Pixatimod (also known as PG-545) is a synthetic modified heparan sulfate mimetic and an agonist of Toll-like receptor 9 (TLR9), showcasing potential immunostimulatory, antitumor, and antiviral properties. It effectively inhibits SARS-CoV-2 by disrupting the interaction between the spike protein and ACE2. Moreover, Pixatimod blocks cancer-promoting processes such as cell proliferation, invasion, metastasis, angiogenesis, and epithelial-mesenchymal transition. These activities have demonstrated significant efficacy across various murine cancer models, including approximately 30 xenograft models and 20 syngeneic models. Pixatimod has been tested in combination with several approved anticancer compounds, underscoring its clinical potential, with drugs like gemcitabine, paclitaxel, sorafenib, platinum-based compounds, and an anti-PD-1 antibody.