Tuvusertib — Investigational Agent
Other · Phase 1/2 · EMD Serono / Merck KGaA
Mechanism of Action
Tuvusertib is an oral, selective ATR kinase inhibitor that targets the replication-stress response pathway. By inhibiting ATR, it prevents stabilization of stalled replication forks and abrogates the S/G2 checkpoint, causing catastrophic DNA damage and death in tumor cells with high replication stress or defective DNA damage response. Tuvusertib is being developed both as monotherapy in DDR-altered tumors and in rational combinations with PARP inhibitors and immune checkpoint inhibitors, where ATR inhibition can enhance immunogenicity via cytosolic DNA sensing (cGAS-STING). This makes it…
Investigational Indications
- DDR-deficient ovarian cancer
- Endometrial cancer
- BRCA/ATM-mutant breast cancer
- PARP-inhibitor-resistant solid tumors