lunresertib (Debio 2513)

lunresertib (Debio 2513) is a novel PKMYT1 inhibitor that has demonstrated encouraging results across multiple clinical trials in difficult-to-treat solid tumors. Licensed from Repare Therapeutics, lunresertib (formerly RP-6306) is a first-in-class, selective and potent, oral small molecule inhibitor of PKMYT1, a cancer target discovered and identified as synthetically lethal with CCNE1 amplification, FBXW7 and PPP2R1A alterations in solid tumors. Currently, the sole PKMYT1 inhibitor known to be in clinical trials, the compound has presented positive initial Phase 1 data from its ongoing Phase 1 MYTHIC trial (NCT04855656), demonstrating proof of concept for lunresertib alone and in combination.