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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.

We have a number of synthetic lethal therapies in development.