NCIt definition : 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.;