acalabrutinib + ceralasertib

Acalabrutinib + ceralasertib is an investigational combination of two orally administered small molecule inhibitors developed for the treatment of cancer. **Acalabrutinib** is a highly selective, irreversible inhibitor of Bruton tyrosine kinase (BTK), which disrupts B-cell receptor signaling, impairs malignant B cell proliferation, and is primarily developed for B-cell malignancies. **Ceralasertib** (AZD6738) is a potent, selective oral inhibitor of ataxia telangiectasia and Rad3-related (ATR) kinase—a key regulator of the DNA damage response pathway—and is designed to sensitize tumor cells to cytotoxic agents and impair DNA repair, particularly in tumors with DNA damage response deficiencies. The combination is being studied to enhance anticancer efficacy by simultaneously targeting B-cell signaling and DNA damage checkpoint pathways. Both drugs are under active clinical development, with AstraZeneca as a principal developer for ceralasertib and acalabrutinib. The combination has been investigated in early-phase clinical trials, including for relapsed/refractory B-cell malignancies.

Brand names

Calquence

Other names

azd6738 + acalabrutinibceralasertib + acalabrutinib