Lunresertib (RP-6306) PKMYT1 Inhibitor
Lunresertib is a first-in-class, oral small molecule inhibitor of PKMYT1.
Using our proprietary, CRISPR-based SNIPRx discovery platform, PKMYT1 was identified as a strong synthetic lethal partner to multiple genomic alterations, including CCNE1 amplification and loss of FBXW7 and PPP2R1A function, key genetic drivers in a broad range of cancers. PKMYT1 regulates the cell cycle and is part of DNA damage repair-related signaling.
Lunresertib (RP-6306) is the first PKMYT1 inhibitor to enter clinical trials.
Lunresertib is the first PKMYT1 inhibitor to enter clinical trials.
Initial results from our MYTHIC Phase 1 clinical trial demonstrate safety, tolerability and early efficacy of lunresertib as a monotherapy and in combination with camonsertib, a potent and selective oral inhibitor of ATR. Lunresertib in combination with camonsertib achieved strong anti-tumor activity across multiple tumor types and genotypes, with the strongest anti-tumor activity to date in gynecologic tumors.