PD-L1 ATR inhibitor antibody-drug conjugate

This antibody-drug conjugate (ADC) consists of a monoclonal antibody targeting Programmed death-ligand 1 (PD-L1) conjugated to a proprietary small-molecule inhibitor of Ataxia telangiectasia and Rad3-related kinase (ATR). Developed by Repare Therapeutics, the agent is designed to selectively deliver the ATR inhibitor payload to tumor cells expressing PD-L1, thereby inducing synthetic lethality in cancers with high replication stress or DNA repair defects. ATR is a master regulator of the DNA damage response (DDR), essential for stabilizing replication forks and facilitating DNA repair. By utilizing an ADC approach, the developer aims to bypass the dose-limiting systemic toxicities often associated with oral ATR inhibitors. Preclinical data indicates that the ATR inhibitor payload retains potency even in cells resistant to Topoisomerase 1 inhibitors (like exatecan) and demonstrates robust efficacy in models of stomach, breast, lung, and colon cancers.

Other names

PD-L1-targeted ATR inhibitor ADCPD-L-1-targeted ATR inhibitor ADCPD-L 1-targeted ATR inhibitor ADC