RLY-2139

RLY-2139 is a selective small molecule inhibitor of cyclin-dependent kinase 2 (CDK2) developed by Relay Therapeutics. It was designed as a targeted oncology therapy for the treatment of HR+/HER2- breast cancer and other solid tumors where CDK2 activity contributes to cell cycle dysregulation or resistance to existing therapies, such as CDK4/6 inhibitors. The compound was part of Relay's broader breast cancer franchise, utilizing their Dynamo platform to optimize selectivity for CDK2 over other cyclin-dependent kinases. In October 2023, Relay Therapeutics announced a strategic decision to pause the development of RLY-2139 to prioritize resources for its more advanced clinical programs and extend its operating runway. Consequently, the drug's development is currently suspended at the preclinical stage.