ceralasertib

Ceralasertib is an orally available, potent, and selective small molecule inhibitor of ataxia telangiectasia and Rad3-related (ATR) kinase. By inhibiting ATR, a master regulator of the DNA damage response (DDR), ceralasertib blocks downstream phosphorylation events such as activation of CHK1, leading to impaired DNA damage checkpoint activation, disruption of DNA repair processes, and induction of tumor cell apoptosis. It is being developed primarily as an anticancer agent for use alone or in combination with other therapies—including chemotherapy agents like paclitaxel or carboplatin and immunotherapies such as durvalumab (anti-PD-L1 antibody). Ceralasertib has demonstrated activity in various solid tumors including non-small cell lung cancer (NSCLC), gastric cancer, ovarian cancer, melanoma, breast cancer (including triple negative), prostate cancer, pancreatic cancer, cholangiocarcinoma, osteosarcoma, gynaecological cancers and others. The drug is under investigation in multiple clinical trials across phases I–III for these indications[1][2][3][4][5][6][7].

Other names

ceralasertib