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  • A synthetic lipid A derivative and selective toll-like receptor 4 (TLR4) agonist composed of glucopyranosyl lipid-A (GLA) in a stable, oil-in-water emulsion (GLA-SE), with potential immunostimulating and antineoplastic activities. Upon intratumoral administration into the immunosuppressed tumor microenvironment (TME), TLR4 agonist G100 binds to and activates TLR4 on various immune cells, thereby stimulating dendritic cells (DCs), monocytes and macrophages. This activation results in the production of pro-inflammatory cytokines and chemokines. This induces a T helper cell-1 (Th1) immune response and activates a cytotoxic T-lymphocyte (CTL) response against tumor-associated antigens (TAAs) that were released in the TME by tumor cells lysed during cytotoxic treatments, such as radiotherapy. TLR4, a member of the TLR family, plays a key role in the activation of innate immunity. Check for \'https://www.cancer.gov/about-cancer/treatment/clinical-trials/intervention/C113649\' active clinical trials using this agent. (\'http://ncit.nci.nih.gov/ncitbrowser/ConceptReport.jsp?dictionary=NCI%20Thesaurus&code=C113649\' NCI Thesaurus)
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