Merck's ATR Inhibitor M1774 Granted IND Approval in China for Extensive-Stage Small Cell Lung Cancer

On June 17, according to the CDE official website, the clinical application of Merck KGaA's Class 1 chemical drug M1774 capsule was accepted.

Source: CDE Official Website

M1774 is an ATR inhibitor. ATR is a member of the phosphatidylinositol 3-kinase-related kinase (PIKK) family of serine/threonine protein kinases. The N-terminus of ATR contains a binding site for ATRIP (ATR-interacting protein), which regulates the localization of ATR at sites of replication stress and DNA damage.

Studies have shown that the ATR kinase plays a crucial role in the G2/M phase checkpoint and DNA damage response. Inhibiting ATR has the potential to exacerbate oncogenic stress and promote cell death. Currently, ATR is considered one of the most promising synthetic lethal targets following PARP inhibitors. The drug's approved clinical trial indication in China is for extensive-stage small cell lung cancer.

According to the Insight database, there are currently no ATR inhibitors approved for marketing globally. The clinical progress of ATR inhibitors from AstraZeneca, Merck, and Repare Therapeutics is at the forefront, with products currently in Phase II clinical trials.

In China, besides M1774, there are 6 other ATR inhibitors under development, including 4 domestically produced and 2 imported ones. Among them, the most advanced is Merck KGaA's Berzosertib/M6620, which is currently in Phase II clinical trials.

Six Other ATR Inhibitors Under Development in China

Source: Insight Database (http://db.dxy.cn/v5/home/)