Pixatimod (also known as PG-545) is a synthetic carbohydrate-modified heparan sulfate mimetic and a Toll-like receptor 9 (TLR9) agonist. It exhibits potential immunostimulatory, antitumor, and antiviral effects. Pixatimod effectively inhibits SARS-CoV-2 by disrupting the spike protein-ACE2 interaction. Additionally, it blocks various cancer-promoting processes such as cell proliferation, invasion, metastasis, angiogenesis, and epithelial-mesenchymal transition. These effects have demonstrated significant efficacy in numerous mouse cancer models, including about 30 xenograft models and 20 syngeneic models. Pixatimod has been tested in combination with several approved anticancer compounds, showing clinical potential when used with gemcitabine, paclitaxel, sorafenib, platinum compounds, and anti-PD-1 antibodies.