GSK4418959

GSK4418959 (also known as IDE275) is a selective, non-covalent, reversible small-molecule inhibitor of Werner syndrome ATP-dependent helicase (WRN), a member of the RecQ family of DNA helicases. WRN plays a critical role in maintaining genome stability and is particularly essential for the survival of microsatellite instability-high (MSI-H) tumors. By inhibiting WRN's ATPase and DNA unwinding functions, GSK4418959 induces DNA damage selectively in MSI-H tumor models and has demonstrated tumor regression even in models resistant to other WRN-targeting agents. The drug is being developed primarily for use in solid tumors with deficient mismatch repair/microsatellite instability-high status (dMMR/MSI-H), including colorectal cancer, endometrial carcinoma, and rectal cancer[1][3][6][7][9].

Other names

IDE275IDE-275IDE 275GSK-4418959GSK4418959GSK 4418959