pixatimod

Pixatimod is a synthetic sugar-modified heparan sulfate mimetic and small molecule with immunomodulatory, antineoplastic, and antiviral activities. It acts as an agonist of toll-like receptor 9 (TLR9), stimulating dendritic cells and B cells to initiate cytokine release and activate innate immune pathways, including natural killer (NK) cell activation. Pixatimod also inhibits heparanase activity, preventing the cleavage of heparan sulfate from cell surface proteoglycans, which reduces tumor-associated macrophage infiltration and angiogenesis. In preclinical models, it enhances the effectiveness of PD-1 inhibitors in cancer therapy. Pixatimod has demonstrated direct antiviral effects by binding to viral proteins such as the SARS-CoV‑2 spike protein, disrupting its interaction with ACE2 receptors. The drug is under clinical investigation for advanced cancers including metastatic colorectal cancer (MSS mCRC), malignant melanoma, non-small cell lung cancer (NSCLC), and has been studied in combination with nivolumab.

Other names

pixatimod [INN]PG-545 free acidPG545 free acidPG 545 free acidUNII-66QR34C83NUNII66QR34C83NUNII 66QR34C83N