Abstract: Cyclic guanosine monophosphate-adenosine monophosphate synthase (cGAS)-stimulator of interferon genes (STING)signaling pathway is critical for sensing abnormal accumulation of DNA in the cytoplasm. cGAS binds to abnormal DNA to generate a second messenger circular dinucleotide. Circular dinucleotide activates the downstream STING, which induces the expression of inflammatory cytokines such as type I interferon, and initiates an immune response. cGAS-STING signaling pathway performs an important immune function in resisting pathogen infection and anti-tumor. Therefore, the discovery of drugs targeting this signaling pathway is of great value in clinical application. This review summarizes the latest research on cGAS-STING signaling pathway and drugs targeting this signaling pathway, so as to provide theoretical basis and practical reference for further development of targeted drugs from cGAS-STING pathway-related inhibitors and agonists.