Springe direkt zu Inhalt

Heteromultivalent polymers and antiviral applications thereof

Haag089-P02-V00

Haag089-P02-V00

A new class of linear heteromultivalent polymers bearing both hemagglutinin-binding and neuraminidase-binding ligands blocks influenza A virus attachment and release. These polymers show synergistic antiviral effects superior to monofunctional or nanoparticle analogs.

Detailed Explanation

The invention discloses linear polyglycerol backbones (7.5–12.5 kDa) substituted with sialyllactose or sialic-acid-derived moieties (HA binders) and zanamivir derivatives (NA binders) at ~40 % each. By simultaneously targeting HA-mediated cell attachment and NA-mediated receptor cleavage, these heteromultivalent constructs synergistically inhibit virus entry and egress. In vitro assays (HAI, MUNANA) revealed low-nanomolar IC₅₀ values, outperforming homomultivalent polymers or physical mixtures. Cell‐based and ex vivo human lung‐tissue tests confirmed potent suppression of diverse H1N1 and H3N2 strains, including zanamivir-resistant variants. Toxicology screens showed no cytotoxicity up to 10 μM. These polymers can be formulated for pulmonary or nasal delivery to prevent or treat influenza infections.

 Key Innovation Features and Advantages

  • Dual-ligand display on one polymer backbone yields strong synergistic HA/NA inhibition.
  • Broad activity against H1, H3, H5, H7 serotypes and NA variants, including drug-resistant strains.
  • High water solubility, biocompatibility, and non‐toxic up to 10 μM in cell assays.

 Use Cases

  • Prophylactic nasal spray for high-risk populations during flu season.
  • Therapeutic aerosol for early-stage influenza A treatment.
  • Surface coating for high-contact areas to prevent viral transmission.

 Commercial Opportunities

  • Licensing to pharmaceutical companies for next-generation antiviral inhalers.
  • Co-development with vaccine makers as a combination prophylactic agent.
    • OEM partnerships for antiviral medical devices and hospital-grade disinfectant coatings.

 Current Status

Patent application WO2024200861A1 filed; prototypes synthesized and validated in vitro and ex vivo. Scale-up and GLP toxicology studies are in planning.

Keywords

  • heteromultivalent polymer, influenza A, hemagglutinin inhibitor, neuraminidase inhibitor, polyglycerol, zanamivir, sialyllactose, antiviral