and PARP inhibitor resistant breast and ovarian tumors (Section 13; Poster Board #1) - Mar 14, 2023 - Abstract #AACR2023AACR_8590; Moreover, studies in cell lines, tumors and tissues revealed that dose and time-dependent accumulation of PAR chains serves as a robust proximal pharmacodynamic biomarker indicative of PARG target engagement. IDE161 is a novel targeted therapy that exploits the synthetic lethal relationship between PARG and genomic instability, thus leading to selective anti-proliferative effects in tumors harboring defects in the HR pathway.
||||||||||Undisclosed PARG inhibitor / Ideaya Biosci [VIRTUAL] Synthetic lethality of PARG inhibition in tumors with homologous recombination deficiencies () - Mar 13, 2021 - Abstract #AACR2021AACR_4463; Furthermore, inhibition of cell proliferation by PARGi is antagonized by PARPi, which is consistent with an on-target cellular mechanism of action (MOA). In conclusion, PARGi induces significant accumulation of PAR chains and decreases cell proliferation both in vitro and in vivo in HR-deficient tumor cells.