Repare Therapeutics & Debiopharm Announce First Patient Dosed in Phase 1/1b MYTHIC Trial Evaluating the Synthetic Lethal Combination of PKMYT1 and WEE1 Inhibition - Seite 2

About Lunresertib

Lunresertib (RP-6306) is a first-in-class, selective and potent oral small molecule inhibitor of PKMYT1, a cancer target Repare discovered and identified as synthetic lethal with CCNE1 amplification, FBXW7 and PPP2R1A alterations in solid tumors. Lunresertib is currently the sole PKMYT1 inhibitor known to be in clinical trials and is being evaluated alone and in combinations across several studies in the US, UK/EU4, and Canada. Repare has presented positive initial Phase 1 data from its ongoing Phase 1/1b MYTHIC trial (NCT04855656) demonstrating proof of concept for lunresertib alone and in combination. In addition to being well tolerated and having a compelling safety profile, Repare presented anti-tumor activity for lunresertib in combination with camonsertib, an ATR inhibitor developed by Repare, expanded clinical studies for which are ongoing.

About Debio 0123

Debio 0123 is an oral, brain-penetrant, highly selective WEE1 kinase inhibitor. WEE1 is a key regulator of the G2/M and S phase checkpoints, activated in response to DNA damage and replication stress, allowing cells to repair their DNA before resuming their cell cycle. WEE1 inhibition, particularly in combination with DNA damaging agents, induces an accumulation of DNA damage and pushes the cells through cell cycle without DNA repair, promoting mitotic catastrophe and induction of apoptosis in cancer cells. Debio 0123 is currently being investigated in clinical trials in patients with solid tumors as a monotherapy and in combination. Debio 0123 is being developed to address high unmet needs of patients living with the burden of difficult-to-treat cancers.

About Repare Therapeutics, Inc.

Repare Therapeutics is a leading clinical-stage precision oncology company enabled by its proprietary synthetic lethality approach to the discovery and development of novel therapeutics. The Company utilizes its genome-wide, CRISPR-enabled SNIPRx platform to systematically discover and develop highly targeted cancer therapies focused on genomic instability, including DNA damage repair. The Company’s pipeline includes lunresertib (also known as RP-6306), a PKMYT1 inhibitor currently in Phase 1/2 clinical development; camonsertib (also known as RP-3500), a potential leading ATR inhibitor currently in Phase 1/2 clinical development; RP-1664, a Phase 1 PLK4 inhibitor program; RP-3467, a preclinical Polθ ATPase inhibitor program; as well as additional, undisclosed preclinical programs. For more information, please visit reparerx.com.