Breast cancer (BC) is a cancer that is prevalent in women. However, the heterogeneity of BC in patients, especially triple-negative breast cancer (TNBC), leads to cases with poor outcomes, which requires more efficient treatment approaches. AZD6738, also known as ceralasertib, a selective inhibitor of Ataxia telangiectasia and Rad3-related (ATR) kinase, can be used for cancer treatment. In clinical practice, it is often used in combination with other drugs or chemotherapy to enhance treatment efficacy. ATR kinase is activated during DNA damage, affecting the cell cycle and responding to DNA replication stress (RS) by activating CHK1 and a series of downstream reactions. AZD6738 can block the ATR pathway by inhibiting the activation of CHK1, thereby inducing cancer cell apoptosis. Moreover, researchers conducted clinical studies on AZD6738 and explored the efficacy of its combination therapy with other drugs, such as PARP inhibitor olaparib. This review focuses on the structure and function of AZD6738, as well as its applications in TNBC clinical trials. Future studies of AZD6738 are required to further explore the mechanisms and clinical applications in the treatment of breast cancer and other cancers.
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