Undisclosed PKMYT1 inhibitor / Arcus Biosciences - LARVOL DELTA

PKMYT1 inhibition is synthetically lethal with CCNE1 overexpression and synergizes with standard of care chemotherapy (AACR 2026) - "The data presented here strongly support targeting CCNE1-high cancer cells with a combination of PKMYT1 inhibition and chemotherapy. CCNE1-high cancer cells, which accumulate DNA damage in S phase due to a dysregulated G1/S checkpoint, are highly susceptible to PKMYT1 inhibition due to the propagation of this increased DNA damage into mitosis. Additionally, chemotherapies targeting S/G2 phases, including nucleoside analogs and topoisomerase inhibitors, combine with PKMYT1 inhibition by further enhancing replication stress."

Synthetic lethality • Colorectal Cancer • Oncology • Solid Tumor • CCNE1 • FBXW7 • PKMYT1