Background: The STimulator of INterferon Genes (STING) plays an essential role in the innate immune system by inducing the expression of type I interferons (IFNs) and inflammatory cytokines upon sensing cytosolic DNA. Although modulating STING has shown promise as a potential treatment for cancers and inflammatory and autoimmune diseases in substantial pre-clinical studies, current preliminary clinical results of STING agonists have demonstrated limited anti-tumor efficacy. Currently, there is ongoing R&D targeting STING and focusing on the delivery of next-generation therapeutics. Whereas no comprehensive analysis on the STING patent landscape has been conducted to fill the gap between basic research progress and drug development and commercialization. Aim of review: This study summarized the current agents in the clinical stage and global patenting profiles to help identify the current status, development trends, and emerging technologies of the nascent field of STING modulation. Key scientific concepts of review: Rapidly increasing R&D efforts and outcomes targeting STING were indicated by the recently increasing number and pharmacologic classes of drug candidates in clinic as well as in emergent technological patenting activities. Despite the overall fragmental ownership of patents, several pioneers that have advanced the clinical evaluation of novel STING agonists have established the basis of STING-relevant inventions through their influential patents in the field. These patents also facilitated progress on novel STING modulators, relevant delivery systems, pharmaceutical compositions, and combination strategies with the potential for further enhancing therapeutic outcomes by targeting STING.