EIK1005

EIK1005 is a small molecule inhibitor of WRN (Werner syndrome ATP-dependent helicase), an enzyme involved in DNA damage repair. It is being developed by Eikon Therapeutics for the treatment of cancers characterized by high microsatellite instability (MSI-high) and other DNA repair–deficient tumors. WRN has emerged as a promising therapeutic target for these tumor types, including certain gastrointestinal and endometrial cancers. By inhibiting WRN, EIK1005 aims to exploit synthetic lethality in cancer cells with defective mismatch repair mechanisms, leading to selective cancer cell death while sparing normal cells. As of early 2025, EIK1005 is in Phase 1 clinical trials[1][2][4][6][9].