guretolimod

Guretolimod (DSP-0509) is a synthetic, systemically available small molecule that acts as a selective agonist of toll-like receptor 7 (TLR7). It is designed for intravenous administration and features a pyrimidine scaffold distinct from other TLR7 agonists such as imiquimod. Guretolimod stimulates the immune system by activating TLR7, leading to the induction of cytokines including type-I interferons and upregulation of MHC class II expression on dendritic cells. This activation results in enhanced anti-tumor immunity through increased infiltration and activation of CD8+ T cells, NK cells, CD4+ T cells, regulatory T cells (Tregs), monocytes, plasmacytoid dendritic cells (pDCs), and granulocytes within the tumor microenvironment. Guretolimod has demonstrated synergistic anti-tumor effects when combined with immune checkpoint inhibitors such as anti-PD-1 antibodies or with other immunomodulatory agents like IDO1 or AXL inhibitors. The drug was developed primarily for use in advanced malignant solid neoplasms and solid tumors.

Other names

guretolimod