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FORX-428 is an orally bioavailable, highly potent and selective small molecule inhibitor of poly(ADP-ribose) glycohydrolase (PARG). It is being developed by FoRx Therapeutics as a targeted anticancer agent, specifically for the treatment of solid tumors. The drug has demonstrated excellent single-agent activity in multiple preclinical tumor models, showing strong anti-tumor efficacy and good tolerability. FORX-428 targets DNA damage response (DDR) pathways by inhibiting PARG, which plays a key role in DNA replication stress—a hallmark of many cancers. Predictive biomarkers have been identified to help select patient populations most likely to benefit from this therapy. As of early 2025, FORX-428 remains in preclinical development with Investigational New Drug (IND) submission anticipated by mid-2025[1][2][3][4][5].
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