zedoresertib + lunresertib

zedoresertib + lunresertib is an investigational, all-oral combination of two small-molecule kinase inhibitors being developed by Debiopharm for the treatment of advanced solid tumors harboring specific genomic alterations, such as CCNE1 amplification or FBXW7 or PPP2R1A mutations. Zedoresertib (Debio 0123) is a highly selective, brain-penetrant inhibitor of WEE1 kinase, originally in-licensed from Almac Discovery. Lunresertib (Debio 2513, formerly RP-6306) is a first-in-class, selective inhibitor of PKMYT1, discovered by Repare Therapeutics and licensed worldwide to Debiopharm in July 2025. Both WEE1 and PKMYT1 are key cell-cycle checkpoint kinases that regulate CDK1 activity at the G2/M checkpoint. Inhibiting both kinases simultaneously represents a synthetic-lethal strategy that forces DNA-damaged cancer cells into premature mitosis, leading to mitotic catastrophe and apoptosis. The combination is currently being evaluated in the Phase 1 MYTHIC trial (NCT04855656) in patients with advanced solid tumors, including ovarian, colorectal, pancreatic, and breast cancers. The FDA has granted Fast Track designation to the combination for the treatment of genomically defined platinum-resistant or refractory ovarian cancer.

Other names

Debio 0123 + Debio 2513Debio 0123 + lunresertibDebio 0123 + RP-6306Debio 2513 + Debio 0123Debio-0123 + Debio-2513Debio-0123 + RP-6306Debio-2513 + Debio-0123RP-6306 + Debio 0123RP-6306 + Debio-0123RP-6306 + zedoresertiblunresertib + Debio 0123lunresertib + zedoresertiblunresertib and zedoresertibzedoresertib + RP-6306zedoresertib and lunresertib