WRN inhibitor GSK4418959

An orally bioavailable inhibitor of the Werner syndrome ATP-dependent helicase (WRN), with potential antineoplastic activity. Upon oral administration, WRN inhibitor GSK4418959 targets, binds to and inhibits the activity of WRN. This may inhibit the growth of susceptible tumor cells, such as ones with high microsatellite instability (MSI-H). WRN, a multifunctional enzyme with both helicase and exonuclease activities, plays a key role in DNA replication and repair. It is overexpressed in a variety of cancer cells.