Ceralasertib — Investigational Agent
Other · Phase 3 · AstraZeneca
Mechanism of Action
Ceralasertib is an oral, selective small-molecule inhibitor of ataxia telangiectasia and Rad3-related (ATR) kinase, a master regulator of the DNA damage response at stalled replication forks and single-strand breaks. By inhibiting ATR, ceralasertib abrogates cell-cycle checkpoint activation (via CHK1) in tumor cells carrying high replication stress or defects in complementary repair pathways (e.g. ATM loss, p53 dysfunction), driving mitotic catastrophe and cell death (synthetic lethality). It also modulates the tumor immune microenvironment, providing a rationale for combination with PD-L1…
Investigational Indications
- Non-small cell lung cancer (NSCLC) after prior anti-PD-(L)1 and platinum therapy (with durvalumab)
- Melanoma (with durvalumab)
- ATM-deficient or DDR-altered solid tumors (with olaparib)
- Other advanced solid tumors with high replication stress