ceralasertib + olaparib

Ceralasertib + olaparib is a combination of two small molecule inhibitors used in oncology clinical trials, particularly for the treatment of cancers with DNA repair deficiencies. Ceralasertib is an oral, selective inhibitor of ataxia telangiectasia and Rad3-related protein (ATR), a key regulator in the DNA damage response pathway. Olaparib is an oral poly(ADP-ribose) polymerase (PARP) inhibitor that impairs single-strand DNA break repair. The combination aims to exploit synthetic lethality by simultaneously inhibiting ATR and PARP pathways, thereby enhancing tumor cell death—especially in tumors with homologous recombination deficiency or resistance to prior PARP inhibitor therapy. This regimen has shown activity in high-grade serous ovarian cancer, platinum-sensitive recurrent ovarian cancer, ATM-mutated tumors, and pediatric cancers with DNA repair defects[2][4][5][6][8]. Both drugs are developed by AstraZeneca.

Brand names

Lynparza (for olaparib)

Other names

AZD6738 + olaparibceralasertib + olaparib